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Presented By:
Ruchi Pal
M. Pharm. (Pharmaceutics)
2nd Sem. 2019-20 Batch
Ocular Drug Delivery System
CSJM University Kanpur
University Institute of Pharmacy
CONTENTS
Introduction1
Anatomy of Eye2
Barriers of Drug Penetration3
Dosage forms of ODDS4
5 Evaluation of ODDS
References6
INTRODUCTION
Pharmaceutical preparation that are applied topically to the eye for the treatment of
surface and intra ocular dysfunction are called Ocular Drug Delivery System.
Ocular administration of drug is primarily associated with the need to treat ophthalmic
diseases.
Advantages-
1.Increased accurate dosing , To overcome the side effects .
2.To provide sustained and controlled drug delivery.
3.To increase the ocular bioavailability of drug .
4.To provide targeting within the ocular globe , prevent the loss to other ocular tissues.
5.To provide comfort , better compliance .
Anatomy of EYE
Diameter 23 mm
Fluid systems in eye
1. Aqueous humor
● Secreted from blood
through epithelium of the
ciliary body.
● Secreted in posterior
chamber and transported to
anterior chamber.
2. Vitreous humor
● Secreted from blood
through epithelium of the
ciliary body.
● Diffuse through the vitreous
body.
Mechanism of Ocular Absorption
1.Non - corneal absorption:
● Penetration across sclera & conjunctiva into intra ocular tissues.
● Non productive - because penetrated drug is absorbed by
general circulation.
2.Corneal absorption:
● Outer epithelium - Pore size 60 only access to small ionic and
lipophilic molecules.
● Trans cellular transport - transport between corneal epithelium
and stroma.
Å
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Barriers of ODDS
Pre-Corneal Barrier Post-Corneal Barrier
Drainage Post Corneal Absorption
Lacrimation Post Sclera Absorption
Tear Dilution Enzymatic Degradation
Drug Protein Binding
Drug Metabolism
Nasolacrimal Drainage
Nasolacrimal Drainage - Tear flow from the external eye to the
nasal cavity
Lacrimation - Abnormal secretion of tears.
● Sterility
● Isotonicity - eg 1.9% boric acid, 0.9% NaCl
● Buffer/pH adjustment
● Less drainage tendency
● Minimum protein binding
● Non Toxic
IDEAL CHARACTERISTICS OF ODDS
CONVENTIONAL-
SOLUTION,
SUSPENSION,
EMULSION ,
OINTMENT
INSERT,
GELS
VESICULAR-
LIPOSOMES
NIOSOMES
DISCOMES
PHARMACOSOMES
ADVANCED-
SCLERAL PLUGS
GENE DELIVERY
STEM CELL
CONTROL RELEASE-
IMPLANTS
HYDROGELS
DENDRIMERS
POLYMERIC SOLUTIONS
CONTACT LENSES
CYCLODEXRIN
MICROEMULSIONS
NANO SUSPENSION PARTICULATE-
Nanoparticles
Microparticles
OCULAR
DELIVERY
SYSTEMS
INSERTS CLASSIFICATION
1. NON ERODIBLE INSERTS
i. Ocusert
ii. Contact lens
2. ERODIBLE INSERTS
i. Lacriserts (Sterile rod shaped device made up of propyl cellulose without any
preservative)
ii. SODI (soluble ocular drug inserts)
iii. Minidisc (4 to 5 mm).
Ocuserts
● A retaining ring of the same material
impregnated with titanium dioxide encloses the
drug reserve oil.
● When this is placed under the upper or lower
eyelid, the pilocarpine molecules dissolves in
the lacrimal fluid and releases at predefined
rates.
● Ocular insert (Ocusert) are sterile preparation
that prolong residence time of drug with a
controlled release manner.
•
Lacriserts
.This is an sterile rod shape device i.e. placed in our
eye to treat dry eyes.
.It is usually use when an artificial tears solution is
not successful .
.This medication may also be used to treat certain
other eye disorders (Keratitis, decreased corneal
sensitivity).
.Inserted into Inferior fornix.
.Composition-Propyl cellulose(without preservative)
Liposomes
● Biocompatible and biodegradable lipid vesicles made up of natural
lipids and about 25–10 000 nm in diameter.
● Limitations - Liposomes are chemical instability, oxidative degradation
of phospholipids, cost and purity of natural phospholipids.
Niosomes
● Chemically stable and can entrap both hydrophobic and hydrophilic
drugs.
● Non-ionic surfactant vesicles that have potential applications in the
delivery of hydrophobic or amphiphilic drugs.
Pharmacosomes
● When they were administered into the eye,
the lysosomal enzymes cause cleavage of
drug from the glyceride moiety.
Discomes
• They are large structures formed by
solubilisation of niosomes with a non-ionic
surfactant.
• They act as drug reservoirs, as they are
capable of entrapping water soluble solutes.
EVALUATION OF ODDS
● THICKNESS OF THE FILM
● DRUG CONTENT UNIFORMITY
● UNIFORMITY OF WEIGHT
● PERCENTAGE MOISTURE ABSORPTION
% moisture absorbed = Final weight – initial weight/initial weight x 10
In-Vitro EVALUATION METHODS
● BOTTLE METHOD
● DIFFUSION METHOD
>MODIFIED ROTATING BASKET METHOD
>MODIFIED ROTATING PADDLE APPARATUS
Limitations
1.Interference with vision.
2.Dosage form can not be terminated during emergency
3.Poor Patient Compliance .
4. Difficulty in placement and removal.
5. Occasional lose during sleep or while rubbing eyes.
6. Movement around the eye.
References:
• Brahmankar D. M., Jaiswal B., “Biopharmaceutics and Pharmacokinetics” - A
Treatise Vallabha Prakashan; Third Edition (2019) Page No. 473-476.
• Jain N. K., “Advances In Controlled & Novel Drug Delivery” CBS Publication,
First Edition 1997 Page No. 82-96.
• Gote. V, Sikder. S, Sicotte. J & Pal. D “Ocular Drug Delivery: Present
Innovations and Future Challenges” Journal Of Pharmacology and
Experimental Therapeutics. May 9 2019.
• Bhavishkar T. D., Jain K. D. “Novel Drug Deliver Systems” Nirali Prakashan
First Edition. 2012. Page No. 112-119.
THANK YOU

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Ocular Drug Delivery System

  • 1. Presented By: Ruchi Pal M. Pharm. (Pharmaceutics) 2nd Sem. 2019-20 Batch Ocular Drug Delivery System CSJM University Kanpur University Institute of Pharmacy
  • 2. CONTENTS Introduction1 Anatomy of Eye2 Barriers of Drug Penetration3 Dosage forms of ODDS4 5 Evaluation of ODDS References6
  • 3. INTRODUCTION Pharmaceutical preparation that are applied topically to the eye for the treatment of surface and intra ocular dysfunction are called Ocular Drug Delivery System. Ocular administration of drug is primarily associated with the need to treat ophthalmic diseases. Advantages- 1.Increased accurate dosing , To overcome the side effects . 2.To provide sustained and controlled drug delivery. 3.To increase the ocular bioavailability of drug . 4.To provide targeting within the ocular globe , prevent the loss to other ocular tissues. 5.To provide comfort , better compliance .
  • 5. Fluid systems in eye 1. Aqueous humor ● Secreted from blood through epithelium of the ciliary body. ● Secreted in posterior chamber and transported to anterior chamber. 2. Vitreous humor ● Secreted from blood through epithelium of the ciliary body. ● Diffuse through the vitreous body.
  • 6. Mechanism of Ocular Absorption 1.Non - corneal absorption: ● Penetration across sclera & conjunctiva into intra ocular tissues. ● Non productive - because penetrated drug is absorbed by general circulation. 2.Corneal absorption: ● Outer epithelium - Pore size 60 only access to small ionic and lipophilic molecules. ● Trans cellular transport - transport between corneal epithelium and stroma. Å
  • 7. Enter subtitle Click here to add content of the text, and briefly explain your point of view. 01 Enter subtitle Click here to add content of the text, and briefly explain your point of view. 02 Enter subtitle Click here to add content of the text, and briefly explain your point of view. 03 Enter subtitle Click here to add content of the text, and briefly explain your point of view. 04 Enter title Enter subtitle
  • 8. 02 Enter your text here, or paste your text here. Barriers of ODDS
  • 9. Pre-Corneal Barrier Post-Corneal Barrier Drainage Post Corneal Absorption Lacrimation Post Sclera Absorption Tear Dilution Enzymatic Degradation Drug Protein Binding Drug Metabolism Nasolacrimal Drainage Nasolacrimal Drainage - Tear flow from the external eye to the nasal cavity Lacrimation - Abnormal secretion of tears.
  • 10. ● Sterility ● Isotonicity - eg 1.9% boric acid, 0.9% NaCl ● Buffer/pH adjustment ● Less drainage tendency ● Minimum protein binding ● Non Toxic IDEAL CHARACTERISTICS OF ODDS
  • 11. CONVENTIONAL- SOLUTION, SUSPENSION, EMULSION , OINTMENT INSERT, GELS VESICULAR- LIPOSOMES NIOSOMES DISCOMES PHARMACOSOMES ADVANCED- SCLERAL PLUGS GENE DELIVERY STEM CELL CONTROL RELEASE- IMPLANTS HYDROGELS DENDRIMERS POLYMERIC SOLUTIONS CONTACT LENSES CYCLODEXRIN MICROEMULSIONS NANO SUSPENSION PARTICULATE- Nanoparticles Microparticles OCULAR DELIVERY SYSTEMS
  • 12. INSERTS CLASSIFICATION 1. NON ERODIBLE INSERTS i. Ocusert ii. Contact lens 2. ERODIBLE INSERTS i. Lacriserts (Sterile rod shaped device made up of propyl cellulose without any preservative) ii. SODI (soluble ocular drug inserts) iii. Minidisc (4 to 5 mm).
  • 13. Ocuserts ● A retaining ring of the same material impregnated with titanium dioxide encloses the drug reserve oil. ● When this is placed under the upper or lower eyelid, the pilocarpine molecules dissolves in the lacrimal fluid and releases at predefined rates. ● Ocular insert (Ocusert) are sterile preparation that prolong residence time of drug with a controlled release manner.
  • 14. • Lacriserts .This is an sterile rod shape device i.e. placed in our eye to treat dry eyes. .It is usually use when an artificial tears solution is not successful . .This medication may also be used to treat certain other eye disorders (Keratitis, decreased corneal sensitivity). .Inserted into Inferior fornix. .Composition-Propyl cellulose(without preservative)
  • 15. Liposomes ● Biocompatible and biodegradable lipid vesicles made up of natural lipids and about 25–10 000 nm in diameter. ● Limitations - Liposomes are chemical instability, oxidative degradation of phospholipids, cost and purity of natural phospholipids. Niosomes ● Chemically stable and can entrap both hydrophobic and hydrophilic drugs. ● Non-ionic surfactant vesicles that have potential applications in the delivery of hydrophobic or amphiphilic drugs.
  • 16. Pharmacosomes ● When they were administered into the eye, the lysosomal enzymes cause cleavage of drug from the glyceride moiety. Discomes • They are large structures formed by solubilisation of niosomes with a non-ionic surfactant. • They act as drug reservoirs, as they are capable of entrapping water soluble solutes.
  • 17. EVALUATION OF ODDS ● THICKNESS OF THE FILM ● DRUG CONTENT UNIFORMITY ● UNIFORMITY OF WEIGHT ● PERCENTAGE MOISTURE ABSORPTION % moisture absorbed = Final weight – initial weight/initial weight x 10 In-Vitro EVALUATION METHODS ● BOTTLE METHOD ● DIFFUSION METHOD >MODIFIED ROTATING BASKET METHOD >MODIFIED ROTATING PADDLE APPARATUS
  • 18. Limitations 1.Interference with vision. 2.Dosage form can not be terminated during emergency 3.Poor Patient Compliance . 4. Difficulty in placement and removal. 5. Occasional lose during sleep or while rubbing eyes. 6. Movement around the eye.
  • 19. References: • Brahmankar D. M., Jaiswal B., “Biopharmaceutics and Pharmacokinetics” - A Treatise Vallabha Prakashan; Third Edition (2019) Page No. 473-476. • Jain N. K., “Advances In Controlled & Novel Drug Delivery” CBS Publication, First Edition 1997 Page No. 82-96. • Gote. V, Sikder. S, Sicotte. J & Pal. D “Ocular Drug Delivery: Present Innovations and Future Challenges” Journal Of Pharmacology and Experimental Therapeutics. May 9 2019. • Bhavishkar T. D., Jain K. D. “Novel Drug Deliver Systems” Nirali Prakashan First Edition. 2012. Page No. 112-119.