ocular drug delivery system

WELCOME:

WELCOME 1

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PRESENTED BY : PATTEKARI SURAJ N. M.PHARM-I (P’ceut), UNDER THE GUIDANCE OF: DR. DIAS R.J. M.PHARM Ph.D SATARA COLLEGE OF PHARMACY,SATARA A SEMINAR ON ADVANCES IN OCULAR DRUG DELIVERY SYSTEM 2

CONTENTS:

CONTENTS Objectives Introduction Anatomy Of Eye Barriers In Ocular Absorption Ocular Absorption Use of Mucoadhesives in Ocular Drug Delivery Nanoparticulate Dug Delivery Ocular Inserts Liposomes In Ocular Drug Delivery Future trends Conclusion References 3

OBJECTIVES:

OBJECTIVES To study the ocular drug delivery system in detail. To explore the success, limitations and future trends of ocular drug delivery system. 4

INTRODUCTION:

INTRODUCTION A drug delivery to circumvent ailments of eye. A challenge to formulator is to avoid protective barrier of eye Importance of cornea. Conventional ocular drug delivery system Need of a successful design 5

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OCULAR ANATOMY AND PHYSIOLOGY 7

ANATOMY OF EYE :

ANATOMY OF EYE 8

BARRIERS IN OCULAR ABSORPTION:

BARRIERS IN OCULAR ABSORPTION Precorneal Constraints It include – Solution drainage Lacrimation Tear dilution Tear turnover Conjunctival absorption Corneal constraints Cornea as rate limiting barrier Anatomy of cornea 1.Outer-Epithelium(lipophilic), 2.Middle-Stroma(hydrophilic), 3.Inner-Endothelium(lipophilic 9

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OCULAR ABSORPTION 10

GENERAL PATHWAY FOR OCULAR ABSORPTION:

GENERAL PATHWAY FOR OCULAR ABSORPTION 11

ADVANCED OCULAR DRUG DELIVERY SYSTEMS :

ADVANCED OCULAR DRUG DELIVERY SYSTEMS 12

USE OF MUCOADHESIVES IN OCULAR DRUG DELIVERY:

USE OF MUCOADHESIVES IN OCULAR DRUG DELIVERY Mucoadhesives contain the dosage form which remains adhered to cornea until the polymer is degraded or mucus replaces itself. Types- Naturally Occurring Mucoadhesives- Lectins, Fibronectins Synthetic Mucoadhesives-PVA,Carbopol, carboxy methyl cellulose, cross-linked polyacrylic acid Drugs incarporated in to this are pilocarpine, lidocaine, benzocaine and prednisolone acetate. 13

Mechanism of mucoadhesion:

Mechanism of mucoadhesion The polymer undergoes swelling in water, Entanglement of the polymer chains with mucin on the epithelial surface. The un-ionized carboxylic acid residues on the polymer form hydrogen bonds with the mucin. The water-swellable yet water-insoluble systems are preferred 14

NANOPARTICULATE DRUG DELIVERY:

NANOPARTICULATE DRUG DELIVERY 15

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Advantages of nanoparticles Sustained drug release and prolonged therapeutic activity Site-specific targeting Higher cellular permeability Protect the drug from chemical or enzymatic hydrolysis Efficient in crossing membrane barriers -blood retinal barrier Act as an inert carrier for ophthalmic drugs 16

Preparation of Nanoparticles:

Preparation of Nanoparticles 17 Solvent evaporation method

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OCULAR INSERTS:

OCULAR INSERTS Sterile preparations, with a thin, multilayered, drug-impregnated, solid or semisolid consistency devices placed into cul-de-sac or conjunctival sac. Advantages Increasing contact time and thus improving bioavailability. Providing a prolong drug release and thus a better efficacy. Reduction of systemic side effects and thus reduced adverse effects. Reduction of the number of administrations and thus better patient compliance. 19

Desired criteria for ocular inserts:

20 Desired criteria for ocular inserts Ease of handling and insertion Lack of expulsion during wear Reproducibility of release kinetics (Zero-order drug delivery) Applicability to variety of drugs Non-interference with vision and oxygen permeability. Sterility. Ease of manufacture

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A) Insoluble inserts-:

A) Insoluble inserts- e.g. Ocusert ® : 20-40µg/hr for 7day Annular ring : Impregnated with Ti0 2 : For Visibility 22 1. Diffusional Inserts : Central reservoir of drug enclosed in Semi permeable or microporous membrane for diffusion of drug. Diffusion is controlled by Lacrimal Fluid penetrating through it. Release follows : Zero Order Kinetics .

3) Contact Lens ::

3) Contact Lens : Presoaked Hydrophilic lens. Drug Release : within 1 st 30 Min. Alternate approach : incorporate drug either as sol n or suspension .e.g. Pilocarpine . Release rate is up to : 180 hr. 23 2) Osmotic inserts A central part surrounded by a peripheral part Central part-single reservoir or two distinct compartments. Peripheral part- an insoluble semi permeable polymer. The tear fluid diffuse and induces dissolution. Solubilized deposits generate a hydrostatic pressure. Drug is then released through these apertures

B) Soluble Inserts:

B) Soluble Inserts 1.SODI: Soluble Ocular Drug Insert . 24 Small water soluble made of soluble synthetic polymers. Composition : Acryl amide, Vinyl Pyrolidone , Ethylacrylate . Weight 15-16 mg. In 10-15 sec Softens; In 10-15 min. turns in Viscous Liquids; After 30-60min. Becomes Polymeric Solution. Single SODI application : replaces 4-12 eye drops Instillation, or 3-6 application of Ointments. Once a day treatment of Glaucoma. Advantages of SODI :

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25 2.The corneal collagen shield A disposable, short-term therapeutic bandage lens for the cornea. It conforms to the shape of the eye, protects the corneal surface, and provides lubrication as it dissolves. The shields are derived from bovine collagen and are 14.5 mm in diameter. Sterilized by gamma irradiation. Disadvantages It is not optically clear. The collagen shield causes some discomfort. Clinical uses Wound healing. Treatment of dry eye.

C) Biodegradable inserts:

1.Lacrisert: Sterile, Rod Shaped device. Composition: HPC. Weight:5mg, Dimension:Diameter:12.5mm, Length:3.5mm Use:-Dry eye treatment. 2. Minidisc: It is made up of counter disc with Convex front & Concave back surface in contact with eye ball. 4-5mm in diameter. Composition : Silicon based polymer. Drug release upto170 hr. 26 C) Biodegradable inserts

LIPOSOMES:

LIPOSOMES 27

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Preparation Of Liposomes:

Preparation Of Liposomes Reverse phase evaporation method 29

Degradation and Drug Release Of Liposomes:

Degradation and Drug Release Of Liposomes 30 Endocytosis 2. Fusion

FUTURE TRENDS:

FUTURE TRENDS The sustained and controlled release technologies are being proposed and the possible benefits of using liposomes, nanoparticles and inserts will be at store in future. Targeted drug delivery with modifications of conventional, advanced and novel ocular drug deliveries has potential as future drug delivery for eye. It is possible to the give effective ocular drug delivery to any part of the eye. 31

CONCLUSION:

CONCLUSION Very few advanced ocular drug delivery systems have been commercialized. The performance of these new products, however, is still far from being perfect. Major improvements are required in each of the technologies discussed in this study. More clinical studies are necessary to provide further information and insights into these advanced ocular drug delivery systems . 32

REFERENCES:

REFERENCES Mitra Ashim k., Opthalmic Drug Delivery System, Marcel Dekker Inc., 1993,1-59,83-111,199-289. Jain N.K., Controlled and Novel Drug Delivery, CBS Publisher, 2004, 82-100. Das Swarnali , K. Preeti , Drug delivery to eye: Special reference to nanoparticles , International Journal of Drug Delivery 2, 2010, 12-21. Rathore K. S., R. Nema , Review on Ocular Inserts Int.J . PharmTech Res.2009, 1(2),164-169. Web Searched: http://www.google/images/eye/anatomy& physiology 33

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The eyes are the mirror of the soul… Take care of your eyes with gentleness . THANK YOU… 34