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Ocular Drug
Delivery
Systems
Department of
Pharmaceutics
Faculty of Pharmacy
Kabul University
Prepared by: [Link]

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3 Introduction of Ophthalmic Drug
Delivery
4 Introduction

o Ocular administration of drug is primarily associated with the need to

treat ophthalmic diseases.
o Eye is the most easily accessible site for topical administration of a
medication.
o The normal volume of tear fluid in the cul- de- suc region of human
eye is about 7= 8 microliter.
o An eye at does not blink can accommodate of about 30 microliter of
fluid, but when blinked retain only about 10 microliter.
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Cont.

o A single drop of an ophthalmic solution or suspension measures about

50 microliter( based on 20 drops/ml).
o So much of an administrated drop be lost.
o The ophthalmic preparations have advantage and disadvantage.
o The disadvantages of various types of ophthalmic preparations can be
overcome by controlled delivery systems that release a drug via
constant rate for a relatively long time.
 Composition of Eye
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o Water- 98%
o Solid- 1.8%
o Organic element- protein- 0.67%
o Sugar- 0.65%
o NaCl- 0.66%
o Other mineral elements, potassium and ammonia- 0.79%
 Human Eye Anatomy
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 Ideal Characteristics of Ophthalmic Drug
8 Delivery System

o Good corneal penetration.

o Maximizing ocular drug absorption through prolong contact time with
corneal tissue.
o Simplicity of instillation for the patient.
o Reduced frequency of administration.
o Patient compliance.
o Lower toxicity and side effect.
 Cont.
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o Minimize precorneal drug loss.

o Non- irrelative and comfortable form( viscous solution should not
provoke lachrymal secretion and reflex blinking).
o Should not cause blurred vision.
o Relatively non- greasy.
o Appropriate rheological properties and concentrations of the viscous
system.
10 Ophthalmic Formulations
 Traditional Ophthalmic Formulations
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1. Eye drops

o Eye drops are accessible in the forms of water and oil solutions,
emulsions, or suspensions of one or mire active ingredients, which
may contain preservatives if stored in multiuse packaging.

o Theses forms are sterile and isotonic.

o The optimum pH for eye drops equal that the tear fluid and is about
7.4.
 Cont.
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2. Ophthalmic solutions
o Are sterile, aqueous solutions used for , among other things, cleaning
and rinsing eyeballs.
o They are contain excipients, which, ,for, example regulate osmotic
pressure, the pH, and viscosity of the preparations.
o The also contain preservatives if stored in multiuse packaging.
 Cont.
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3. Eye ointments
o Are semisolid dosage forms for external use, usually consisting of solid
or semisolid hydrocarbon base of melting or softening point close to
human body temperature.
 Limitations of Traditional Formulations
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o Due to their low concentration, the solutions quickly leave the eye
after use, the absorption of the drug is not complete and the biological
availability is reduced.
o In addition, their short retention time in the eye often leads to
repeated doses of the drug.
o The active ingredients in eye drops are unable to penetrate the
posterior part of the eye.
o Eye drops are mainly used to treat diseases of the anterior segment
of the eye.
 Cont.
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o Ointments are sterile semi-solid dosage forms that are applied to the
conjunctiva of the eye to produce a lasting effect.
o Ointments have a higher concentration, are not eliminated from the
eye as quickly as liquid formulations, but they cause dryness of the
eye, therefore, they are less acceptable to patients.
o Advanced ophthalmic formulations can overcome some of these
challenges.
 Advanced Ophthalmic Formulations
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1. Micro emulsions
o Are promising drug forms, inexpensive to produce, and easy to
sterilize and stable, providing the possibility to introduce larger
amounts of active ingredient.
o In- vivo research and clinical examination of healthy volunteers
proved extended time periods effectiveness and increased
bioavailability of drugs applied in these forms.
 Cont.
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o The mechanism of action involves the adsorption of Nano drops

constituting a reservoir of the drug and the inner phase of
micro emulsion on the corneal surface, which limits the
overflow.
2. In situ gels
o Are viscous liquids, showing the ability to undergo sol- to- gel
transitions when influenced by external factors, like pH,
temperature.
 Cont.
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o Hydrogels formed in situ are a type of environmentally sensitive

hydrogel that rapidly adapt to the eye and quickly convert to gel.
o These types of hydrogels increase the duration of drug retention in
the eye and prevent their rapid elimination.
o In situ thermo sensitive hydrogels are not only easy to apply as eye
drops, but also prolong drug retention time and release the drug
continuously, thereby increasing bioavailability.
 Cont.
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3. Contact lenses coated with drugs

o This drug form can absorb on the surface water- soluble substances,
released after apply the drug over the eyeball for a longer period of
time.
o Hydrogels are suitable for use as contact lenses because:
• They are biocompatible
• Have excellent mechanical stability,
• As well as being permeable to water.
 Cont.
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o Hydrogel lenses are soft polymeric devices that are placed directly in
the eye, bringing the drug product into contact with the cornea.
o The most common type of hydrogel used in contact lens is silicon,
because:
• They have high oxygen permeability.
 Cont.
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4. liposomes
o Are phospholipid drug carriers.
o The pointed- out advantages of these carriers are their
biocompatibility, biodegradability, amphiphilic properties and relative
in toxicity.
5. Niosomes
o Are chemically stable, built of nonionic surfactants, two- layered
carriers used for both hydrophilic and hydrophobic particles, without
the disadvantage of liposomes( chemical instability, oxidative
degradation, of phospholipids, and expensiveness of natural
phospholipids).
 Cont.
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6. Discosomes
o Discosomes are modified forms of niosomes, which also may act as
carriers for ophthalmic drugs.
o The size varies from 12 to 16 nm.
7. Ocuserts or ocular inserts
o Are defined as sterile preparations, with a thin, multilayered, drugs-
impregnated, solid or semisolid consistency devices placed into cul-
de- suc or conjunctiva sac and whose size and shape are especially
designed for ophthalmic applications.
 Cont.
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o The classification is based on their solubility behavior:

1. Insoluble ophthalmic insert
2. Soluble ocular insert
 Marketed Products
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25 Cont.
26 References

1. Textbook on Novel Drug Delivery System (PB 2021) Paperback – 1 January 2021.
2. A Textbook of Controlled Drug Delivery Systems: With Novel Natural Controlled
Release Polymer (Hibiscus Rosa Sinensis gum) Paperback – August 16, 2019
3. Dua K, Mehta M, Pinto TD, Pont LG, Williams KA, Rathbone M, editors. Advanced
Drug Delivery Systems in the Management of Cancer. Elsevier; 2021 Jun 24.
4. Adepu S, Ramakrishna S. Controlled drug delivery systems: current status and
future directions. Molecules. 2021 Sep 29;26(19):5905.
5. Misra A, Shahiwala A. Novel Drug Delivery Technologies. Springer:
Berlin/Heidelberg, Germany; 2019
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