Key words: Ophthalmic Irritancy, advanced ocular therapy, Ocular Drug Delivery, safety evaluation

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Presented By
SYEDA AMENA
B.pharm (2017)
DEPARTMENT OF PHARMACEUTICS
DECCAN SCHOOL OF PHARMACY

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 INTRODUCTION
 COMPOSITION OF EYE
 ANATOMY AND PHYSIOLOGY
 MECHANISM OF OCCULAR ABSORPTION
 FACTORS AFFECTING INTRA OCCULAR BIOAVABILITY
 BARRIERS FOR OCULAR DELIVERY
 ROUTES OF DRUG DELIVERY IN EYES
 TYPES OF OCCULAR DRUG DELIVERY SYSTEM
 ADVANTAGES OF ODDS
 DISADVANTAGES OF ODDS
 RECENT FORMULATION TRENDS IN ODDS
 EVALUATION
 CONCLUSION
 REFERENCES

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• Ocular administration of drug is primarily associated with
the need to treat ophthalmic disease.
• Eye is the most easily accessible site for topical
administration of a medication..
• Ideal ophthalmic drug delivery must be able to sustain the
drug release and to remain in the vicinity of front of the eye
for prolong period of time.

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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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1) Lacrimal Fluid
2) Nasolacrimal Drainage
3) Molecular size
4) Partition Coefficient
5) Protein Binding
6) Charge

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CORNEAL CONSTRAINTS:
Cornea as rate limiting barrier
Protects front of the eye
BLOOD – RETINAL BARRIER
Protects back of the eye
PRECORNEAL CONSTRAINTS :
 Solution drainage-drains from pre corneal area
 Nasolacrimal drainage-absorbed across nasal mucosa in systemic
circulation
 Conjuctival drainage-major site for drainage
 Tear turnover-amount of tears circulated
 Dilution by tears-decreases absorption
 Metabolism in pre corneal area
 Misc: drug entity, pH, tonicity of dosage form etc

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NON ERODIBLE INSERTS
 Ocusert
 Contact lens
ERODIBLE INSERTS
 Lacriserts
 SODI
 Mindisc

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NON ERODIBLE INSERTS
Ocusert
 The ocusert therapeutic system is a flat, flexible, elliptical device
designed to be placed in the inferior cul-de-sac between the sclera and the
eyelid and to release pilocarpine continuously at a steady rate for 7 days.
 The device consist of 3 layers
1. Outer Layer – Ethylene vinyl acetate copolymer layer.
2. Inner core – Pilocarpine gelled with alginate main polymer.
3. A retaining ring – Composed of EVA impregnated with titanium.

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Contact Lens :
Presoaked Hydrophilic lens.
Drug Release : within 1st30 Min.
 Alternate approach : incorporate drug either
as soln or suspension of solid monomer
mixture.
Release rate is up to : 180 hr
Erodible Inserts
1.Lacrisert:
Sterile, Rod Shaped device.
 Composition: HPC without preservative.
 Weight:5mg,
Dimension:Diameter:12.5mm, Length:3.5mm
Use:-For the treatment of dry eye syndromes

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2.SODI: Soluble Ocular Drug Insert.
Small water soluble developed for Cosmonauts by soviet scientists who could not use
their eye drop in weightless conditions.
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
3.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 pre polymer.
Hydrophilic or Hydrophobic.
Drug release for 170 hr.
Further increase in gentamycin sulphateto 320 hrs

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Increased contact time and thus improved bio-availability.
Possibility of providing a prolonged drug release and thus a better efficacy.
Administration of an accurate dose in the eye and thus a better therapy.
Reduction of systemic side effects and thus reduced adverse effects.
Reduction of the number of administrations and thus better patient.
Compliance, Comfort.
Lack of explosion.
Ease of handling and insertion.
The insert may be lost immediately.
The necessity of using preservative.
Its poor bioavilibility

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Conventional delivery systems
EYE DROPS
OINTMENT AND GELS:
Prolongation of drug contact time with the external ocular surface
can be achieved using ophthalmic ointment vehicle

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 Gel containing pilocarpine was used to provide sustain action
over a period of 24 hours.
VESICULAR SYSTEM:
a) Liposome:
Liposome are biocompatible and biodegradable lipid
vesicles made up of natural lipids and about 25–10 000
nm in diameter
b) Nisomes
They are osmotically active and relatively stable.
They be have invivo alike liposome's.
c) Pharmacosomes
When they were administered into the eye, the
lysosomal enzymes cause cleavage of drug from the
glyceride moiety

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Iontophoresis: - In Iontophoresis direct current drives ions into cells or tissues.
For Iontophoresis the ions of importance should be charged molecules of the
drug.
Dendrimers: Dendrimers are successfully used for different routes of drug
administration and have better water-solubility, bioavailability and
biocompatibility.
Collagen Shield: Collagen shield basically consist of cross linked collagen,
fabricated with foetal calf skin tissue and developed as a corneal bandage to
promote wound healing.
CONTROL DELIVERY SYSTEMS:
d) Discomes
They are large structure formed by solubilisation of niosomes with a non-
ionic surfactant .
They act as drug reservoirs, as they are capable of entrapping water soluble
solutes.

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CONTROL DELIVERY SYSTEMS:
PARTICULATES SYSTEM (NANOPARTICLES AND MICROPARTICLES)
The maximum size limit for microparticles for ophthalmic administration is
about 5-10 mm.
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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RETRO METABOLIC DELIVERY SYSTEM

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 Uniformity of Thickness: The thickness of the ocular
insert between 0.263+-0.0054mm to 0.352+-0.0036mm.
 Uniformity of Weight: The weight of the ocular insert
were found to be in the range of 21.94+- to 26.51+-0.4475mg.
 Drug Contain Uniformity
 Determination of Surface pH
 % Moisture Absorption
% moisture absorbed = Final weight – Initial weight × 100
Initial weight
% Moisture Loss
% moisture loss = Initial weight – Final weight × 100
Initial weight

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 In-Vitro Evaluation Methods
Bottle method
Diffusion method
Modified rotating basket method
 In-Vivo Evaluation Methods
Rabbit is used as an experimental animal
because of a number of anatomical and
physiological ocular similarities and also
due to larger size of the eye.

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 Ocular drug delivery has to overcome unique barriers.
 However, several approaches have been show
experimentally to improve ocular drug absorption.
 Constantly increasing understanding of the absorption
processes offers new possibilities in the future.
 It seems that new tendency of research in ocular drug
delivery system is directly towards a combination of several
drug delivery technologies.

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1) Yie W. Chien: Novel Drug delivery systems, Introduction to eye, volume
50(2nd edition); 269-300.
2) N.K .Jain: Controlled and novel drug delivery system; Structure and
function of eye in man, 82-99.
3) Howard C. Ansel: Pharmaceutical dosage form and drug delivery system,
Anatomy of eye and orbit; 7th edition, 244,547-551.
4) K. P. Sampath Kumar, et al : Ocular Inserts: A Novel Controlled Drug
Delivery System . The Pharma Innovation - Journal , Vol. 1 No. 12 2013 .
5) Ramaiyan Dhanapal et al :Ocular Drug Delivery System. International
Journal of Innovative Drug Discovery .
6) K.S.G.Arul Kumaran,etal:Comparative Review On Conventional And Ad
vanced Ocular Drug Delivery Formulations. International Journal of
Pharmacy and Pharmaceutical Sciences , Vol 2, Issue 4, 2010 .
7) D. Satya Sireesha, et al :Advanced Approaches And Evaluation Of Ocular
Drug Delivery System. Ajptr, Volume 1, Issue 4, 2011.
8) Shravan Kumar Paswan, et al : Advance Technique In Ocular Drug
Delivery System..wjpps, Vol 4, Issue 05, 2015.

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