A Seminar on

OCULAR DRUG

DELIVERY SYSTEM

VAIBHAV KATARE

1st Year M.Pharm

(Pharmaceutics)

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PRESENTED BY:

GUIDED BY:

Dr.G.S ASANE(Dept. of pharmaceutics)

• Introduction

• Anatomy And Physiology Of Eye

• Mechanism Of Ocular Absorption

• Ophthalmic Dosage Form Introduction And

Classification

• Advanced Ocular Drug Delivery System

• Marketed Ocular Drug Delivery Products

• Evaluation Of OCDDS

• Conclusion And Future Outlook

• References2 2

INTRODUCTION

• Designed to treat ophthalmic diseases.

• Meant for local therapy and not for systemic action.

• Eye - easily accessible site for topical administration.

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IDEAL CHARACTERISTICS OF OCDDS

Sterility

Isotonicity:

e.g.: 1.9% boric acid, 0.9% NaCl

Buffer/pH adjustment

Less drainage tendency

Minimum protein binding

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COMPOSITION OF EYE

Water - 98%

Solid -1.8%

Organic element – Protein - 0.67%

Sugar - 0.65%

NaCl - 0.66%

Other mineral element sodium, potassium and

ammonia - 0.79%.

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ANATOMY AND PHYSIOLOGY OF EYE

The Sclera

The Cornea

The Choroid

The Iris

The Lens

The Retina

The Conjunctiva

Vitreous Humor

Aqueous Humor

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ROUTES OF OCULAR DELIVERY

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D R U G I N T E A R F L U I D

Ocular Absorption

(5% of the dose) Systemic Absorption

(50-100% of the dose)

Major Routes:

-Conjuctiva of eye

-Nose

Minor Routes:

-Lacrimal Drainage

-Pharynx

-Aqueous Humor

-Inner Ocular Tissues

Corneal

Route:

-Primary Route.

-Small Lipophilic

Drugs.

Conjunctival

and Sclera

Route:

-Secondary Route.

-Large Hydrophilic

Drugs.

Aqueous

Humor

Ocular Tissue Elimination

MECHANISM OF OCCULAR DRUG ABSORPTION

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OPHTHALMIC DOSAGE FORM

Ophthalmic preparations are sterile products (free

from foreign particles.) that are intended to be applied

topically to cornea or instilled in the space between the

eyeball and lower eyelid (cul-de-sac cavity).

The following dosage forms have been developed to

ophthalmic drugs.

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OCULAR DELIVERY SYSTEMS

CONVENTIONAL VESICULAR

CONTROL RELEASE PARTICULATE

SOLUTION

SUSPENTION

EMULSION

OINTMENT

INSERT

GELS

IMPLANTS

IONTOPHORESIS

DENDRIMER

MICROEMULSION

NANOSUSPENSION

MICRONEEDLE

MUCOADHESIVE

POLYMERS

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MICROPARTICLES

NANOPARTICLES

LIPOSOMES

NIOSOMES

DISCOMES

CLASSIFICATION OF OCDDS

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SELECTED TYPES OF OCDDS:

1. Aqueous eye drops

2. Oily eye drops

3. Eye ointments

4. Eye lotions

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5. Paper strips

6. Ocuserts

and Laciserts

7. Hydro gel contact

lenses

8. Collagen shields

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1) CONVENTIONAL DELIVERY SYSTEMS:

Eye Drops:

Widely administered drugs as liquid dosage form

Only 5 % of the dose is absorbed

Mostly absorbed through systemic circulation.

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Ointment and Gels:

Prolongation of drug contact time.

blurring of vision & matting of eyelids

can limit its use.

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Ocuserts and Lacrisert:

Sterile Preparation

Controlled Release Dosage Form

Treatment Of Dry Eye Syndrome And Keratitis Sicca.

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2) VESICULAR SYSTEM:

Liposomes:

Liposomes are biocompatible and biodegradable lipid vesicles

made up of natural lipids.

They include the drugs with low partition coefficient, poor

solubility. 16 16

Niosomes and Discomes

They are non toxic and do not require special handling

techniques:

• Niosomes are nonionic surfactant vesicles that have

potential applications in the delivery of hydrophobic or

amphiphilic drugs.

• Discomes act as potential drug delivery carriers as they

released drug in a sustained manner at the ocular site.17

3) CONTROL DELIVERY SYSTEMS:

1. Implants

2. Iontophoresis

3. Dendrimer

4. Microemulsion

5. Nanosuspensions

6. Microneedle

7. Mucoadhesive Polymers18 18

4) PARTICULATE SYSTEM :(NANOPARTICLES AND MICROPARTICLES) The maximum permissible size limit for

microparticles is about 5-10 mm for ophthalmic

administration.

Nanoparticles are prepared using bioadhesive

polymers to provide sustained effect to the entrapped

drugs.

That is why microspheres and nanoparticles are

promising drug carriers for ophthalmic application.

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1. Scleral Plugs Therapy.

2. Gene Therapy.

3. Stem Cell Therapy.

4. Cell Encapsulation.

5. siRNA therapy.

6. Oligonucliotide therapy.

7. Aptamer.

8. Ribozyme therapy.

ADVANCED DRUG DELIVERY SYSTEM (4)

New Ophthalmic Drug Delivery System (NODDS) (7)

Delivers precise amount of drug to the eye.

Device consists of medicated film attached to paper

cover and handled by a short and thin membrane.

All components are packed individually and sterilized by

gamma irradiation.

Membrane dissolves in lacrimal fluid and delivers the drug.

Conclusion: NODS produced 8-fold increase in

bioavailability for pilocarpine with respect to standard eye

drop formulation.21

MARKETED PRODUCTS(3)

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Brand Name Drug Dosage Form Use

DICHOL Carbachol Sterile solution and

prefilled syrings

Used in ophthalmic

surgery

REFRESH

TEARS®

Hydroxypropyl-

methylcelluose

Drops Eye lubricants and

dryness of eye

GELTEAR/

VISCOTEAR

Corbomer Bioadhesive gel Treatment of

soreness, burning

Timolol® XE Timolol maleate In-situ gel Keratoconjuctivitis

PRED

FORTE®

prednisolone

acetate

suspensions Antiallergic and

anti-inflammatory

ACIVIR EYE Acyclovir Ointment Anti-infective

REFRESH®

Classic

Artificial tear fluid convenient single

use vials

Moisturizes and

relieves dry eyes

RESTASIS® Cyclosporine emulsion Chronic dry eye

diseases

EVALUATION OF OCDDS (3)

1. Thickness of film

2. Content uniformity

3. Uniformity of Weight

4. Percentage moisture absorption

5. Percentage moisture loss

6. In-vitro drug release

7. In-vivo drug release

8. Accelerated stability studies.

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CONCLUSION & FUTURE OUTLOOK (8)

Ocular drug delivery systems provide local as well as

systemic delivery of the drugs.

The novel advanced delivery systems offer more protective

and effective means of drug delivery.

The latest available targeted drug delivery systems focus

on the localised delivery of the drugs as well as certain

macromolecular substances like proteins, genes like DNA,

siRNA to the internal parts of the eye.

Further developments are preferable which will eliminate

the disadvantages of these available advanced delivery

systems and will make readily acceptable among the

patients.24

References

1. N.K.Jain, “Advances in Controlled & Novel Drug Delivery”,

CBS Publication, & distributor, New Delhi, pg No. 219-223,

110-120.

2. N. K. Sahane, “Ocular Inserts: A Review” , Drug Invention

Today 2010, 2(1), 57-64.

3. Jitendra, Sharma P.K. Banik A. and Dixit S., “A New Trend:

Ocular Drug Delivery System”, An International Journal Of

Pharmaceutical Sciences, July-2011,Vol-2,Issue-3,ISSN:

0976-7908.

4. Patel Vishal, Agrawal Y K, “Current Status And Advanced

Approaches In Ocular Drug Delivery System”, Journal of

Global Trends in Pharmaceutical Sciences, ISSN: 2230-7346,

Vol.2, Issue 2, April-June 2011, pp -131-148.25 25

5. A.Rajasekaran, K.S.G.Arul Kumaran, J.Padma Preetha And

K.Karthika, “A Comparative Review On Conventional And

6. Advanced Ocular Drug Delivery Formulations”, International

Journal Of Pharmtech Research, ISSN : 0974-4304, Vol.2,

No.1, pp 668-674, Jan-Mar 2010

7. S.L Harikumar, Arora Sonia “Nanotechnological approaches

in Ophthalmic delivery systems”, Int. J. Drug Dev. & Res.,

Oct-Dec 2011, 3(4): 9-19.

8. Venkata Ratnam G, Madhavi S, Rajesh P, “ Ocular Drug

Delivery: An Update Review”, International Journal of

Pharmacy and Biological Sciences (eISSN: 2230-7605),

Volume 1| Issue 4 |OCT-DEC |2011|437-446.

9. www.mims-india.com/date of citation on

03/12/2012/time/12.38pm

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