The ocular drug delivery system is one of the very important drug delivery systems, in this ppt, I tried to add all-important recent advancements of ocular drug delivery systems. ocular drug delivery system involves the entrapment of immunologically isolated cells with hollow fibers or microcapsules. Certainly, further considerations should be made with the most efficacious combinations of optimal drugs, dose, route, and drug release pattern (sustained-release, pulsatile-release, or controlled-release responding to a trigger) according to the pathophysiology and progressive courses of the targeted disease.
The document discusses ocular drug delivery and barriers to drug permeation in the eye. It describes the anatomy of the eye and mechanisms of drug absorption through corneal and non-corneal routes. The major barriers to ocular drug delivery are precorneal drainage, blinking, lacrimation, and barriers posed by the cornea, conjunctiva, sclera, blood-ocular barriers, and physiological factors. Methods to overcome these barriers include alternative delivery routes like intravitreal injections and novel drug delivery systems providing controlled release and improved permeability. Conventional systems like solutions, suspensions, and ointments have limitations like poor bioavailability and frequent dosing that novel particulate and vesicular systems aim to address.
Ophthalmic drug delivery system :Challenges and Approaches.Ashish Kumar Mishra
This presentation mainly cover all the challenges which the pharmaceuticals scientist are facing in formulation of an ocular drug delivery system and the method involved to overcomes the problems and provided an more stable and convenient ODDS with increased Bio-availability.
The document discusses ocular drug delivery systems. It begins with an introduction to ocular drug delivery and the need for such systems given barriers to drug permeation in the eye. It then covers eye anatomy and physiology, classification of various ocular drug delivery systems including conventional and vesicular systems, methods to overcome barriers like penetration enhancers, and ideal characteristics of ocular delivery systems. Evaluation of these systems is also mentioned.
This document discusses various ocular drug delivery systems. It begins by outlining conventional systems like solutions, suspensions, emulsions and ointments/gels. It notes advantages like ease of use but also disadvantages like short residence time. Vesicular systems like liposomes, niosomes and pharmacosomes are described as able to better target drug delivery to the eye. Controlled release systems such as implants, iontophoresis, dendrimers and nanotechnology approaches are also summarized as ways to sustain drug effects. The document provides an overview of considerations and examples for different ophthalmic formulations.
This document discusses ocular drug delivery systems. It begins by introducing the need for ocular drug delivery and routes of administration to the eye. It then describes the anatomy and barriers of the eye. The document outlines various traditional and advanced ocular drug delivery systems including solutions, suspensions, ointments, inserts, and vesicular systems like liposomes and niosomes. It discusses factors influencing drug absorption in the eye and characteristics of ideal ocular drug delivery formulations. The trends in ocular drug delivery include controlled release systems like implants and iontophoresis.
The document discusses ocular drug delivery systems. It describes the anatomy and physiology of the eye and factors that influence drug absorption through the cornea. Various ocular drug delivery formulations are discussed including solutions, suspensions, emulsions, ointments, polymeric solutions, and particulate/vesicular systems. Recent advances include bioadhesive systems, collagen shields, pseudolatices, and penetration enhancers. Ocular inserts provide sustained drug release and increased bioavailability. Evaluation methods for these systems include in vitro drug release and in vivo studies in animals.
The document discusses ocular drug delivery and barriers to drug permeation in the eye. It describes the anatomy of the eye and mechanisms of drug absorption through corneal and non-corneal routes. The major barriers to ocular drug delivery are precorneal drainage, blinking, lacrimation, and barriers posed by the cornea, conjunctiva, sclera, blood-ocular barriers, and physiological factors. Methods to overcome these barriers include alternative delivery routes like intravitreal injections and novel drug delivery systems providing controlled release and improved permeability. Conventional systems like solutions, suspensions, and ointments have limitations like poor bioavailability and frequent dosing that novel particulate and vesicular systems aim to address.
Ophthalmic drug delivery system :Challenges and Approaches.Ashish Kumar Mishra
This presentation mainly cover all the challenges which the pharmaceuticals scientist are facing in formulation of an ocular drug delivery system and the method involved to overcomes the problems and provided an more stable and convenient ODDS with increased Bio-availability.
The document discusses ocular drug delivery systems. It begins with an introduction to ocular drug delivery and the need for such systems given barriers to drug permeation in the eye. It then covers eye anatomy and physiology, classification of various ocular drug delivery systems including conventional and vesicular systems, methods to overcome barriers like penetration enhancers, and ideal characteristics of ocular delivery systems. Evaluation of these systems is also mentioned.
This document discusses various ocular drug delivery systems. It begins by outlining conventional systems like solutions, suspensions, emulsions and ointments/gels. It notes advantages like ease of use but also disadvantages like short residence time. Vesicular systems like liposomes, niosomes and pharmacosomes are described as able to better target drug delivery to the eye. Controlled release systems such as implants, iontophoresis, dendrimers and nanotechnology approaches are also summarized as ways to sustain drug effects. The document provides an overview of considerations and examples for different ophthalmic formulations.
This document discusses ocular drug delivery systems. It begins by introducing the need for ocular drug delivery and routes of administration to the eye. It then describes the anatomy and barriers of the eye. The document outlines various traditional and advanced ocular drug delivery systems including solutions, suspensions, ointments, inserts, and vesicular systems like liposomes and niosomes. It discusses factors influencing drug absorption in the eye and characteristics of ideal ocular drug delivery formulations. The trends in ocular drug delivery include controlled release systems like implants and iontophoresis.
The document discusses ocular drug delivery systems. It describes the anatomy and physiology of the eye and factors that influence drug absorption through the cornea. Various ocular drug delivery formulations are discussed including solutions, suspensions, emulsions, ointments, polymeric solutions, and particulate/vesicular systems. Recent advances include bioadhesive systems, collagen shields, pseudolatices, and penetration enhancers. Ocular inserts provide sustained drug release and increased bioavailability. Evaluation methods for these systems include in vitro drug release and in vivo studies in animals.
The document discusses ocular drug delivery systems. It begins with an agenda that outlines the objectives and topics to be covered, including the anatomy and physiology of the eye, factors affecting intraocular bioavailability, and various approaches and classifications of ocular drug delivery systems. The document then provides details on the anatomy of the eye, mechanisms of ocular absorption, factors that influence drug availability in the eye, and different approaches to improve ocular bioavailability such as using viscosity enhancers, penetration enhancers, prodrugs, and mucoadhesives. It also describes various types of ocular delivery systems including solutions, suspensions, gels, ointments, inserts, and intraocular implants and injections.
Implants are cylindrical, monolithic devices of millimeter or centimeter dimensions, implanted into the subcutaneous or intramuscular tissue by an minor surgical incision or injected through a large bore needle; and release the incorporated drug in a controlled manner, allowing the adjustment of release rates over extended periods of time, ranging from several days up to one year.
The eye is the most interesting organ due to its drug
disposition characteristics.
▪ The Novel approach of drug delivery system in which
the drug that can be Instilled on the cull de sac cavity of the eye is
known as the Ocular drug delivery system.
(cull de sac cavity: the space between eyelids and eye
balls)
▪Ocular drug delivery is one of the most challenging
tasks faced by Pharmaceutical researchers.
▪One of the major barriers of ocular medication is to
obtain and maintain a therapeutic level at the site of
action for a prolonged period of time.
▪The bioavailability of ophthalmic drugs is very poor
due to efficient protective mechanisms of the eye.
The document discusses ocular drug delivery systems. It begins by outlining the composition of tear fluid and how drugs administered via the eye are typically absorbed. It then categorizes various ocular drug delivery systems including conventional, vesicular, particulate, and implant-based systems. Specific examples like liposomes, niosomes, ocular inserts and implants are described in further detail. Key advantages and disadvantages of different systems are provided. Testing parameters for ocular thin films are also listed.
Ocular inserts are sterile solid or semisolid preparations designed to prolong the residence time of drugs in the eye through controlled release over extended periods of time. There are two main types - non-erodible inserts like Ocusert which use a drug-filled reservoir surrounded by a rate-controlling membrane, and erodible inserts that gradually dissolve in the eye releasing drug. Examples include Lacriserts, SODI, and Minidisc inserts. Ocular inserts can provide several advantages over eye drops like increased contact time, reduced dosing requirements, and better drug efficacy and patient compliance.
ODDS (Ocular Drug Delivery Systems) provide novel approaches for instilling drugs onto the eye's surface or inside the eye. Common ODDS include gels, ointments, microspheres, and nanoparticles, and they offer benefits like increased dosing accuracy, sustained drug release, and improved ocular bioavailability. However, they also present disadvantages such as inability to stop treatment during emergencies and potential interference with vision. The eye has multiple barriers that limit drug penetration, including the tear film, cornea, conjunctiva, sclera, and blood-retinal barrier. Physical methods like iontophoresis, sonophoresis, and microneedles can enhance drug transport across these barriers. A
The document discusses ocular inserts, which are thin, solid or semi-solid drug-impregnated devices placed in the eye to provide prolonged drug delivery. It defines ocular inserts and describes different types including soluble, insoluble, and erodible inserts. Applications include treatments for glaucoma, infections, and inflammation. Advantages are prolonged contact time and drug release, while disadvantages include potential loss or irritation. The document outlines manufacturing methods and innovations in ocular insert technologies and drug delivery to the eye.
Barriers and routes of occular drug delivery systemShresthaPandey1
The document discusses various barriers to ocular drug delivery and routes to overcome these barriers. The key barriers include anatomical barriers like the cornea and conjunctiva, physiological barriers like tear turnover and drainage, and blood-ocular barriers. Methods to improve bioavailability and provide controlled drug delivery include adjusting viscosity, using prodrugs, penetration enhancers, and ocular inserts. Inserts can be non-erodible like Ocusert or erodible like Lacriserts, SODI, and Mindisc to continuously deliver drugs to the eye.
This document discusses ocular drug delivery systems. It begins with an introduction defining ocular drug delivery and noting the challenges in overcoming barriers in the eye. It then describes the anatomy and barriers of the eye, including physiological barriers like tear turnover and anatomical barriers like the cornea. Finally, it discusses various methods to improve bioavailability and control drug delivery, such as using viscosity enhancers, ointments, gels, and nanoparticles. The overall purpose is to explore how to effectively deliver drugs to the eye by overcoming its protective barriers.
The document provides an overview of ocular drug delivery systems. It discusses the anatomy and physiology of the eye, routes of drug delivery to the eye, factors affecting drug absorption, and barriers to drug permeation. It then describes various ocular drug delivery formulations including conventional systems like solutions, suspensions, emulsions and ointments as well as vesicular systems like liposomes and niosomes. The document also discusses particulate systems using micro and nanoparticles and various controlled release systems like implants, inserts and iontophoresis.
Contents
Introduction
Objective
Anatomy of the Eye
Routes of drug delivery of the eye
Mechanism of ocular absorption
Factors affecting intra-ocular bioavailability
Barriers of ocular drug absorption
Methods to overcome drug barriers
Evaluation
Conclusion
Reference
Ocular administration of drug is primarily associated with the need to treat ophthalmic diseases.
Applied topically to the cornea, or instilled in the space between the eyeball and lower eyelid
Definition: Ocular DDS are designed to instilled on to topical or intra-ocular or peri-ocular to eye.
Most commonly used ocular dosage forms-
- Solutions
- Suspensions
- ointments
Ideal ophthalmic drug delivery must be able to sustain the drug release and to remain in the vicinity of front of the eye for prolong period of time.
The document discusses ocular drug delivery systems. It provides an overview of eye anatomy and the various routes of ocular drug administration including topical, subconjunctival, and intravitreal. It describes barriers to ocular drug delivery such as drug loss from the eye surface and blood-ocular barriers. Methods to overcome these barriers include viscosity adjustment, prodrugs, penetration enhancers, and various controlled release systems like inserts, implants, and microparticulates. Evaluation of ocular drug delivery systems is also mentioned.
ocular barriers and methods to overcome barriersTarun Gollapudi
This document summarizes barriers to ocular drug delivery and methods to overcome them. The major barriers include ocular surface barriers like the cornea, ocular wall barriers like the sclera, retinal barriers, the vitreous body, lachrymal fluid, and properties of the drug itself like solubility and molecular weight. Methods to enhance delivery include microneedles, ultrasound, iontophoresis, periocular routes, and intravitreal injections. Various ophthalmic formulations are also discussed like eye drops, gels, ointments, and inserts that utilize approaches like prodrugs, penetration enhancers, and nanoparticle carriers to improve ocular bioavailability.
The document discusses ocular drug delivery systems. It begins with an introduction to eye anatomy and factors affecting drug absorption in the eye. It then describes various ophthalmic formulations like solutions, suspensions, and ointments. It discusses advances in controlled release ocular systems including inserts, contact lenses, and nanoparticles to prolong drug release. Finally, it outlines new approaches in ocular drug delivery research focusing on combining technologies for targeted and sustained drug delivery to the eye.
This document discusses different types of controlled drug delivery systems. It classifies systems as rate preprogrammed, activation modulated, or feedback regulated. Rate preprogrammed systems are further broken down into polymer membrane permeation controlled systems, polymer matrix diffusion controlled systems, and microreservoir partition controlled systems. The key aspects and release kinetics of each system type are described through examples. Factors that influence drug release rates from these systems include membrane thickness, drug solubility, diffusivity, and partitioning coefficients.
Intrauterine & Intravaginal Drug Delivery SystemPRASHANT DEORE
This document discusses intrauterine and intravaginal drug delivery systems. It begins with an introduction and overview of anatomy and physiology of the female reproductive system. It then describes various types of intravaginal drug delivery systems including suppositories, bioadhesive semisolids, elastomeric rings, and solid polymeric carriers. Factors affecting vaginal drug absorption are also discussed. The document concludes by describing intrauterine drug delivery systems including non-hormonal and hormonal IUDs, and discussing advantages and disadvantages of both intravaginal and intrauterine systems.
ADVANCED APPROACHES OF OCULAR DRUG DELIVERY SYSTEMSyeda Amena
The document discusses ocular drug delivery systems. It begins with an introduction and overview of eye anatomy and physiology. It then covers the mechanisms of ocular absorption and barriers to drug delivery in the eye. Various routes of administration and types of ocular drug delivery systems are described, including advantages and disadvantages. Recent formulation trends include particulate systems, iontophoresis, and dendrimers. Evaluation methods both in vitro and in vivo are also discussed. The document concludes with the potential of combining drug delivery technologies to improve ocular drug absorption.
Implant : Challenging Drug Delivery Systembiniyapatel
This document discusses implantable drug delivery systems. Implants provide controlled delivery of drugs over long periods of time at the site of implantation. There are biodegradable and non-biodegradable implants. Implants can be classified based on their release mechanism, such as membrane permeation controlled, matrix diffusion controlled, or activation modulated systems. Implants offer benefits like continuous drug delivery and avoidance of peak concentrations but have disadvantages like requiring surgery and host reactions. Common applications of implants include cancer treatment, contraception, and ocular diseases.
This document discusses ocular drug delivery systems. It begins by describing the anatomy of the human eye and then discusses mechanisms of ocular absorption. There are various pathways and factors that can affect intraocular bioavailability. Controlled release systems are then described as they can provide accurate dosing, increased shelf life, and prolonged drug delivery. Various types of ocular controlled release systems are classified including non-erodible, erodible, nanoparticle, and liposome systems. Recent advances in ocular drug delivery technologies are also mentioned such as gels, prodrugs, and mucoadhesive polymers.
This document summarizes recent advances in ocular drug delivery systems. It describes the anatomy of the eye and various barriers to drug delivery. It discusses both conventional and advanced delivery methods including topical drops, intravitreal injections, implants, nanoparticles, and contact lenses. It also covers factors that influence drug absorption and challenges with ocular drug delivery such as short contact time, drainage, and barriers to posterior segment delivery. Polymeric systems, mucoadhesives, and penetration enhancers are presented as approaches to overcoming these challenges.
This document discusses ocular drug delivery systems. It begins with an introduction to why these systems were developed to treat eye diseases locally without causing irritation. It then describes the physiology and common diseases of the eye. Various ocular drug delivery systems are outlined, including viscous solutions, hydrogels, mucoadhesive formulations, liposomes, nanoparticles, and implants. The advantages of these systems are that they increase contact time, allow accurate dosing and controlled drug release to reduce side effects. In conclusion, these novel delivery systems provide more effective treatment of eye diseases.
The document discusses ocular drug delivery systems. It begins with an agenda that outlines the objectives and topics to be covered, including the anatomy and physiology of the eye, factors affecting intraocular bioavailability, and various approaches and classifications of ocular drug delivery systems. The document then provides details on the anatomy of the eye, mechanisms of ocular absorption, factors that influence drug availability in the eye, and different approaches to improve ocular bioavailability such as using viscosity enhancers, penetration enhancers, prodrugs, and mucoadhesives. It also describes various types of ocular delivery systems including solutions, suspensions, gels, ointments, inserts, and intraocular implants and injections.
Implants are cylindrical, monolithic devices of millimeter or centimeter dimensions, implanted into the subcutaneous or intramuscular tissue by an minor surgical incision or injected through a large bore needle; and release the incorporated drug in a controlled manner, allowing the adjustment of release rates over extended periods of time, ranging from several days up to one year.
The eye is the most interesting organ due to its drug
disposition characteristics.
▪ The Novel approach of drug delivery system in which
the drug that can be Instilled on the cull de sac cavity of the eye is
known as the Ocular drug delivery system.
(cull de sac cavity: the space between eyelids and eye
balls)
▪Ocular drug delivery is one of the most challenging
tasks faced by Pharmaceutical researchers.
▪One of the major barriers of ocular medication is to
obtain and maintain a therapeutic level at the site of
action for a prolonged period of time.
▪The bioavailability of ophthalmic drugs is very poor
due to efficient protective mechanisms of the eye.
The document discusses ocular drug delivery systems. It begins by outlining the composition of tear fluid and how drugs administered via the eye are typically absorbed. It then categorizes various ocular drug delivery systems including conventional, vesicular, particulate, and implant-based systems. Specific examples like liposomes, niosomes, ocular inserts and implants are described in further detail. Key advantages and disadvantages of different systems are provided. Testing parameters for ocular thin films are also listed.
Ocular inserts are sterile solid or semisolid preparations designed to prolong the residence time of drugs in the eye through controlled release over extended periods of time. There are two main types - non-erodible inserts like Ocusert which use a drug-filled reservoir surrounded by a rate-controlling membrane, and erodible inserts that gradually dissolve in the eye releasing drug. Examples include Lacriserts, SODI, and Minidisc inserts. Ocular inserts can provide several advantages over eye drops like increased contact time, reduced dosing requirements, and better drug efficacy and patient compliance.
ODDS (Ocular Drug Delivery Systems) provide novel approaches for instilling drugs onto the eye's surface or inside the eye. Common ODDS include gels, ointments, microspheres, and nanoparticles, and they offer benefits like increased dosing accuracy, sustained drug release, and improved ocular bioavailability. However, they also present disadvantages such as inability to stop treatment during emergencies and potential interference with vision. The eye has multiple barriers that limit drug penetration, including the tear film, cornea, conjunctiva, sclera, and blood-retinal barrier. Physical methods like iontophoresis, sonophoresis, and microneedles can enhance drug transport across these barriers. A
The document discusses ocular inserts, which are thin, solid or semi-solid drug-impregnated devices placed in the eye to provide prolonged drug delivery. It defines ocular inserts and describes different types including soluble, insoluble, and erodible inserts. Applications include treatments for glaucoma, infections, and inflammation. Advantages are prolonged contact time and drug release, while disadvantages include potential loss or irritation. The document outlines manufacturing methods and innovations in ocular insert technologies and drug delivery to the eye.
Barriers and routes of occular drug delivery systemShresthaPandey1
The document discusses various barriers to ocular drug delivery and routes to overcome these barriers. The key barriers include anatomical barriers like the cornea and conjunctiva, physiological barriers like tear turnover and drainage, and blood-ocular barriers. Methods to improve bioavailability and provide controlled drug delivery include adjusting viscosity, using prodrugs, penetration enhancers, and ocular inserts. Inserts can be non-erodible like Ocusert or erodible like Lacriserts, SODI, and Mindisc to continuously deliver drugs to the eye.
This document discusses ocular drug delivery systems. It begins with an introduction defining ocular drug delivery and noting the challenges in overcoming barriers in the eye. It then describes the anatomy and barriers of the eye, including physiological barriers like tear turnover and anatomical barriers like the cornea. Finally, it discusses various methods to improve bioavailability and control drug delivery, such as using viscosity enhancers, ointments, gels, and nanoparticles. The overall purpose is to explore how to effectively deliver drugs to the eye by overcoming its protective barriers.
The document provides an overview of ocular drug delivery systems. It discusses the anatomy and physiology of the eye, routes of drug delivery to the eye, factors affecting drug absorption, and barriers to drug permeation. It then describes various ocular drug delivery formulations including conventional systems like solutions, suspensions, emulsions and ointments as well as vesicular systems like liposomes and niosomes. The document also discusses particulate systems using micro and nanoparticles and various controlled release systems like implants, inserts and iontophoresis.
Contents
Introduction
Objective
Anatomy of the Eye
Routes of drug delivery of the eye
Mechanism of ocular absorption
Factors affecting intra-ocular bioavailability
Barriers of ocular drug absorption
Methods to overcome drug barriers
Evaluation
Conclusion
Reference
Ocular administration of drug is primarily associated with the need to treat ophthalmic diseases.
Applied topically to the cornea, or instilled in the space between the eyeball and lower eyelid
Definition: Ocular DDS are designed to instilled on to topical or intra-ocular or peri-ocular to eye.
Most commonly used ocular dosage forms-
- Solutions
- Suspensions
- ointments
Ideal ophthalmic drug delivery must be able to sustain the drug release and to remain in the vicinity of front of the eye for prolong period of time.
The document discusses ocular drug delivery systems. It provides an overview of eye anatomy and the various routes of ocular drug administration including topical, subconjunctival, and intravitreal. It describes barriers to ocular drug delivery such as drug loss from the eye surface and blood-ocular barriers. Methods to overcome these barriers include viscosity adjustment, prodrugs, penetration enhancers, and various controlled release systems like inserts, implants, and microparticulates. Evaluation of ocular drug delivery systems is also mentioned.
ocular barriers and methods to overcome barriersTarun Gollapudi
This document summarizes barriers to ocular drug delivery and methods to overcome them. The major barriers include ocular surface barriers like the cornea, ocular wall barriers like the sclera, retinal barriers, the vitreous body, lachrymal fluid, and properties of the drug itself like solubility and molecular weight. Methods to enhance delivery include microneedles, ultrasound, iontophoresis, periocular routes, and intravitreal injections. Various ophthalmic formulations are also discussed like eye drops, gels, ointments, and inserts that utilize approaches like prodrugs, penetration enhancers, and nanoparticle carriers to improve ocular bioavailability.
The document discusses ocular drug delivery systems. It begins with an introduction to eye anatomy and factors affecting drug absorption in the eye. It then describes various ophthalmic formulations like solutions, suspensions, and ointments. It discusses advances in controlled release ocular systems including inserts, contact lenses, and nanoparticles to prolong drug release. Finally, it outlines new approaches in ocular drug delivery research focusing on combining technologies for targeted and sustained drug delivery to the eye.
This document discusses different types of controlled drug delivery systems. It classifies systems as rate preprogrammed, activation modulated, or feedback regulated. Rate preprogrammed systems are further broken down into polymer membrane permeation controlled systems, polymer matrix diffusion controlled systems, and microreservoir partition controlled systems. The key aspects and release kinetics of each system type are described through examples. Factors that influence drug release rates from these systems include membrane thickness, drug solubility, diffusivity, and partitioning coefficients.
Intrauterine & Intravaginal Drug Delivery SystemPRASHANT DEORE
This document discusses intrauterine and intravaginal drug delivery systems. It begins with an introduction and overview of anatomy and physiology of the female reproductive system. It then describes various types of intravaginal drug delivery systems including suppositories, bioadhesive semisolids, elastomeric rings, and solid polymeric carriers. Factors affecting vaginal drug absorption are also discussed. The document concludes by describing intrauterine drug delivery systems including non-hormonal and hormonal IUDs, and discussing advantages and disadvantages of both intravaginal and intrauterine systems.
ADVANCED APPROACHES OF OCULAR DRUG DELIVERY SYSTEMSyeda Amena
The document discusses ocular drug delivery systems. It begins with an introduction and overview of eye anatomy and physiology. It then covers the mechanisms of ocular absorption and barriers to drug delivery in the eye. Various routes of administration and types of ocular drug delivery systems are described, including advantages and disadvantages. Recent formulation trends include particulate systems, iontophoresis, and dendrimers. Evaluation methods both in vitro and in vivo are also discussed. The document concludes with the potential of combining drug delivery technologies to improve ocular drug absorption.
Implant : Challenging Drug Delivery Systembiniyapatel
This document discusses implantable drug delivery systems. Implants provide controlled delivery of drugs over long periods of time at the site of implantation. There are biodegradable and non-biodegradable implants. Implants can be classified based on their release mechanism, such as membrane permeation controlled, matrix diffusion controlled, or activation modulated systems. Implants offer benefits like continuous drug delivery and avoidance of peak concentrations but have disadvantages like requiring surgery and host reactions. Common applications of implants include cancer treatment, contraception, and ocular diseases.
This document discusses ocular drug delivery systems. It begins by describing the anatomy of the human eye and then discusses mechanisms of ocular absorption. There are various pathways and factors that can affect intraocular bioavailability. Controlled release systems are then described as they can provide accurate dosing, increased shelf life, and prolonged drug delivery. Various types of ocular controlled release systems are classified including non-erodible, erodible, nanoparticle, and liposome systems. Recent advances in ocular drug delivery technologies are also mentioned such as gels, prodrugs, and mucoadhesive polymers.
This document summarizes recent advances in ocular drug delivery systems. It describes the anatomy of the eye and various barriers to drug delivery. It discusses both conventional and advanced delivery methods including topical drops, intravitreal injections, implants, nanoparticles, and contact lenses. It also covers factors that influence drug absorption and challenges with ocular drug delivery such as short contact time, drainage, and barriers to posterior segment delivery. Polymeric systems, mucoadhesives, and penetration enhancers are presented as approaches to overcoming these challenges.
This document discusses ocular drug delivery systems. It begins with an introduction to why these systems were developed to treat eye diseases locally without causing irritation. It then describes the physiology and common diseases of the eye. Various ocular drug delivery systems are outlined, including viscous solutions, hydrogels, mucoadhesive formulations, liposomes, nanoparticles, and implants. The advantages of these systems are that they increase contact time, allow accurate dosing and controlled drug release to reduce side effects. In conclusion, these novel delivery systems provide more effective treatment of eye diseases.
This document discusses ocular (eye) drug delivery systems. It begins by providing an overview of the anatomy of the eye and challenges of delivering drugs to the eye, such as barriers like the cornea and blood-ocular barriers. It then describes various routes of ocular drug administration including topical, subconjunctival, and intravitreal delivery. Novel drug delivery approaches aimed at overcoming ocular barriers are also outlined, such as nanoparticles, liposomes, dendrimers, drug-loaded contact lenses, and intraocular implants. The document concludes that developing safe and effective ocular drug delivery strategies remains an ongoing challenge that researchers are addressing through nanotechnology and novel techniques.
Ocular drug delivery systems are designed to administer drugs onto or inside the eye. Conventional systems include eye drops, emulsions, suspensions, and ointments. However, only a small portion of the drug reaches the eye's interior using these methods. Novel nanotechnology-based systems like micelles, nanoparticles, liposomes, and dendrimers can more effectively target internal ocular tissues and increase drug residence in the eye. These novel systems may help improve treatment of diseases affecting the eye's anterior and posterior segments.
This document summarizes a seminar presentation on ocular drug delivery systems. It discusses the anatomy of the eye, barriers to drug permeation, and various routes and methods for ocular drug delivery. The key barriers include the cornea, tear turnover, and blood-ocular barriers. Delivery methods aimed to overcome these barriers include viscosity adjustment, penetration enhancers, prodrugs, and controlled release systems like inserts and implants. The document provides an overview of recent trends and advances in ocular drug delivery formulations and technologies.
Ocular drug delivery systems aim to overcome barriers to drug absorption by the eye and provide sustained drug release. They include novel formulations like liposomes, niosomes, microparticles and nanoparticles that can target ocular tissues. Controlled release systems like implants, contact lenses and Ocuserts maintain drug levels for extended periods. Alternative routes like intravitreal injections provide direct access to intraocular structures. Together, these approaches enhance ocular bioavailability and drug efficacy while reducing administration frequency.
The document discusses various aspects of ocular drug delivery systems. It describes the anatomy of the eye and factors influencing ocular drug absorption such as the corneal layers. Various ocular dosage forms are described including solutions, suspensions, ointments, gels and inserts. Insert-based delivery systems can provide sustained release and increased bioavailability. Inserts can be soluble, erodible or non-erodible depending on the polymer used. Collagen shields and soluble ocular drug inserts are examples of insert systems that dissolve gradually releasing the drug over time.
The document discusses ocular drug delivery systems. It outlines two approaches to overcoming barriers in ocular drug delivery: alternative delivery routes and novel drug delivery systems. It then describes various alternative delivery routes like intravitreal injection, subconjunctival injections, and intracameral injections. It also discusses conventional and novel ocular drug delivery systems like solutions, suspensions, emulsions, ointments, gels, liposomes, niosomes, inserts, implants, and particulate systems. The document provides details on various types of inserts and factors affecting drug release from ocuserts.
This document discusses ocular drug delivery systems (OCDDS) that aim to prolong drug release in the eye. It introduces various approaches for controlled release, including polymeric solutions, phase transition systems, mucoadhesive dosage forms, collagen shields, and ocular inserts. Specific examples are provided, such as Ocusert which releases pilocarpine at controlled rates over 4-7 days to treat glaucoma. The document outlines the ideal characteristics of OCDDS and mechanisms of controlled drug release via diffusion, osmosis and bioerosion. It also reviews factors influencing ocular drug penetration and absorption.
This document provides an introduction to ocular drug delivery systems (ODDS). It discusses the anatomy and physiology of the eye, challenges with conventional ophthalmic dosage forms, and advantages of new drug delivery systems. Various types of ocular drug delivery systems are described, including inserts, contact lenses, and vesicular systems like liposomes, niosomes, and pharmacosomes. Routes of ocular drug administration and mechanisms of drug absorption through the eye are also summarized. Common eye infections that can be treated with these drug delivery systems are listed.
This document provides an overview of ocular drug delivery systems. It discusses the composition of the eye, mechanisms of ocular absorption, factors affecting drug bioavailability, and barriers to drug delivery. Various traditional and advanced dosage forms are described, including solutions, suspensions, emulsions, ointments, inserts, and particulate systems. Recent formulation trends involve vesicular, controlled release, and in-situ gelling systems to improve precorneal residence time and drug absorption. Inserts like Ocuserts, Lacriserts, and Minidiscs provide sustained drug release while in-situ gels transform from liquid to gel upon instillation in the eye.
Recent Advancement in Ocular Drug Delivery System.pptxManshiRana2
This document summarizes recent advancements in ocular drug delivery systems. It discusses developments like intravitreal implants that provide sustained drug release, nanoparticles and microparticles for drug delivery, and hydrogels. It also covers recent progress in ocular gene therapy, with the FDA approval of the first gene therapy drug for an ocular condition. Barriers to ocular drug delivery are the eye's anterior and posterior segments, and new research is investigating nano-based systems to help lower intraocular pressure and treat glaucoma over the long term.
Introduction
Anatomy and physiology of human eye
Ocular delivery system
Optimum characters of ophthalmic drugs
Routes of ophthalmic drugs
Mechanism of ocular drug absorption
Barriers and fate of ocular drug delivery
Formulation consideration of ocular dosage forms
Evaluation tests
References
Ophthalmic drug delivery systems aim to enhance drug bioavailability in the eye. Topical eye drops are commonly used but have poor bioavailability due to barriers like tear turnover and drainage. Various approaches can improve ocular drug delivery, such as using viscosity enhancing polymers to prolong precorneal residence time, penetration enhancers to increase corneal permeability, and particulate systems like liposomes, niosomes and nanoparticles that can encapsulate drugs. In situ forming gels are also used, which are liquid on instillation and form a gel in the eye to increase retention time. Overall, optimizing ophthalmic formulations can help overcome barriers to improve drug absorption and efficacy.
The document discusses bioadhesive ocular drug inserts (BODI). BODI are soluble polymeric inserts that can incorporate various drugs and prolong their contact time in the eye through controlled release. They overcome issues with conventional eye drops like rapid drug loss and poor bioavailability. BODI are prepared using methods like solvent casting that dissolve polymers and drugs, and cast the mixture into films. They provide advantages over other inserts like not requiring removal from the eye.
This document discusses ocular drug delivery systems. It begins by introducing the need for ocular drug delivery to treat eye diseases and the benefits of topical administration. It then covers conventional dosage forms like solutions and gels as well as advanced controlled release systems like inserts, contact lenses, and implants. Vesicular systems like liposomes and niosomes are described as ways to encapsulate both hydrophilic and hydrophobic drugs and provide sustained release. The ideal properties of ocular delivery systems are prolonged residence at the eye, sustained drug release, and patient comfort. Barriers to drug delivery via the eye are also summarized.
ocular DRUG DELIVERY SYSTEMS: MECHANISMS AND PROGRESSIONSSumant Saini
This document discusses ocular drug delivery systems and the various challenges associated with delivering drugs to the eye. It outlines the key barriers to ocular drug delivery including the tear film, corneal and blood-ocular barriers which hinder drug absorption and efficacy. Various routes of administration are presented along with their benefits and challenges - topical delivery has low bioavailability due to tear dilution and efflux pumps. Emerging delivery systems aim to overcome these barriers and provide sustained drug release to target ocular tissues.
The document discusses ocular drug delivery systems. It begins by introducing the challenges with conventional eye drop formulations and how ocular drug delivery aims to increase bioavailability. It then describes the key parts of the human eye and various approaches to ocular drug delivery classification including inserts, nanoparticles, gels and more. Evaluation methods are also summarized such as drug content uniformity, in vitro diffusion testing and more. The document provides an overview of ocular drug delivery approaches and considerations.
This document discusses ocular drug delivery systems (ODDS) which are dosage forms used to administer drugs to the eye. Commonly used forms are solutions, suspensions, and ointments. Newer forms include gels, gel-forming solutions, ocular inserts, and implants. Drug absorption through the eye is poor due to protective mechanisms like tear drainage and blinking. Drugs can be absorbed through the cornea or non-corneally. Barriers to absorption include anatomy, physiology, and blood-ocular barriers. Methods to improve bioavailability and provide controlled release include viscosity adjustment, prodrugs, penetration enhancers, and inserts. The ideal ODDS has properties like good corneal penetration and prolonged contact time while being non
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Recent Advancements in Ocular Drug Delivery Systems
1. RECENT ADVANCEMENTS IN OCULAR
DRUG DELIVERY SYSTEM
Presented at National Webinar organized by
Shree HN Shukla Institute of Pharmaceutical Education and Research,
Rajkot, Gujarat
April10, 2021
Presented by : Dr. KAMAL SINGH RATHORE,
Associate Professor
HOD, Dept. of Pharmaceutics,
BN College of Pharmacy, Udaipur-Raj.313002
4/16/2021 1
3. Non-Corneal
Absorption
• Penetration across Sclera & Conjuctiva into Intra Ocular tissues
• Non-Productive: because penetrated drug is absorbed by
general circulation
Corneal
Absorption
• Outer Epithelium: rate limiting barrier, with pore size 60A,
Only access to small ionic & lipophilic molecules
• Trans cellular transport: transport between corneal epithelium
& stroma.
4/16/2021 3
5. Factors Affecting Intraocular Bioavailability:
• 1. Inflow & Outflow of Lachrymal fluids.
• 2. Efficient naso-lachrimal drainage.
• 3. Interaction of drug with proteins
of lachrimal fluid.
• 4. Dilution with tears.
Role of Polymer in ODDS.
Solution Viscosity : Solution Drainage.
Polymer Mucoadhesive Vehicle: Retained in the eye
due to non-covalent bonding between with conjuctival
mucine.
Mucine is capable of picking of 40-80 times of
weight of water.
4/16/2021 5
8. Route of
Administration
Advantages Limitations
Topical Convenient to deliver drugs Inefficient delivery to the
posterior segment, nasolacrimal
drainage, short contact time of
drug on the ocular surface
Systemic Convenient to deliver large amounts as compared to
eye drops
Poor bioavailability of drug in the
retina and systemic absorption
Intravitreal Drug delivered directly to the vitreous and retina in
the form of injections and implants
Problems such as cataract,
endophthalmitis, retinal
detachment and hemorrhage
Subconjunctival Both anterior and vitreous level of the drug can be
achieved and act as common route of
administration
Difficult to deliver drugs to the
retina due to the presence of
retinal pigment epithelium
Retrobulbar Provide medication to the posterior segments for
the treatment of posterior diseases
Effect provide by this route is very
less as drug may enter the globe
of the eye
Intracameral Deliver drugs directly to the anterior and vitreous
chamber
Difficult to deliver the drugs to the
posterior segment
Subretinal Deliver drugs to the retina Retinal detachment occurs as a
result of sub retinal delivery
Ocular Routes for Delivery of Bioactives
4/16/2021 8
9. Common Ocular Disorders Associated with Various
Tissues of Eye
Conjunctiva
(Conjunctivitis)
Cornea
(Keratitis)
Sclera
(Scleritis)
Miscellaneous
Infective Conjunctivitis,
Allergic Conjunctivitis
Ulcerative Keratitis,
Non-ulcerative Keratitis
Glaucoma,
Diabetic Retinopathy,
ARMD
Episcerates
Scleritis(anterior,
posterior)
4/16/2021 9
10. Principles and Practices of Various Drug Delivery
Systems to Eye
DRUG CATEGORIES
H1 Receptor antagonists
Anti glaucoma drugs
Anti-fibrotic drugs
Anti-inflammatory drugs
Anti-viral drugs
Anti-fungal agents
Immunomodulatory drugs
Antibiotics
4/16/2021 10
11. Requisites of Controlled Ocular Delivery Systems
• Polymeric solutions e.g.: MC, PVA, HPC& PVP
• Phase transition systems :stimuli sensitive
e.g.: Lutrol FC-127& Polaxomer 407 viscosity
increases when its temperature raised to 32-37
CAP- pH sensitive, Ion exchange, UV, Light
• Mucoadhesive/Bioadhesive dosage forms
e.g.: Polycarbophil(acrylic acid based polymer)
• Collagen shields, Collasomes
e.g.: antibiotic impregnated soft contact lenses
• Polymeric colloidal dispersions (o/w type emulsion)
• Ocular penetration enhancers
• Ocular Iontophoresis
4/16/2021 11
12. OCULAR DRUG DELIVERY
SYSTEMS
ADVANCED
DELIVERY SYSTEMS
Scleral plugs , Punctum plugs
Gene therapy
Stem cell, siRNA
CONTROLLED
DELIVERY SYSTEMS
Implants
Hydrogels
Dendrimers
Iontophorosis
Polymeric solution
Penetration enhanc
Contact lenses
Nanosuspensions
Microemulsions
Cyclodextrins
Phase transition
systems(in-situ)
Mucoadhesives,
Nanowafers
PARTICULATE
SYSTEMS
Nanoparticles
Microparticles,
NLC, SLN
VESICULAR
DELIVERY SYSTEMS
Liposomes
Niosomes
Pharmacosomes
Discomes
Cubosomes
RETRO METABOLIC
DELIVERY SYSTEMS
Soft-drug Approach,
Prodrug,
Chemical Delivery Systems
SOLUTIONS
GELS
OINTMENTS
SUSPENSIONS
EYE DROPS
CONVENTIONAL
DOSAGE FORMS
4/16/2021 12
15. Advantages and Disadvantages of Various Delivery Systems to Eye
S.No. Delivery/Dosage
Form
Advantages Disadvantages
1 Drops -easy to apply
-good patient acceptance
-Poor ocular bioavailability
-short duration of action
2 Systemic
administration
-more effective to treat diseases of the
posterior segment of the eye than drops
-do not bypass blood ocular
barriers
-side effects: systemic toxicity
3 Intravitreal,
Periocular,
Subconjuctival
injections
-improve drug absorption
-no systemic toxicity
-deliver to target site of the eye
-inj. Display 1st order kinetics
-short half life
-poor acceptance by patients
4 Implants -The biodegradable implants do not need
to be removed
-stabilization of the drug
-side effects increased risk
-uncontrollable release of
drug to eye
5 Microparticles,
Nanoparticles ,
Liposomes
-increase half-life
-decrease peak conc.
-localized drug delivery
-side effects
-risk associated drug delivery
6 Cell encapsulation -patient compliance
-limitations of toxicity
-side effects
-risk of operation
7 Iontophoresis -non-invasive easy method
-may use in combination
-more patient compliance
-No sustained half-life
-risk of side effects
-frequent administration
required
4/16/2021 15
16. OCULAR DRUG DELIVERY DEVICES
MATRIX-TYPE DRUG DELIVERY SYSTEMS
• Hydrophilic soft contact lenses
• Soluble ocular inserts
• Scleral buckling materials
CAPSULAR TYPE DRUG DELIVERY SYSTEMS
• Ocusert
• Implantable silicone rubber device
IMPLANTABLE DRUG DELIVERY PUMPS
• Osmatic mini pump and implantable infusion system
OTHER DELIVERY DEVICES
• Ocufit, BioCor® and Lacrisert
• Minidisk ocular therapeutic systems
4/16/2021 16
17. Contact Lens
Hydrophilic soft contact lenses
• Made up of hydrogels
• Marketed products are
Bionite was developed by Griffin Lab.
Soflens was developed by Bausch& Lomb
here the drug is fluorescein
• Other drugs: antiviral idoxuridine(IDU)
polymyxin B, pilocarpine
• Ability of presoaked hydrophilic lens
• Contact lenses made from PHP(Hefilcon-A)
copolymer(80% 2-hydroxy ethyl methacrylate &
20% N-vinyl-2-pyrrolidone)
diameter 16mm, thickness 0.3mm&
their hydration was 40-45%
Now using Molecular imprinting technology
Modern system classifies contact lens into three major types such as (i) Soft
(ii) Semi- soft
(iii) Hard contact lens
4/16/2021 17
18. Contact lens hydrogel containing molecular
sites with drug affinity
Liposomes on the surface of a contact lens
hydrogel(left), liposomes with in a contact
lens hydrogels(right)
Drug polymer film coated by a contact lens
hydrogel
4/16/2021 18
19. Ocular Inserts
Ophthalmic inserts
Soluble Bioerodable Insoluble
natural polymer collagen shields reservoir
systems
E.g.:SODI E.g.:Lacrisert,
PVAI minidisc
•Diffusion
based(ocusert)
•Osmatic based
•Soft (presoaked)
contact lenses
Sterile preparations with a thin, multilayered , drug
impregnated solid or semi solid consistency devices
placed into cul-de-sac (or) conjunctival sac
4/16/2021 19
20. Soluble Ocular Inserts
1) Poly Vinyl Alcohol Inserts(PVAI)
• Thin, elastic & oval plates
• Impregnated with antibiotics, sulfonamides, pilocarpine, atropine
etc.
Limitations : poor patient compliance & difficulty of self insertion
2) Soluble Ophthalmic Drug Inserts(SODI)
• Thin, elastic & oval plates
• Composition: polymers and copolymers of polyacryl amide, Vinyl
pyrolidone, ethyl acrylate.
• Weight 15-16mg
• In 10-15 sec softens
• In 10-15 min turns in viscous liquids
• After 30-90 min becomes polymeric solution
Advantage:
• Single SODI application: replaces 4-12 eye drops
• Ones a day treatment of Glaucoma & Trachoma
4/16/2021 20
21. Advantages of ocular inserts
• Increased ocular residence
• Releasing drugs at a
slow,constant rate
• Acurate dosing
• Reduction of systemic absorption
• Better patient compliance
Disadvantages of
ocular inserts
•A capital disadvantage of
ocular inserts resides In
their solidity
•The occasional inadvertent
loss during sleep or while
•Their interference with vision
•Difficult placement of the
ocular inserts
Desired Criteria For Control Release Ocular Inserts.
The following have to be evaluated for
ocular inserts:
1.Uniformity of thickness.
2.Uniformity of weight.
3.Drug content
4.Percentage moisture absorption.
5.Percentage moisture loss.
6.Surface pH.
7.Eye irritancy test.
8.Stability studies.
9.In vitro drug release study.
10.In vivo drug release study.
11.Microbiological studies.
4/16/2021 21
22. 4/16/2021 22
Phase transition with Poloxamers, pluronics, tetronics are used.
[Poloxamer 407+chitosan], [PEO-PPO-PEO with chitosan],
Poly(N-isopropylacrylamide) are well researched thermogelling polymers
23. Scleral Buckling Material
• Two types 1) Gelatin Film
2) Solid Silicone Elastomer
• Antibiotic preparations are
chloramphenicol & lincomycin
• Immersing the devices into aqueous antibiotic
solution and then dried. They found sustained
release of the antibiotic from these devices
Use: To prevent postoperative infections after
retinal detachment surgery
4/16/2021 23
24. Ocusert:
• Capsular-type drug delivery systems
• Developed by ALZA corporation
• Oval, flexible ocular insert
• Annular ring impregnated with Ti02 for flexibility
• Dimensions: major axis:13.4mm; minor axis:5.7mm,
thickness:0.3mm
• Two types of Ocusert are available, Ocusert Pilo-20& Pilo-40
Part Material
Drug reservoir Pilocarpine
Carrier material Alginic acid
Rate controller Ethylene vinyl acetate (EVA) copolymer
membrane
Energy source Conc. of pilocarpine
Flux enhancer Di(2-ethyl hexyl) phthalate
4/16/2021 24
25. Implantable Silicone
Rubber Devices
• Drug delivery device for hydrophobic drugs
e.g.:-BCNU(1,3-bis(2-chloro ethyl)-1-nitroso
urea)---- an intraocular malignancy agent
• The device consists of two sheets of silicone
rubber glued together only at the edges with
silicone adhesive
• A tube of the same material extends from
device
• The device released BCNU at a constant rate
about 200-400mcg/hr
4/16/2021 25
26. Implantable Drug Delivery Pumps
• Osmatic mini pump(ALZET)
Constant drug delivery rate with a
pumping duration of up to two
weeks
• Implantable infusion
system(Infusaid)
Permitted long term infusion via
refilling
• A drug pellet coated with polyvinyl
alcohol and ethylene vinyl acetate
• A polysulfone capillary fiber (PCF)
4/16/2021 26
27. Lacrisert
• Sterile , rod shaped device
• Composition: HPC without preservative
• The devices have long retention(2 weeks
or more) and sustained release features
• Weight: 5 mg
• Dimension: diameter 12.7mm, length
3.5mm
Use:- Dry eye treatment, Keratitis
4/16/2021 27
28. Minidisk
• It shaped like contact lens, with convex
front & concave back surface in contact
with eye ball
• 4-5mm in diameter
• Composition: silicon based polymer
• Hydrophilic or hydrophobic
• Drug release from 170hr
4/16/2021 28
29. Hydrogel template strategy
The hydrogel template strategy was developed
to fabricate homogeneous polymeric
microparticles. The versatility of the hydrogel
template strategy for the development of
nanowafer-based ocular drug delivery systems.
The fabrication of dexamethasone-loaded
nanowafers using polyvinyl alcohol. The
nanowafer, a small circular disk, is placed on the
ocular surface, and it releases a drug as it slowly
dissolves over time, thus increasing ocular
bioavailability and enhancing efficiency to treat
eye injuries.
4/16/2021 29
30. Quantum dots
Quantum dots are nanoscale semiconductor crystals
with characteristic size and tunable optical properties,
which deliver bright and stable fluorescence suitable
for bioimaging and labelling. ... Quantum
dots potentially provide a range of diagnostic and
therapeutic applications in ophthalmology.
4/16/2021 30
31. Retrometabolic delivery system
• Combination of SAR and SMR Retrometabolic drug design (RMDD)
• Metabolic activation of inactive delivery forms: chemical delivery systems
CDS Drug
inactive active
Alkyl oxime datives oximes(enzymes located in iris-celiary body)
• Metabolic deactivation of specifically designed active species: soft drugs
SD Mi
Active inactive metabolites
hydrocortisone spirothiazolidine
• RMDD represent novel, systemic approach to achieve these goals include
two distinct methods aimed to increase the therapeutic index
SOFT DRUG design
CHEMICAL DELIVERY SYSTEM design
4/16/2021 31
32. The chemical delivery systems(CDSs)- chemical compounds – produced by synthetic chemical
reaction(s) forming covalent bonds between the drug(D) and specifically designed ‘Carrier ’
and other moieties. At least one chemical bond needs to be broken for active compound (D)
to be released. The release of active compound from CDSs takes pace by enzymatic or
hydrolytic cleavage.
The basic principle of retrometabolic drug design approaches is that the drug metabolism
considerations should actually be involved at a very early stage of the design process- not as
an after thought in order to explain some of the behaviours of the drug
SAR+SMR=RETROMETABOLIC DRUG DELIVERY SYSTEM
Drug targeting by CDS’s
1.Enzymatic physical chemical
based targeting
2.Site specific-enzyme activated
targeting
3.Receptor based chemical
targeting
Drug targeting by soft drugs
1.Soft drug analogs
2.Activated soft compounds
3.Active metabolite type soft drugs
4.Controlled release of
endogenous soft compounds
5.Inactive metabolic approach
4/16/2021 32
33. Nanoparticles
• The drug absorption in the eye is enhanced significantly in comparison to eye
drop solutions by 10 to 1000 nm particles.
• Supramolecular structure, complexes and composites belongs to np systems
Includes: microemul., liposomes, niosomes, dendrimers and CD.
• PEG, Poly alkyl cyano acrylate(PACA) nanoparticles and nanocapsules
improve corneal penetration of hydrophilic and lipophilic drugs
Limitation: disruption of corneal epithelium cell membrane
• Poly- ԑ-caprolactone(PECL) nanocapsules increase ocular penetration of
lipophilic drugs such as metipranolol, betaxolol.
• PECL taken up by the corneal epithelium cells without damaging the cell
membrane
• Colloidal nature of the carrier is the main factor responsible for favorable
corneal transport of drugs
• Produced from Eudragit RS100, RL100
PARTICULATE SYSTEM FOR OCULAR DRUG DELIVERY
4/16/2021 33
34. Liposomes
• Non-toxic, non irritant biodegradable in nature
• Ability to incorporate almost any type of the drug regardless of the
solubility
• Intimate contact with cornea and conjunctival surfaces
• Protect the drug from metabolic enzymes
• Phospholipids used are: phosphotidylcholine, phosphotidic acid,
sphingomyline, phosphotydyleserine, cardiolipine
• 4 fold increase in passage of penicillin G across rabbit cornea & 10 fold
enhancement of indoxole passage across rat cornea were observed when
the formulations compared with solutions
VESICULAR SYSTEM FOR OCULAR DRUG DELIVERY
4/16/2021 34
35. Niosomes are non-ionic surfactant based multilamellar(>0.05µm),small
unilamellar(0.025-0.05µm) or large unilamellar vesicles(>0.1µm) in which an
aqueous solution of solute(s) is entirely enclosed by a membrane resulted from
organization of surfactant macromolecules as bilayers
STRUCTURAL COMPONENTS USED
• Surfactants (dialkyl polyoxy ethylene ether non ionic surfactant)
• Cholesterol
CHOLESTROL:
1. Cannot form bilayers, but bring changes in fluidity and permeability to bilayers.
2. Can be used in high molar concentrations.
3. Stabilize and prevent leak from vesicles.
ADVANTAGES:
•The vesicle suspension being water based offers greater patient compliance over oil
based systems
•Since the structure of the niosome offers place to accommodate hydrophilic, lipophilic as
well as ampiphilic drug moieties, they can be used for a variety of drugs.
•The characteristics such as size, lamellarity etc. of the vesicle can be varied depending on
the requirement.
•The vesicles can act as a depot to release the drug slowly and offer a controlled release.
•They are osmotically active and stable.
•They increase the stability of the entrapped drug
•Improves therapeutic performance of the drug by protecting it from the biological
environment and restricting effects to target cells, thereby reducing the clearance of the
drug.
DISADVANTAGES
• Physical instability, Aggregation, Leaking of entrapped drug, Fusion,
Niosomes
4/16/2021 35
36. PHARMACOSOMES
• The vesicle formation takes place not only just by association of
phospholipids but also by amphiphilic molecular association
• Since many drugs are also amphiphiles, they can form the vesicles
Advantages:
• Drug metabolism can be decreased
• Controlled release profile can be achieved
DISCOMES
• Soluble surface active agents when added in critical amount to
vesicular dispersion leads to solubilization or breakdown of vesicles
& translates them into mixed micellar systems
e.g.: Egg yolk phosphotidyl choline liposomes by the addition of
non ionic surfactants of poly oxy ethylene cetyl ether till the lamellar
and mixed lamellar coexist
Advantages:
• Minimal opacity imposes no hindrance to vision
• Increased patient compliance
• Zero order release can be easily attained
4/16/2021 36
37. Advantages of Vesicular Systems
1. No difficulty of insertion as in the case of ocular
inserts
2. No tissue irritation and damage as caused by
penetration enhancers
3. Provide patient compliance as there is no difficulty of
insertion as observed in the case of inserts
4. The vesicular carriers are biocompatible and have
minimum side effects
5. Degradation products formed after the release of
drugs are biocompatible
6. They prevent the metabolism of drugs from the
enzymes present at tear/corneal epithelium interface
7. Provide a prolong and sustained release of drug
4/16/2021 37
41. Noninvasive Drug-Delivery Systems for the Posterior Disorders
Future perspectives
Various strategies for enhancing b.a. using solubility, retention and
permeability enhancers. Drug-loaded contact lenses, np tech., smart
dds-release their payload in response to a stimulus. Ocular implants,
delay or prevent blindness could be made by artificial corneas, drug-
eluting IOL, novel materials for vitreous humor replacement as lifelong
one-off implantable drug del depots could potentially be realized
‘Quality of life’ benefits.
4/16/2021 41
42. Conclusion
• Quality, Efficacy and Safety should be the
optimal parameters for drug delivery to
eye in this context, more clinical studies
are necessary to provide further
information and insight in to new ocular
drug delivery system.
4/16/2021 42
43. Ocular drug delivery is a complex field in which
multiple factors determine the drug concentrations
and, thus, efficacy at the target site.
Furthermore, drug loading and required release rates
are strongly dependent on the local site of drug
administration and location of the target tissue.
Here, I have presented a simple guideline for dose and
delivery system selection to augment decision-making
and initial drug delivery system design in recent ocular
drug development.
4/16/2021 43
44. References
• Ophthalmic Drug Delivery System: Challenges and Approaches
PB Patel, DH Shastri, PK Shelat, AK Shukla
•Ocular Transporters in Ophthalmic Diseases and Drug Delivery;
Edited by Joyce Tombran-Tink, Colin J. Barnstable.
• Targeted & Controlled Drug Delivery Novel Carrier Systems by
S.P.Vyas, R.K.Khar
•Anatomy and Physiology: Tora Tora
• Ophthalmic Drug Delivery Systems-Recent Advances:
Dr.K.S.Rathore
Web searched:
•http://www.google/images/eye/anatomy&physiology
http://pharmaxchange.info
• Advances in Ophthalmic Drug Delivery, Ther.Deliv.(2014), 5(12),
1297-1315.
• ElianaB.Souto, Advances Formulation Approaches for Ocular Drug
Delivery: State-of-the Art and Recent Patents. Pharmaceutics, 2019,
11, 460.
4/16/2021 44