The document discusses transdermal drug delivery systems (TDDS), which facilitate the passage of drugs through the skin for systemic effects. It describes the stratum corneum as the major barrier to drug transport through the skin and the various routes drugs can take (hair follicles, sweat ducts, intercellularly). Factors that affect percutaneous absorption include drug properties like solubility, molecular weight, and concentration, as well as skin properties like hydration, temperature, and condition. The document also discusses permeation enhancers that can increase skin permeability through physical or chemical means.
This document discusses transdermal drug delivery systems. It defines transdermal delivery as delivering drugs through the skin into systemic circulation at predetermined rates over prolonged periods. The key advantages are avoiding gastrointestinal degradation and first-pass metabolism, providing controlled drug levels, and increasing patient compliance. The document covers skin anatomy, permeation pathways, factors influencing permeation like drug properties, and technologies used to develop transdermal patches.
This document discusses semisolid dosage forms, including their anatomy, mechanisms of drug penetration through skin, and factors influencing dermal penetration of drugs. It defines semisolids as topical dosage forms used for therapeutic, protective, or cosmetic purposes on the skin or other mucous membranes. The main types of semisolids discussed are ointments, pastes, creams, and gels. Key aspects like ideal properties, ingredients, preparation, classifications, and excipients of these semisolid dosage forms are described in detail. The roles and advantages of various ointment bases like oleaginous, absorption, and emulsion bases are also summarized.
1) The document discusses semi-solids like ointments, creams, pastes and gels. It describes the three layers of skin - epidermis, dermis and hypodermis - and factors that influence skin penetration like vehicle, pH, drug properties, skin conditions and more.
2) It also discusses mechanisms of drug permeation through skin and various penetration enhancement techniques using chemicals or physical methods. Common chemical penetration enhancers mentioned include surfactants, fatty acids, alcohols, dimethyl sulfoxide and others.
3) The mechanisms of different penetration enhancers are explained, such as their effects on skin lipids and proteins. Ideal properties of penetration enhancers and their
the all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
SEMISOLID DOSAGE FORM PRESENTATION.
Pharmaceutics,
B.Pharmacy 1st year
INTRODUCTION OF SEMISOLID DOSAGE FORM,
Semisolid dosage forms are pharmaceutical formulations which contain one or more active ingredients dissolved or uniformly dispersed in a suitable base and any suitable excipients and are normally presented in the form of creams , jells , ointments or pastes..They are traditionally used for treating topical disorders..The majority of them are meant for skin applications.
Mechanism of dermal penetration of drugs,
This document summarizes transdermal drug delivery systems. It discusses that transdermal delivery administers drugs through the skin for systemic effects. The skin provides a barrier for drug penetration via various routes. Factors like a drug's properties, skin characteristics, and formulation components influence transdermal absorption. Desirable drug properties for transdermal delivery include low molecular weight, adequate solubility, and short half-life. A transdermal patch consists of a polymer matrix containing the drug, pressure sensitive adhesives, and may include permeation enhancers.
This document provides an overview of transdermal drug delivery systems (TDDS). It discusses the advantages and disadvantages of TDDS. Key aspects covered include the anatomy and structure of skin, routes of drug penetration, factors affecting permeation, and basic components of TDDS such as polymers, drugs, and penetration enhancers. The structure of skin is described in three layers: epidermis, dermis, and hypodermis. Drugs can penetrate the skin through transfollicular or transdermal routes. Successful TDDS design considers biological, physicochemical, and environmental factors influencing permeation.
Transdermal drug delivery systems (TDDS) deliver drugs through the skin and into systemic circulation at a controlled rate. TDDS provide advantages like avoidance of first-pass metabolism and allowing controlled drug levels. The skin is a barrier, so permeation involves partitioning into the stratum corneum then diffusion across layers. Factors like a drug's physicochemical properties, the delivery system composition, and skin conditions influence permeation kinetics. TDDS have components like polymer matrices, drugs, and permeation enhancers. They are evaluated for properties such as adhesive peel adhesion to ensure removal does not damage skin.
This document discusses transdermal drug delivery systems. It defines transdermal delivery as delivering drugs through the skin into systemic circulation at predetermined rates over prolonged periods. The key advantages are avoiding gastrointestinal degradation and first-pass metabolism, providing controlled drug levels, and increasing patient compliance. The document covers skin anatomy, permeation pathways, factors influencing permeation like drug properties, and technologies used to develop transdermal patches.
This document discusses semisolid dosage forms, including their anatomy, mechanisms of drug penetration through skin, and factors influencing dermal penetration of drugs. It defines semisolids as topical dosage forms used for therapeutic, protective, or cosmetic purposes on the skin or other mucous membranes. The main types of semisolids discussed are ointments, pastes, creams, and gels. Key aspects like ideal properties, ingredients, preparation, classifications, and excipients of these semisolid dosage forms are described in detail. The roles and advantages of various ointment bases like oleaginous, absorption, and emulsion bases are also summarized.
1) The document discusses semi-solids like ointments, creams, pastes and gels. It describes the three layers of skin - epidermis, dermis and hypodermis - and factors that influence skin penetration like vehicle, pH, drug properties, skin conditions and more.
2) It also discusses mechanisms of drug permeation through skin and various penetration enhancement techniques using chemicals or physical methods. Common chemical penetration enhancers mentioned include surfactants, fatty acids, alcohols, dimethyl sulfoxide and others.
3) The mechanisms of different penetration enhancers are explained, such as their effects on skin lipids and proteins. Ideal properties of penetration enhancers and their
the all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
SEMISOLID DOSAGE FORM PRESENTATION.
Pharmaceutics,
B.Pharmacy 1st year
INTRODUCTION OF SEMISOLID DOSAGE FORM,
Semisolid dosage forms are pharmaceutical formulations which contain one or more active ingredients dissolved or uniformly dispersed in a suitable base and any suitable excipients and are normally presented in the form of creams , jells , ointments or pastes..They are traditionally used for treating topical disorders..The majority of them are meant for skin applications.
Mechanism of dermal penetration of drugs,
This document summarizes transdermal drug delivery systems. It discusses that transdermal delivery administers drugs through the skin for systemic effects. The skin provides a barrier for drug penetration via various routes. Factors like a drug's properties, skin characteristics, and formulation components influence transdermal absorption. Desirable drug properties for transdermal delivery include low molecular weight, adequate solubility, and short half-life. A transdermal patch consists of a polymer matrix containing the drug, pressure sensitive adhesives, and may include permeation enhancers.
This document provides an overview of transdermal drug delivery systems (TDDS). It discusses the advantages and disadvantages of TDDS. Key aspects covered include the anatomy and structure of skin, routes of drug penetration, factors affecting permeation, and basic components of TDDS such as polymers, drugs, and penetration enhancers. The structure of skin is described in three layers: epidermis, dermis, and hypodermis. Drugs can penetrate the skin through transfollicular or transdermal routes. Successful TDDS design considers biological, physicochemical, and environmental factors influencing permeation.
Transdermal drug delivery systems (TDDS) deliver drugs through the skin and into systemic circulation at a controlled rate. TDDS provide advantages like avoidance of first-pass metabolism and allowing controlled drug levels. The skin is a barrier, so permeation involves partitioning into the stratum corneum then diffusion across layers. Factors like a drug's physicochemical properties, the delivery system composition, and skin conditions influence permeation kinetics. TDDS have components like polymer matrices, drugs, and permeation enhancers. They are evaluated for properties such as adhesive peel adhesion to ensure removal does not damage skin.
This document discusses semi-solid dosage forms such as ointments, pastes, creams, and gels used for dermal drug delivery. It describes the three potential routes of drug penetration through the skin including via sweat ducts, across the stratum corneum, and through hair follicles. Factors that influence dermal penetration include biological factors like skin condition, age, and blood flow as well as physicochemical factors like skin hydration, temperature, drug concentration, and molecular size. Common bases used for semi-solid formulations are discussed including oleaginous, absorption, emulsion, and water soluble bases. Excipients commonly included in these formulations and their purposes are also outlined.
This document discusses transdermal drug delivery systems (TDDS). It provides an introduction and overview of the skin layers involved in percutaneous absorption. It describes the factors influencing drug delivery through the skin and the components of a typical TDDS including the polymer matrix, drug, pressure sensitive adhesives, backing membrane, and release liner. It also discusses various techniques for enhancing transdermal drug delivery and different types of TDDS. The document is authored by a group of 6 students.
The document discusses the major pathways for skin penetration including the intercellular, intracellular, intrafollicular, and polar pathways. It also examines factors that affect skin penetration such as molecule size and skin conditions. Several types of penetration enhancers are covered, including those that modify the polar or non-polar routes, act through extraction of skin lipids, or affect the skin through enzymatic or vesicular mechanisms. In general, smaller molecules below 500 Daltons can more easily penetrate skin through these various routes and pathways.
Transdermal drug delivery systems (TDDS), also known as transdermal patches, deliver drugs through the skin for systemic circulation. TDDS consist of a drug reservoir between a backing layer and rate-controlling membrane. Drugs must have certain properties to permeate the skin via transcellular, transappendageal, or transfollicular routes. Factors like skin properties, drug properties, and permeation enhancers affect the permeation rate. Common TDDS formulations include polymer membrane, adhesive matrix, and microreservoir systems. TDDS provide advantages over other delivery methods like sustained release and non-invasiveness but also have some disadvantages.
This document provides an overview of transdermal drug delivery systems (TDDS). It defines TDDS and lists their advantages and disadvantages. It describes the structure of skin and the routes and mechanisms of absorption for TDDS. Factors affecting percutaneous absorption are outlined. Approaches to increase skin permeation include chemical, physical and carrier system methods. Transdermal patches, their components and types are defined. Evaluation methods for TDDS are provided in brief.
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
The document discusses transdermal patches, which deliver medication through the skin in a time-released manner. It covers the structure of skin and absorption mechanisms, the history and components of transdermal patches, different types of patches including polymer membrane and matrix patches, evaluations of patches, recent advances like iontophoresis and sonophoresis, and some marketed preparations. The key advantages of transdermal patches are avoiding presystemic metabolism, maintaining drug levels, and improving compliance through extended duration of action.
Transdermal drug delivery systems deliver drugs through the skin at a controlled rate, providing an alternative to oral delivery and hypodermic injection. They avoid gastrointestinal absorption issues, provide extended therapy with a single application, and allow for easy termination of treatment. However, some drugs permeate the skin too slowly to achieve therapeutic effects, and the system components can sometimes cause skin irritation. The performance of transdermal drug delivery depends on factors related to the drug, skin characteristics, formulation components, and delivery system design.
The document discusses transdermal drug delivery systems and the factors that affect percutaneous absorption of drugs. It notes that the skin plays an important role as a barrier to drug absorption but also serves as a route for drug delivery. Drugs can have effects on the skin surface, within the stratum corneum, or more deeply in the epidermis and dermis. The major routes of drug penetration are through intercellular channels. Factors like the drug properties, vehicle used, skin conditions, and occlusion affect the rate of absorption. Transdermal drug delivery systems are designed to control the rate of drug delivery through the skin and into systemic circulation. They aim to deliver drugs safely and effectively at a controlled rate.
This document discusses transdermal drug delivery systems. It provides information on:
1. Transdermal drug delivery involves administering therapeutic agents through intact skin for systemic effects. Only a small number of drug products are available for this route.
2. The skin provides an effective barrier for drug penetration. The epidermis is the main control element, and drugs can penetrate via hair follicles, sweat ducts, or diffusion across the stratum corneum.
3. Transdermal patches must consider the drug's properties, skin structure, and factors like permeability enhancers to effectively deliver medication through the skin.
TRANSDERMAL THERAPEUTIC DRUG DELIVERY SYSTEMS N Anusha
This document discusses transdermal therapeutic systems (TTS). It begins by defining TTS as self-contained dosage forms that deliver drugs through intact skin at a controlled rate. It then covers various topics related to TTS including advantages/disadvantages, factors affecting skin permeation, mechanisms of drug permeation, and techniques to enhance permeation like physical methods (iontophoresis, electroporation, etc.), chemical enhancers, and patch design/evaluation. The document provides details on the design, preparation, and evaluation of various TTS with the goal of improving transdermal drug delivery.
Transdermal drug delivery has made an important contribution to medical practice, but has yet to fully achieve its potential as an alternative to oral delivery and hypodermic injections. First-generation transdermal delivery systems have continued their steady increase in clinical use for delivery of small, lipophilic, low-dose drugs. Second-generation delivery systems using chemical enhancers, non-cavitational ultrasound and iontophoresis have also resulted in clinical products; the ability of iontophoresis to control delivery rates in real time provides added functionality. Third-generation delivery systems target their effects to skin’s barrier layer of stratum corneum using microneedles, thermal ablation, microdermabrasion, electroporation and cavitational ultrasound. Microneedles and thermal ablation are currently progressing through clinical trials for delivery of macromolecules and vaccines, such as insulin, parathyroid hormone and influenza vaccine. Using these novel second- and third-generation enhancement strategies, transdermal delivery is poised to significantly increase impact on medicine.
Transdermal drug delivery system- structure of skinAkankshaPatel55
Transdermal drug delivery systems (TDDS) have transcended the realm of simple nicotine patches and entered an exciting era of innovation. Gone are the days of bulky, uncomfortable adhesives; in their place stand sophisticated systems capable of delivering a myriad of therapeutic agents through the seemingly impregnable barrier of the skin. To truly understand the magic behind this technology, we delve deeper, exploring its intricate mechanisms and promising future. The journey begins with a microscopic waltz at the skin's outermost layer, the stratum corneum. Drug molecules, meticulously formulated into miniscule particles, are incorporated into a semi-permeable patch. This patch acts as a launchpad, adhering snugly to the skin and initiating the drug's odyssey. Guided by the principles of Fick's Law of Diffusion, the drug embarks on a clandestine mission. Driven by a concentration gradient, it permeates the intercellular lipids of the stratum corneum, navigating a labyrinthine path formed by keratinocytes. This passive journey, governed by factors like drug lipophilicity and skin thickness, determines the rate and extent of absorption. However, diffusion plays just the first act in this multi-part drama. Once traversing the stratum corneum, the drug encounters the viable epidermis, a dynamic landscape teeming with enzymes and metabolic pathways. Here, some compounds may undergo degradation, limiting their systemic bioavailability. To overcome this hurdle, scientists devise ingenious strategies:
Penetration Enhancers: Chemical agents like propylene glycol or oleic acid temporarily disrupt the skin's lipid packing, easing the drug's passage.
Iontophoresis: Electric current gently guides charged molecules through the skin, bypassing enzymatic barriers and boosting delivery.
Microneedle Technology: Tiny, painless needles create transient microchannels, facilitating the delivery of larger molecules like proteins and peptides. The Symphony of Controlled Release:
A key advantage of TDDS lies in their ability to sustain drug release over extended periods. This controlled release symphony is orchestrated by sophisticated reservoir systems:
Matrix Systems: The drug is homogeneously dispersed within a polymer matrix, gradually diffusing out over time.
Reservoir Systems: A distinct drug reservoir separates from the adhesive layer, allowing for precise and prolonged delivery.
Programmable Systems: Advanced patches incorporate microfluidic channels and microchips, enabling customized release profiles and even pulsatile delivery for specific therapeutic needs.
Benefits Beyond Convenience:
The charm of TDDS extends far beyond the mere convenience of avoiding needles. They offer distinct advantages over traditional oral and parenteral routes:
Enhanced Bioavailability: By bypassing first-pass metabolism in the liver, certain drugs achieve higher systemic concentrations through transdermal delivery.
Improved Patient Compliance: Continuous, hassle-free adminis
This document provides an overview of transdermal drug delivery systems. It defines transdermal therapeutic systems as self-contained dosage forms that deliver drugs through the skin at a controlled rate. The document outlines the contents to be covered, which include the advantages and structure of the skin, permeation through skin, and formulation and evaluation of transdermal drug delivery systems. It also briefly discusses the history and factors affecting permeation through skin.
This document discusses transdermal drug delivery systems (TDDS). TDDS deliver drugs through the skin at a controlled rate. Key points:
1. TDDS have advantages like delivering drugs over an extended period with less fluctuations compared to oral dosing. However, only small lipophilic drugs can currently be delivered.
2. The skin is the rate-limiting barrier, with the stratum corneum restricting drug entry and exit. Drugs must penetrate this layer to be absorbed systemically.
3. Factors like skin conditions, age, temperature, and drug properties affect transdermal permeation. Ideal TDDS components include potent drugs, polymers to control release, permeation enhancers,
The document discusses transdermal drug delivery systems (TDDS). It defines TDDS and provides their advantages over other drug delivery methods. It describes the skin structure, especially the stratum corneum layer, and how drugs penetrate the skin through various routes. Factors that affect transdermal drug permeability are outlined. Ideal drug candidates and components of TDDS like polymers and permeation enhancers are also discussed.
transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream
The document discusses the skin and integumentary system. It describes the skin as a large organ composed of three main layers - the epidermis, dermis and subcutaneous layer. The epidermis provides protection while the dermis contains blood vessels, glands and sensory receptors. Accessory organs include nails, hair follicles, sebaceous glands and sweat glands. The skin plays an important role in temperature regulation through processes like sweating and vasodilation. Wound healing occurs through inflammation, clotting, cell reproduction and scar formation.
Quality control involves sampling, testing, and ensuring products meet specifications before release. It is focused on identifying defects in finished products. Key responsibilities include testing raw materials, conducting in-process testing, and approving or rejecting starting materials, packaging, intermediates, and finished products. Quality control aims to fulfill quality requirements and ensure only products passing tests are released.
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Similar to Lect 5a transdermal drug delivary system B 2016.ppt
This document discusses semi-solid dosage forms such as ointments, pastes, creams, and gels used for dermal drug delivery. It describes the three potential routes of drug penetration through the skin including via sweat ducts, across the stratum corneum, and through hair follicles. Factors that influence dermal penetration include biological factors like skin condition, age, and blood flow as well as physicochemical factors like skin hydration, temperature, drug concentration, and molecular size. Common bases used for semi-solid formulations are discussed including oleaginous, absorption, emulsion, and water soluble bases. Excipients commonly included in these formulations and their purposes are also outlined.
This document discusses transdermal drug delivery systems (TDDS). It provides an introduction and overview of the skin layers involved in percutaneous absorption. It describes the factors influencing drug delivery through the skin and the components of a typical TDDS including the polymer matrix, drug, pressure sensitive adhesives, backing membrane, and release liner. It also discusses various techniques for enhancing transdermal drug delivery and different types of TDDS. The document is authored by a group of 6 students.
The document discusses the major pathways for skin penetration including the intercellular, intracellular, intrafollicular, and polar pathways. It also examines factors that affect skin penetration such as molecule size and skin conditions. Several types of penetration enhancers are covered, including those that modify the polar or non-polar routes, act through extraction of skin lipids, or affect the skin through enzymatic or vesicular mechanisms. In general, smaller molecules below 500 Daltons can more easily penetrate skin through these various routes and pathways.
Transdermal drug delivery systems (TDDS), also known as transdermal patches, deliver drugs through the skin for systemic circulation. TDDS consist of a drug reservoir between a backing layer and rate-controlling membrane. Drugs must have certain properties to permeate the skin via transcellular, transappendageal, or transfollicular routes. Factors like skin properties, drug properties, and permeation enhancers affect the permeation rate. Common TDDS formulations include polymer membrane, adhesive matrix, and microreservoir systems. TDDS provide advantages over other delivery methods like sustained release and non-invasiveness but also have some disadvantages.
This document provides an overview of transdermal drug delivery systems (TDDS). It defines TDDS and lists their advantages and disadvantages. It describes the structure of skin and the routes and mechanisms of absorption for TDDS. Factors affecting percutaneous absorption are outlined. Approaches to increase skin permeation include chemical, physical and carrier system methods. Transdermal patches, their components and types are defined. Evaluation methods for TDDS are provided in brief.
Transdermal Drug Delivery System (TDDS) is the one of the novel technology to deliver the molecules through the skin for long period of time.
Transdermal Drug Delivery System (TDDS) are defined as self contained, discrete dosage forms which are also known as “patches” 2, 3 when patches are applied to the intact skin, deliver the drug through the skin at a controlled rate to the systemic circulation
The document discusses transdermal patches, which deliver medication through the skin in a time-released manner. It covers the structure of skin and absorption mechanisms, the history and components of transdermal patches, different types of patches including polymer membrane and matrix patches, evaluations of patches, recent advances like iontophoresis and sonophoresis, and some marketed preparations. The key advantages of transdermal patches are avoiding presystemic metabolism, maintaining drug levels, and improving compliance through extended duration of action.
Transdermal drug delivery systems deliver drugs through the skin at a controlled rate, providing an alternative to oral delivery and hypodermic injection. They avoid gastrointestinal absorption issues, provide extended therapy with a single application, and allow for easy termination of treatment. However, some drugs permeate the skin too slowly to achieve therapeutic effects, and the system components can sometimes cause skin irritation. The performance of transdermal drug delivery depends on factors related to the drug, skin characteristics, formulation components, and delivery system design.
The document discusses transdermal drug delivery systems and the factors that affect percutaneous absorption of drugs. It notes that the skin plays an important role as a barrier to drug absorption but also serves as a route for drug delivery. Drugs can have effects on the skin surface, within the stratum corneum, or more deeply in the epidermis and dermis. The major routes of drug penetration are through intercellular channels. Factors like the drug properties, vehicle used, skin conditions, and occlusion affect the rate of absorption. Transdermal drug delivery systems are designed to control the rate of drug delivery through the skin and into systemic circulation. They aim to deliver drugs safely and effectively at a controlled rate.
This document discusses transdermal drug delivery systems. It provides information on:
1. Transdermal drug delivery involves administering therapeutic agents through intact skin for systemic effects. Only a small number of drug products are available for this route.
2. The skin provides an effective barrier for drug penetration. The epidermis is the main control element, and drugs can penetrate via hair follicles, sweat ducts, or diffusion across the stratum corneum.
3. Transdermal patches must consider the drug's properties, skin structure, and factors like permeability enhancers to effectively deliver medication through the skin.
TRANSDERMAL THERAPEUTIC DRUG DELIVERY SYSTEMS N Anusha
This document discusses transdermal therapeutic systems (TTS). It begins by defining TTS as self-contained dosage forms that deliver drugs through intact skin at a controlled rate. It then covers various topics related to TTS including advantages/disadvantages, factors affecting skin permeation, mechanisms of drug permeation, and techniques to enhance permeation like physical methods (iontophoresis, electroporation, etc.), chemical enhancers, and patch design/evaluation. The document provides details on the design, preparation, and evaluation of various TTS with the goal of improving transdermal drug delivery.
Transdermal drug delivery has made an important contribution to medical practice, but has yet to fully achieve its potential as an alternative to oral delivery and hypodermic injections. First-generation transdermal delivery systems have continued their steady increase in clinical use for delivery of small, lipophilic, low-dose drugs. Second-generation delivery systems using chemical enhancers, non-cavitational ultrasound and iontophoresis have also resulted in clinical products; the ability of iontophoresis to control delivery rates in real time provides added functionality. Third-generation delivery systems target their effects to skin’s barrier layer of stratum corneum using microneedles, thermal ablation, microdermabrasion, electroporation and cavitational ultrasound. Microneedles and thermal ablation are currently progressing through clinical trials for delivery of macromolecules and vaccines, such as insulin, parathyroid hormone and influenza vaccine. Using these novel second- and third-generation enhancement strategies, transdermal delivery is poised to significantly increase impact on medicine.
Transdermal drug delivery system- structure of skinAkankshaPatel55
Transdermal drug delivery systems (TDDS) have transcended the realm of simple nicotine patches and entered an exciting era of innovation. Gone are the days of bulky, uncomfortable adhesives; in their place stand sophisticated systems capable of delivering a myriad of therapeutic agents through the seemingly impregnable barrier of the skin. To truly understand the magic behind this technology, we delve deeper, exploring its intricate mechanisms and promising future. The journey begins with a microscopic waltz at the skin's outermost layer, the stratum corneum. Drug molecules, meticulously formulated into miniscule particles, are incorporated into a semi-permeable patch. This patch acts as a launchpad, adhering snugly to the skin and initiating the drug's odyssey. Guided by the principles of Fick's Law of Diffusion, the drug embarks on a clandestine mission. Driven by a concentration gradient, it permeates the intercellular lipids of the stratum corneum, navigating a labyrinthine path formed by keratinocytes. This passive journey, governed by factors like drug lipophilicity and skin thickness, determines the rate and extent of absorption. However, diffusion plays just the first act in this multi-part drama. Once traversing the stratum corneum, the drug encounters the viable epidermis, a dynamic landscape teeming with enzymes and metabolic pathways. Here, some compounds may undergo degradation, limiting their systemic bioavailability. To overcome this hurdle, scientists devise ingenious strategies:
Penetration Enhancers: Chemical agents like propylene glycol or oleic acid temporarily disrupt the skin's lipid packing, easing the drug's passage.
Iontophoresis: Electric current gently guides charged molecules through the skin, bypassing enzymatic barriers and boosting delivery.
Microneedle Technology: Tiny, painless needles create transient microchannels, facilitating the delivery of larger molecules like proteins and peptides. The Symphony of Controlled Release:
A key advantage of TDDS lies in their ability to sustain drug release over extended periods. This controlled release symphony is orchestrated by sophisticated reservoir systems:
Matrix Systems: The drug is homogeneously dispersed within a polymer matrix, gradually diffusing out over time.
Reservoir Systems: A distinct drug reservoir separates from the adhesive layer, allowing for precise and prolonged delivery.
Programmable Systems: Advanced patches incorporate microfluidic channels and microchips, enabling customized release profiles and even pulsatile delivery for specific therapeutic needs.
Benefits Beyond Convenience:
The charm of TDDS extends far beyond the mere convenience of avoiding needles. They offer distinct advantages over traditional oral and parenteral routes:
Enhanced Bioavailability: By bypassing first-pass metabolism in the liver, certain drugs achieve higher systemic concentrations through transdermal delivery.
Improved Patient Compliance: Continuous, hassle-free adminis
This document provides an overview of transdermal drug delivery systems. It defines transdermal therapeutic systems as self-contained dosage forms that deliver drugs through the skin at a controlled rate. The document outlines the contents to be covered, which include the advantages and structure of the skin, permeation through skin, and formulation and evaluation of transdermal drug delivery systems. It also briefly discusses the history and factors affecting permeation through skin.
This document discusses transdermal drug delivery systems (TDDS). TDDS deliver drugs through the skin at a controlled rate. Key points:
1. TDDS have advantages like delivering drugs over an extended period with less fluctuations compared to oral dosing. However, only small lipophilic drugs can currently be delivered.
2. The skin is the rate-limiting barrier, with the stratum corneum restricting drug entry and exit. Drugs must penetrate this layer to be absorbed systemically.
3. Factors like skin conditions, age, temperature, and drug properties affect transdermal permeation. Ideal TDDS components include potent drugs, polymers to control release, permeation enhancers,
The document discusses transdermal drug delivery systems (TDDS). It defines TDDS and provides their advantages over other drug delivery methods. It describes the skin structure, especially the stratum corneum layer, and how drugs penetrate the skin through various routes. Factors that affect transdermal drug permeability are outlined. Ideal drug candidates and components of TDDS like polymers and permeation enhancers are also discussed.
transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream
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The document discusses the skin and integumentary system. It describes the skin as a large organ composed of three main layers - the epidermis, dermis and subcutaneous layer. The epidermis provides protection while the dermis contains blood vessels, glands and sensory receptors. Accessory organs include nails, hair follicles, sebaceous glands and sweat glands. The skin plays an important role in temperature regulation through processes like sweating and vasodilation. Wound healing occurs through inflammation, clotting, cell reproduction and scar formation.
Quality control involves sampling, testing, and ensuring products meet specifications before release. It is focused on identifying defects in finished products. Key responsibilities include testing raw materials, conducting in-process testing, and approving or rejecting starting materials, packaging, intermediates, and finished products. Quality control aims to fulfill quality requirements and ensure only products passing tests are released.
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This document discusses factors that affect oral drug absorption. It describes three main categories of factors: physiological, physical-chemical, and formulation factors. Under physiological factors, it discusses membrane physiology, how drugs pass membranes through different transport mechanisms like passive diffusion and active transport, and gastrointestinal physiology. It provides details on the anatomy and environments of different parts of the GI tract and how they impact drug absorption. It also discusses gastric emptying time and how it affects drug absorption.
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This document discusses drug metabolism and biotransformation. It explains that drugs are chemically altered in the body through phase I and phase II reactions to make them more water soluble and able to be excreted. The major site of drug metabolism is the liver through enzymes like cytochrome P450. Factors like genetic variations, age, and drug interactions can impact an individual's ability to metabolize drugs.
1. There are three main mechanisms of drug absorption from the gastrointestinal tract: transcellular/intracellular transport, paracellular/intercellular transport, and vesicular/endocytosis transport.
2. Transcellular transport is the most common pathway and involves drugs passing across the GI epithelium, while paracellular transport through cell junctions is minor.
3. Vesicular transport involves transport of substances within vesicles across the cell membrane.
This document discusses factors that affect the distribution of drugs in the body. It covers:
- Drug distribution refers to the reversible transfer of drugs between blood and extravascular tissues. Drugs enter circulation after absorption and must cross membranes to reach tissues.
- Factors like a drug's physiochemical properties (size, ionization, lipophilicity), tissue permeability, organ perfusion rates, and binding to blood/tissue components influence its distribution. Physiological barriers like the blood-brain barrier also restrict diffusion.
- The apparent volume of distribution is a measure of how a drug is distributed between plasma and tissues after dosing. It depends on a drug's concentration in plasma and ability to concentrate in extravascular spaces
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Date: May 29, 2024
Tags: Information Security, ISO/IEC 27001, ISO/IEC 42001, Artificial Intelligence, GDPR
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2. 2
• Transdermal drug delivery systems (TDDSs) facilitate
the passage of therapeutic quantities of drug
substances through the skin and into the general
circulation for their systemic effects.
• In 1965, Stoughton first conceived of the percutaneous
absorption of drug substances.
• The first transdermal system, Transderm Scop
(Baxter), was approved by the Food and Drug
Administration (FDA) in 1979 for prevention of nausea
and vomiting associated with travel, particularly at sea.
3. 3
• The stratum corneum, being
keratinized tissue, behaves as a
semipermeable membrane, and
drug molecules penetrate by
passive diffusion.
• It is the major rate-limiting
barrier to transdermal drug
transport.
• Once through the stratum
corneum, drug molecules may
pass through the deeper
epidermal tissues and into the
dermis.
• When the drug reaches the
vascularized dermal layer, it
becomes available for absorption
into the general circulation.
4. 4
• The rate of drug movement across this layer
depends on its concentration in the vehicle, its
aqueous solubility, and the oil– water partition
coefficient between the stratum corneum and
the vehicle.
• Substances with both aqueous and lipid solubility
characteristics are good candidates for diffusion
through the stratum corneum, epidermis, and
dermis.
5. 5
Routes of penetration
• The diffusant has three potential entry routes to
the viable tissue:
• Through the hair follicles with their associated
sebaceous glands,
• Via the sweat ducts;
• ( Transcellular or Intercellular) across the
continuous stratum corneum between these
appendages
7. 7
Skin appendages
• Their fractional area available for absorption is small
(about 0.1%) and this route usually does not contribute
appreciably to the steady-state flux of a drug.
• However, the route may be important for ions and
large polar molecules that cross intact stratum
corneum with difficulty.
• For electrolytes and large molecules with low diffusion
coefficients, such as polar steroids and antibiotics, and
for some colloidal particles, the appendages may
provide the main entry route.
9. 9
Epidermal route
• The epidermal barrier function resides mainly in
the stratum corneum.
• The corneocytes, consisting of hydrated keratin,
are embedded in the in a complex lipid mixture of
ceramides, fatty acids, cholesterol and cholesterol
esters, formed into multiple bilayers.
• Most molecules penetrating through the skin use
this intercellular microroute.
11. 11
• Simplified diagram of skin structure and routes of
drug penetration,
• (a) Macroroutes:
(1) via the sweat ducts;
(2) across the continuous stratum corneum;
(3) through the hair follicles with their
associated sebaceous glands,
• (b) Representation of the stratum corneum
membrane, illustrating two possible Microroutes
for permeation ( Transcellular or Intercellular) .
12. 12
FACTORS AFFECTING
PERCUTANEOUS ABSORPTION
• Not all drug substances are suitable for Transdermal
delivery.
• Among the factors playing a part in percutaneous
absorption are the physical and chemical properties
of the drug, including its molecular weight, solubility,
partitioning coefficient and dissociation constant
(pKa), the nature of the carrier vehicle, and the
condition of the skin.
13. 13
Physicochemical factors
• Skin hydration.
• Temperature and pH.
• Diffusion coefficient
• Drug concentration
• Partition coefficient
• Molecular size and shape
14. 14
Drug concentration
• Drug concentration is an important factor.
• Generally, the amount of drug percutaneously
absorbed per unit of surface area per time
interval increases with an increase in the
concentration of the drug in the TDDS.
15. 15
the area and time of application
• The larger the area of application (the larger
the TDDS), the more drug is absorbed.
• Generally, the longer the medicated
application is permitted to remain in contact
with the skin, the greater is the total drug
absorption.
16. 16
solubility of the drug in
both lipid and water
• The drug should have a greater physicochemical
attraction to the skin than to the vehicle so that the
drug will leave the vehicle in favor of the skin.
• Some solubility of the drug in both lipid and water is
thought to be essential for effective percutaneous
absorption.
• the aqueous solubility of a drug determines the
concentration presented to the absorption site, and
the partition coefficient influences the rate of
transport across the absorption site.
17. 17
• Generally, drugs penetrate the skin better in
their unionized form.
• Non-polar drugs tend to cross the cell barrier
through the lipid-rich regions (intercellular
route), whereas the polar drugs favor transport
between cells (transcellular route).
• For example, erythromycin base demonstrates
better percutaneous absorption than
erythromycin ethyl succinate.
18. 18
Drugs molecular weight
• Drugs with molecular weights of 100 to 800
and adequate lipid and aqueous solubility can
permeate skin.
• The ideal molecular weight of a drug for
Transdermal drug delivery is believed to be
400 or less.
19. 19
Hydration of the skin
• Hydration of the skin generally favors
percutaneous absorption.
• The TDDS acts as an occlusive moisture barrier
through which sweat cannot pass, increasing
skin hydration.
20. 20
Temperature and pH
• The penetration rate of material through human skin
can change tenfold for a large temperature variation,
as the diffusion coefficient decreases as the
temperature falls.
• Clothing on most of the body would usually prevent
wide fluctuations in temperature and penetration
rates.
• Occlusive vehicles increase skin temperature by a few
degrees, but any consequent increased permeability is
small compared to the effect of hydration.
21. 21
PH
• Only unionized molecules pass readily across lipid
membranes. So when weak acids and bases
dissociate to different degrees, depending on the
pH and their pKa or pkb values. Thus, the
proportion of unionized drug in the applied phase
mainly determines the effective membrane
gradient, and this fraction depends on pH.
22. 22
Partition coefficient
• Polar cosolvent mixtures, such as propylene glycol with water,
may produce saturated drug solutions and so maximize the
concentration gradient across the stratum corneum.
• However, the partition coefficient of a drug between the
membrane and the solvent mixture generally falls as the
solubility in the solvent system rises.
• Thus, these two factors - increase in solubility and decrease in
the magnitude of the partition coefficient - may oppose each
other in promoting flux through the membrane, when the
system is not saturated.
• Hence it is important not to over solubilize a drug if the aim is
to promote penetration: the formulation should be at or near
saturation.
24. 24
Skin condition
• The intact, healthy skin is a strong barrier but many agents can
damage it.
• acids and alkalis injure barrier cells and thereby promote
penetration, as do cuts, abrasions and dermatitis.
• skins may lose their reactivity or 'harden' because of frequent
contact with irritant chemicals.
• Disease commonly alters skin condition; In diseases characterized
by a defective stratum corneum ( e.g. psoriasis), percutaneous
absorption usually increases.
• permeability increases: the skin inflamed, with loss of stratum
corneum and altered keratinization.
• permeability decreases: the organ thickened, with corns, calluses
and warts,
25. 25
Skin age
• It is often assumed that the skin of the young and
the elderly is more permeable than adult tissue
• Children are more susceptible to the toxic effects of
drugs and chemicals, partly because of their greater
surface area per unit body weight; thus potent
topical steroids, boric acid and hexachlorophane
have produced severe side-effects and death.
26. 26
Blood flow
• an increased blood flow could reduce the amount of
time a penetrant remains in the dermis, and also
raise the concentration gradient across the skin
( Sink condition ) .
Regional skin sites
• Variations in cutaneous permeability around the
body depend on the thickness and nature of the
stratum corneum and the density of skin
appendages.
27. 27
Skin metabolism
• The skin metabolizes steroid hormones, and some
other drugs.
• Such metabolism may determine the therapeutic
efficacy of topically applied compounds (particularly
prodrugs)
29. 29
CHEMICAL ENHANCERS
• increases skin permeability by reversibly
damaging or altering the physicochemical
nature of the stratum corneum to reduce its
diffusion resistance
• Among the alterations are:
• increased hydration of the stratum corneum,
• a change in the structure of the lipids and
lipoproteins in the intercellular channels through
solvent action or denaturation, or both
30. 30
skin penetration enhancers
• Water
• Sulphoxides (especially dimethylsulphoxide) and
their analogues
• Pyrrolidones
• Fatty acids and alcohols
• Azone and its derivatives
• Surfactants - anionic, cationic and non-ionic
• Urea and its derivatives
• Alcohols and glycols
• Essential oils, terpenes and derivatives
• Synergistic mixtures.
31. 31
• The selection of a permeation enhancer
should be based on:
• its efficacy in enhancing skin permeation
• its dermal toxicity (low)
• its physicochemical and biologic compatibility
with the system’s other components
32. 32
Physical methods
• Iontophoresis and Sonophoresis.
• Iontophoresis is delivery of a charged chemical compound
across the skin membrane using an electrical field.
A number of drugs have been the subject of iontophoretic
studies; they include Lidocaine; dexamethasone; amino
acids, peptides, and insulin ; Verapamil; and propranolol.
• Sonophoresis, or high-frequency ultrasound,
Among the agents examined are hydrocortisone, lidocaine,
and salicylic acid in such formulations as gels, creams, and
lotions. It is thought that high frequency ultrasound can
influence the integrity of the stratum corneum and thus affect
its penetrability.