1
Ocular Drug
Delivery
Systems
Department of
Pharmaceutics
Faculty of Pharmacy
Kabul University
Prepared by: [Link]
2
3 Introduction, Ophthalmic
Formulations
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.
5
Cont.
o A single drop of an ophthalmic solution or suspension measures about 50
microliter( based on 20 drops/ml). 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
6
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%
Ideal characteristics of ophthalmic drug
7 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. Lower toxicity and side effect.
o Minimize precorneal drug loss.
8 Cont.
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.
9 Ophthalmic Formulations
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.
10 Cont.
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, he
pH, and viscosity of the preparations. The also contain preservatives if stored in
multiuse packaging.
11 Cont.
3. 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.
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.
12 Cont.
4. In situ gels
o Are viscous liquids, showing the ability to undergo sol- to- gel transitions when
influenced by external factors, like pH, temperature.
5. 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.
13 Cont.
6. 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.
7. liposomes
o Are phospholipid drug carriers.
o The pointed- out advantages of these carriers are their biocompatibility,
biodegradability, amphiphilic properties and relative in toxicity.
14 Cont.
8. Noisomes and Discosomes
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).
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.
15 Cont.
9. 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
conjunctival sac and whose size and shape are especially designed for
ophthalmic applications.
o The classification is based on their solubility behavior:
1. Insoluble ophthalmic insert
2. Soluble ocular insert
16 Evaluation
o Thickness of the film
o Drug content uniformity
o Uniformity of weight
o Percentage moisture absorption
o In- vitro evaluation method
• Bottle method
• Diffusion method
17
• Modified rotating basket method
• Modified rotating paddle apparatus
o In- vivo study
o Accelerated stability studies
o Metal particle test
o sterility test
o Leakage test
Marketed Products
18
19 Cont.
20 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
21
22