Ocular Drug Delivery Systems: Seminar On

Seminar on
Ocular Drug Delivery Systems
Presented By
AMAR K. RANA
M. Pharm. Part-II
Roll No. 09
Department of Pharmaceutics and Pharmaceutical Technology,

L. M. College of Pharmacy,
Ahmedabad
24 / 10 / 07 L. M. COLLEGE OF PHARMACY : PAPER – 421 : M. PHARM - II 1 / 78
CONTENTS
ROUTES FOR OCULAR DRUG DELIVERY
ELIMINATION ROUTES
CONVENTIONAL EYE PREPARARIONS
RECENT TRENDS IN ODDS

ROUTES FOR OCULAR DRUG
DELIVERY
Trans - scleral
Topical
Systemic
Intravitreal (not Shown)
CLASSIFICATION OF OCULAR DRUG
DELIVERY SYSTEMS
 LIQUIDS : SOLUTIONS SOL TO GEL SYSTEMS
SPRAYS SUSPENSIONS
EMULSIONS.
 SOLIDS : OCULAR INSERTS FILTER PAPER STRIPS

CONTACT LENSES COLLAGEN SHIELDS,
ARTIFICIAL TEAR INSERTS.
 SEMI-SOLIDS : OINTMENTS
GELS.
 MISCELLANEOUS : OCULAR IONTOPHORESIS,

VESICULAR SYSTEMS,
MUCOADHESIVE DOSAGE FORMS,
PARTICULATES,
OCULAR PENETRATION ENHANCERS.

MARKET POTENTIAL OF
VARIOUS ODDS
SOLUTIONS
OINTMENTS
62.4%
17. 4%
OTHERS
11. 5%

TOPICALLY APPLIED OCULAR DOSAGE FORM
Diffusion Dissolution Erosion Absorption

Corneal&
Drug in tear film Conjunctival
Irritation
Lacrimal
Metabolism
turnover
Also induces
lacrimation
Drug in inner
ocular
structures
Drainage & aqueous humour
ONLY 1-5 % OF
ADMINISTERED
Loss
DOSE
SOLUTIONS
Most widely used dosage form to administer
drug in eye.
Disadvantages:-
1. Less residence time.
2. Poor bio availability.
3. Stability of dissolved drug.

HOW CAN WE ENHANCE RESIDENCE TIME
OF SOLUTION DOSAGE FORM IN EYE?
TWO APPROACHES
EARLY APPROACH:- RECENT APPROACH:-

ENHANCE THE VISCOSITY SOL TO GEL SYSTEMS
METHYL CELLULOSE {PHASE TRANSITION SYSTEMS}
POLY VINYL ALCOHOL
HYDROXY PROPYL CELLULOSE
POLY VINYL PYRROLIDINE

When administered
in to Eye
Liquid CONVERTED
Droplets IN TO GEL

INITIALISATION
OF
GEL FORMATION
x √
MUST FORM
TRANSPARENT
SYSTEM

MECHANISM OF SOL - GEL TRANSITION
1 . ION DEPENDENT GELLING:-
KEY INGREDIENTS :-
 SODIUM ALGINATE &
 GELRITE®

ADD HEAT
GEL 1 GEL 2
3- DIMENTIONAL
BI-HELICAL
STRUCTURE OF
GELLAN GUM.
REF: Robinson, G., Manning, C.E., Morris, E.R., 1991, Conformation and physical
properties of the bacterial polysaccharides gellan, welan and rhamsan, in Food
polymers, gels, and colloids, Dickinson, E., Editor. Royal Society Chemistry, London.
1. CARBOXYLATE- - - - - -Ca++ - - - - - - CARBOXYLATE
STRONGER
2. CARBOXYLATE- - - - - -K+ - - - - - - CARBOXYLATE

WEAKER
2.pH DEPENDENT GELLING:-
KEY INGEDIENTS:-
 CELLULOSE ACETATE PTHALATE

 CHITOSAN
 CARBOMERS

SIALIC
ACID
Chitosan is a unique polysaccharide which has positive charge & interacts with the
sialic acid present in the mucin layer of the corneal epithelium.
This property of chitosan is responsible for use of chitosan as a penetration
enhancer.
( REF :- Polymeric materials for ophthalmic drug delivery: trends and perspectives J. Mater. Chem., 2006, 16, 3439–3443)
3.TEMPERATURE DEPENDENT GELLING:-
KEY INGREDIENTS:-
 POLOXAMER 407
 LUTROL FC - 127
4 .ENZYME DEPENDENT GELLING:-

KEY INGREDIENT:-
XANTHAN GUM :-

RECENT TRENDS IN
PHASE TRANSITION SYSTEMS
GRAFT COPOLYMERS
1. MATP AND HA GRAFTING
{Hyaluronic acid-g- poloxamer}
2. MATP AND C6S GRAFTING
{C6S-g-Poloxamer}
MATP : Mono Amine Terminated poloxamer

HA : Hyaluronic acid
C6S : Condroitin 6 - Sulphate
(Ref:-Drug Development and Industrial Pharmacy,31:455–463, 2005)
EMULSIONS
W/O MICRO EMULSIONS ARE PREFFERED.
W/O MICRO LIQUID PROVIDE

EMULSION CRYSTALINE SUSTAINED
STATE RELEASE

RABBIT CORNEAL RABBIT CORNEAL
IMAGE BEFORE IMAGE AFTER
ADMINISTATION ADMINISTRATION
(REF:- W/O microemulsions for ocular delivery: Evaluation of ocular irritation and
precorneal retention; Journal of Controlled Release 111 (2006) 145–152)
CATIONIC EMULSIONS
A BREAKTHROUGH IN
EMULSION DRUG DELIVERY
IN EYES

(REF:- CURRENT OCULAR DRUG DELIVERY CHELLENGES;INDUSTRY OVERVIEW AND DEALS;
DRUG DELIVERY REPORT AUTUMN / WINTER,2005)

ATTRACTION BETWEEN
POSITIVELY CHARGED
DROPLETS AND NEGATIVELY
CHARGED MEMBRANE

COMPARISION BETWEEN ANIONIC AND
(I) CATIONIC EMULSION

( II )

CONFIRMATION OF PENETRATION
OF CATIONIC EMUSION
UP TO THE POSTERIOR REGION OF EYE

( III )
√ √ √ √
√ √ √ √ √ √ √
√ √ √
ANIONIC EMULSION CATIONIC EMULSION
CONFOCAL LASER SCANNING MICROSCOPY PHOTOGRAPHS

OF SAMPLES INCUBATED WITH NEGATIVELY OR POSITIVELY
CHARGED EMULSIONS OFSEOF CONTAINING
THE FLOURESCENT DYE DIL C18

EYE SPRAY
Not commonly used.
Some practitioners use mydriatics or

cycloplegics alone or in combination
in the form of eye spray.
These sprays are used in the eye for dilating

the pupil or for cycloplegic examination.

OCULAR DRUG DELIVERY
DEVICES
1. Soft Contact Lenses 7. Soluble Ophthalmic
Drug Inserts (SODI)
2. Implantable Systems
8. Bioadhesive Ophthalmic
3. Ganciclovir implant Drug Inserts (BODI)
4. PROSERT® 9. Collagen Shields
5. MYDRIASERT®
6. OCUSERT®

OCULAR DRUG DELIVERY DEVICES
Provide controlled, sustained and continuous drug
delivery.
Avoid the side effects of pulsed drug delivery.
Maintain an effective drug concentration in the

target tissues &minimize the number of applications.
Limited popularity due to unnoticed expulsion from

the eye, membrane rupture etc.

Soft Contact Lenses
MOST WIDELY USED MATERIAL:-
poly-2-hydroxyethyl methacrylate
It has tendency to absorb up to 80% water.
METHOD OF DRUG LOADING :-
DISADVANTAGE :-The drug is not bound to the matrix.
MANIPULATION :-
A controlled release could be obtained by binding
the active ingredient via biodegradable covalent linkages.

Soluble Ophthalmic Drug Inserts
(SODI)
MATERIAL:-
Soluble copolymer of Acrylamide,
N-vinyl pyrrolidone, Ethyl acrylate,
cross linked poly-peptide matrix.
STRUCTURE:-
It is in the form of sterile thin films
or wafers of oval shape, weighing
15 to 16 mg.
HOW TO APPLY:-
RELEASE MECHANISM:-
STEP 1:- Hydration of matrix
STEP 2:- Diffusion
Bioadhesive Ophthalmic Drug Inserts
(BODI)
LIMIIATION OF CONVENTIOAL EYE INSERTS:-

RISK OF EXPULSION FROM THE SITE.
 TO AVOID SUCH LIMITATION,

BIOADHESIVE OPTHALMIC DRUG
INSERTS ARE DEVELOPED.

Collagen Shields
MATERIAL:- PORCINE SCLERAL TISSUE : WHICH BEARS A COLLAGEN
COMPOSITION SIMILAR TO
THAT OF THE HUMAN CORNEA.
DRUG LOADING :-BY SOAKING IN DRUG SOLUTION.
STRUCTURE :- 0.1 MM THICKNESS

6 – 9 MM DIAMETER.
ADVANTAGES:- 1) BIOLOGICAL INERTNESS

2) STRUCTURAL STABILITY
3) GOOD BIOCOMPATIBILITY
4) LOW COST OF PRODUCTION
DISADVANTAGES:-
1) INSERTION TECHNIQUE IS DIFFICULT
2) EXPULSION OF THE SHIELD MAY OCCUR
3) NOT FULLY TRANSPARENT AND THUS REDUCE VISUAL ACUITY
MARKETED PRODUCTS:-
1) MEDI LENS® ( CHIRON, IRVINE, CA)
2) PRO SHIELD® (ALCON, FORT WORTH, TX)

OCUSERT®
TRANSPARENT
RATE
CONTROLLING
MEMBRANE
DRUG – POLYMER
MATRIX
TIO2 RING
TRANSPARENT RATE
CONTROLLING
24 / 10 / 07 L. M. COLLEGE OF PHARMACY : PAPER – 421 : M. PHARM - II
MEMBRANE 36 / 78
13.4 mm x 5.7 mm x 0.3 mm
Wt :- 19 mg
OCUSERT

PROSERT®
tears
tears
tears
tears Drug release
through
membrane
• PROSERT® is an ophthalmic placebo insert which is

insoluble, sterile and biocompatible.
• It is having a matrix able to contain one or several active

components, surrounded by a dyalisantic membrane of a
changeable thickness which allows the releasing
controlled by the tears .
MYDRIASERT®
Mydriasert is an insoluble
ophthalmic insert, gradually
releasing two well-known
active ingredients:
Phenylephrine and
Tropicamide.
It is indicated in pre surgical

mydriasis.

LACRISERT®
• It is used in dry eye syndrme.
• It is made up with Hydroxy propyl
cellulose.

DEGRADATION OF LACRISERT
BEFORE 2 MONTHS AFTER

IMPLANTATION IMPLANTATION
1 MONTH AFTER 3 MONTHS AFTER

IMPLANTATION IMPLANTATION
(REF:- Kunou, N.; Ogura, Y.; Hashiozoe, M.; Honda, Y.; Hyon, S.H.; Ikada, Y. J. Contr. Rel. 1995, 37,143–150.)

COLLOIDAL SYSTEMS
FOR
OCULAR DRUG DELIVERY
LIPOSOMES
NEOSOMES
PHARMACOSOMES
NANOPARTICLES
COLASOMES
LIPOSOMES
LIPOSOMES HAVE POTENTIAL TO ACCOMMODATE

HYDROPHILIC AND LIPOPHILIC DRUG IN A SINGLE
VESICLE
IN – VIVO CORNEAL
PERMEABILITY FOR LIPOSOMES
++++
__
++++
__
> > > >
POSITIVELY CHARGED
LIPOSOMES HAS BETTER
CORNEAL PERMEABILITY
=
LIPOSOME SEEMS TO BE
IDEAL ONE BUT THIS IS NOT
SO…
MAJOR DISADVANTAGES:-
• UNSTABILITY BECAUSE DECOPOSITION
OF PHOSPHOLIPIDS IN FORMULATION.
• LIMITED DRUG LOADING CAPACITY.
• TECHNICAL DIFFICULTIES IN OBTAINING

STERILE LIPOSOMAL PREPARATION.

NEOSOMES
THEY ARE DEVELOPED TO CIRCUMVENT
THE LIMITATION OF LIPOSOMES.
ALSO KNOWN AS NON IONIC SURFACTANT

VESICLES.
MIXTURE
OF
CHOLESTEROL HYDRATION
&
SINGLE ALKYL CHAIN
NON- INONIC
SURFACTANT
NEOSOMES
DISCOSOMES
A SPECIAL TYPE OF NEOSOMES.
DISC SHAPE VESICLES AS THE NAME REVEALS.
LARGER THAN NEOSOMES SO BETTER FIT IN

TO CUL- DE - SAC AND THEREFORE NO LOSS
DUE TO DRAINAGE.

PHARMACOSOMES
• PURE DRUG VESICLES.
( IF DRUG IS AMPHIPHILIC )
• VESICLES WITH 100% DRUG LOADING.
OH
ESTERIFICATION AMPHIPHILIC
COOH COOH
DRUG
NH2
A DRUG WITH COOH OR
ACTIVE H CONTAINING PHARMACOSOMES
GROUP. GENERATED
ON DILUTION
WITH WATER
NANOPARTICLES
MOST WIDELY STUDIED COLLOIDAL SYSTEM OVER
THE PAST 2 DECADES.
THESE ARE THE POLYMERIC COLLOIDAL PARTICLES

RANGING FROM 10 nm.-1micr.m.
IN WHICH DRUG IS DISSOLVED /

ENTRAPPED /
ENCAPSULATED /
ADSORPED.
FOR OCULAR DELIVERY; NANOCAPSULES ARE

BETTER THAN NANOSPHERES.
1 . Calvo, P.; Thomas, C.; Alonso, M.J.;
VilaJato, J.; Robinson, J.R.
Int. J. Pharm. 1994, 103, 283–291.
2. Zimmer, K.; Kreuter, J.; Robinson, J.R.

J. Microencaps.1991, 8, 497–504.
In above it was clearly described that..

Nanoparticles consisting of poly (alkyl cyanoacrylate)
damaged the corneal Epithelium by disrupting the cell
membranes.

 The drug is applied with an
electrode carrying the same
charge as the drug.
 The ground electrode,

which is of the opposite
charge, is placed elsewhere
on the body to complete the
circuit.
 The drug serves as a

conductor of the current
through the tissue.
1ST GENERATION IONTOPHORETIC
DRUG DELIVERY – USING EYE CUP.
IONTOPHORETIC
DRUG DELIVERY
USING EYE CUP.
2ND GENERATION IONTOPHORETIC DRUG
DELIVERY BY OCUPHOR TECHNOLOGY
FiG: Ocular iontophoretic system using a DRUG DELIVERY

saturated hydrogel (OcuPhor), inserted into
BY OCUPHOR
the inferior cul-de-sac of a human eye.
Used by Fischer TECHNOLOGY
small silicone shell
composed of polyacetal sponge
Ocular iontophoretic system using drug-loaded disposable hydrogels.

HOW
THE KNOWLEDGE
OF
CHEMISTRY
HELPFUL
IN
DESIGNING
A PERFECT DOSAGE FORM

APPROACH:1 : CHEMICAL DRUG
DELIVERY SYSTEM
INCTIVE
ACTIVE DRUG
DRUG
WITH PERMEABITY
WITH NO
PROBLEM
PROBLEM
OF PERMEABILITY
WHEN ADMINISTERED IN EYE

IT UNDERGOES
ENZYMATIC METABOLISM
AND CONVERTED IN TO
ACTIVE FORM
AND
PROVOKE A RESPONSE
EXAMPLE:1:-
• SITE SPECIFIC AND STEREOSPECIFIC
ß – BLOKERS.
Oxime and Methoxime Analogs of β-blockers:
1. Alprenolol and
2. Betaxolol
ADVANTAGES:-
1. STABLE AT ROOM TEMPERATURE.
2. LONG LASTING IOP REDUCTION IN EYES.
3. Z / E ISOMER EQUILIBRIUM IS 300 – 500
TIMES FASTER THAN NOMAL DERIVATIVES.

EXAMPLE:-2
EPINEPHRINE DIPIVEFRIN
☺10 FOLD INCREASE IN RESPONSE WAS OBSERVED.
(Ref :-Karback, M.B.; Podos, S.M.; Haibin, T.S.; Madell,A.; Becker, B. Am. J. Ophthalmol. 1976, 81,768–772.)

APPROACH:2:-
ION – PAIR COMPLEX FORMATION
EXAMPLES:-
TIMOLOL
CARTEOLOL

APPROACH:3:-
SOFT DRUG APPROACH
Produce the desired pharmacological activity at the site
of application but at other sites do not show any action
even though the same receptor is present.
EXAMPLE:- ADAPROLOL – A ß-BLOCKER

- A NEW TOPICAL ANTIGLAUCOMA AGENT
ADVANTAGES:-
1. GOOD CORNEAL PERMEABILITY
2. BETTER STABILITY
3. LESS SIDE EFFECTS ( BRONCO-CONSTRICTION ) BECAUSE SITE
SPECIFIC ACTIVITY.

PENETRATION
ENHANCERS
Cyclodextrins
in eye drop
formulations

TEAR FILM CORNEA
Ref:-Cyclodextrin in ophthalmic drug delivery. Adv Drug Deliv Rev 36: 59–79;1999.
Dexamethasone in an
aqueous cyclodextrin
solution
Dexamethasone in
suspension (Maxidex®)
Ref:-Int J Pharm vol:104: 181–184;1994.

REF: Acta Ophthalmol. Scand. 2002: 80: 144–150
S.No Drug Formulation Category Polymers / Bases
1 Pilocarpine Ointment Miotic agent Petrolatum bases
2 Pilocarpine Emulsion Miotic agent ----
3 Pilocarpine Sol to gel Miotic agent C.A.P.
4 Pilocarpine Matrices Miotic agent HPC & PVP
Polyacrylic acid and

5 Pilocarpine Hydrogel Miotic agent
Polyacrylamide
Suspension
6 Dexamethasone ----
Anti-inflammatory
C.A.P.,
7 Dexamethasone Ocularinsert Anti-inflammatory Eudragit RS. 100
and RL 100
8 Pilocarpine nitrate Miotic agent Collagen

Ocularinsert
9 Pilocarpine nitrate Ocularinsert Miotic agent Na hyaluronate
10 Tropicamide Ocularinsert Mydriatic agent Na hyaluronate
11 Pilocarpine nitrate Gel Miotic agent Polyacrylic acid

12 Timolol Sol to gel Anti-glaucoma agent GelriteÒ
13 Timolol Maleate Ocular insert Anti-glaucoma agent (PVME - MA)
Na hyaluronate
14 Methyl Prednisolone Microspheres Anti-inflammatory
15 Flurbiprofen Gels Anti-inflammatory Pluronic F 127

16 Timolol maleate Solutions Anti-glaucoma agent Polyacrylic acid
17 Penicillin G Liposomes Antibiotic Phospholipids
18 Pilocarpine Solution Miotic agent Na hyaluronate
In-situ HPMC and
19 Timolol maleate Anti-glaucoma agent
forming gel Polyacrylic acid
Gentamicin,
20 Tobramycin and Iontophoresis Anti-infective agents
---
Ciprofloxacin
Gentamicin, Corneal
21 Tobramycin and collagen Anti-infective agents Collagen
Ciprofloxacin shield
Sulphacetamide
22 sodium and Solution Anti-infective agents ---
Trimethoprim
23 Pilocarpine Solution Miotic agent ----
Poloxamer and
24 Piroxicam Micro emulsion Anti-inflammatory
Stearylamine
Nanocapsules
25 Indomethacin Anti- inflammatory Poloxamer
Micro emulsion
26 Hydrocortisone Solution Anti-inflammatory HP-ß-CD
Chitosan and Poly-L-
27 Indomethacin Nanocapsules Anti-inflammatory
Lysine
Pilocarpine Pluronic
28 Gels Miotic agent
Hydrochloride F127,MC,HPMC
29 Ciprofloxacin Ocular insert Anti-infective agent HPMC,MC,PVP
30 Insulin Ocular devices Anti diabetic Gelatin sponge
31 Tropicamide Liposomes in gel. Mydriatic agent Polycarbophil
32 Indomethacin Solution Anti-inflammatory PluronicF68& F127
33 Ketorolac
Ocular Inserts Anti-inflammatory HPMC,PVP,MC
Tromethamine

EVALUATION
• SOLUTIONS:-
1) pH
2) sterility
3) osmolarity
• SUSPENSIONS:-
1) particle size
2) adsorption on the inner wall of container
• PHASE – TRANSITION SYSTEMS:-

1) gelling efficiency
2) transparency of formed gel
3) release pattern
• SEMISOLIDS:-
1) ease of application
2) particle size if drug is suspended.

OCULAR INSERTS:-
1) Uniformity of Thickness
2) Uniformity of Weight
3) Drug Content Uniformity
4) Percentage Moisture
5) Percentage Moisture Loss
6) In vitro Drug Release Study
7) Draize Eye Irritancy Test
8) In vivo Drug Release Study

REFERENCES
• Maria J. Alanco,Pilar calvo, Jose L. Vila-Jato. Evaluation of cationic polymer coated nanocapsules
as ocular drug carriers,Inter.J.Pharm,153(1997),41-50.
• A.Radomska,R.Dobrucki. The use of some ingredients for microemulsion preparation containing

retinol and its esters,Inter.J.Pharm.196(2000),131-134.
• M.A.Eger,F.Gamisans, F.Lacoulonche, A.chaavet, M.Espina, M.L.Garcia.Flurbiprofen-loaded

nanospheres: Analysis of the matrix structure by thermal methods,Inter.J.Pharm,179(1999)37-48.
• J.Kreuter,K.Langer, E.Matshceler,G.Lambrecht, D.Mayer, G. Troschau,F.Styeneker.Methyl

methacrylate sulfopropyl methacrylate copolymer nanoparticles for drug
delivery.Inter.J.Pharm,158(1997)219-231
• S.P.Vyas,Roop K.Khar. Controlled drug delivery (Concepts &Advances) First Edition 2002,383-
411.
• M.S.Nagarsankar,Vaishali y.Londhe,G.D.Nadkarni. Preparation &Evaluation of liposomal

formulations of tropicamide for ocular delivery ,Inter.J.Pharm.190(1999)63-71
•
• R.Gurny,S.EinmachlM.Zignani,E.Varesio,J.Heller,J.L.Veathey,C.Tabatabay. Concomitant and
controlled release of dexamethasone and 5-Flourouracil form poly(ortho ester),Inter.J.
Pharm.185(1999),189-198.
• Jagdish balsubhramanium,Shrikani jayant, Kumar Pandit, Invitro in vivo evaluation of the

Gelrite® Gellan gum based ocular delivery system for indomethacin,Acta Pharm 53(2003),251-
261.
• Marie Sherlund. Insitu gelling drug delivery systems for periodontal Anaesthesia.Ph.D. Thesis
,Acta university .(2002)

• Jing Xu, Jeffrey J. Heys, Victor h. Barocas, and Theodare W. Randolph.Permeability and diffusion
in vitreus humar : Implications for Drug Delivery.Pharm.Res. Vol.17,No.6,2000,664-669.
• Vankateshwar Rao, Somasekar shyale. Preparation & Evaluation of ocular Inserts containing
Norfloxacin.Turk.J.Med.Sci.34(2004),239-246.
• Bente steffansen, Paul Ashton, Anders Buur. Intraocular drug delivery, In vitro release studies of 5-
Flouracil from N,-alkoxy carbonyl prodrugs in silicone
• Almira I. Blazek-welsh, David G.Rhodes.Maltodextrin Based Proniosomes,AAPS Pharm Sci 2001,

3(1) Article-1, 1-8.
• A. S. Mundada and B. K. Shrikhande, Controlled Release of Ciprofloxacin Hydrochloride Drug

Development and Industrial Pharmacy, 32:443–448, 2006
• Suketu D. Desai and James Blanchard, Drug Delivery, 7:201–207, 2000
• Roberta Cavalli, M. Roosa Gasco, Patrizia chetoni, Susi Burgalassi, M. Fabrizio saettone. Solid lipid
Nanoparticles (SLN) as Ocular delivery system for tobramycin.Inter.J.Pharm. 238(2002),241-245.
• Inda P.Kaur, Alka Garg, Anil K. Singla, Beepika Agrawal. Vesicular systems in ocular drug delivery
an overview.Inter.J. Pharm,269(2004)1-14.
• P.M.Dandugi.F.V.Manvi, M.B.Patil, V.S.Mastiholimath and R.Rathod.Development and Evaluation

of ocular films of cromolyn sodium.Ind.J.Pharm. sci.2004,66(3),259-370.
• Naseem A.Charoo, Kanchan Kohli, Asgar Ali.Preparation of In situ- forming ophthalmic gels of
ciprofloxacin hyudrochloride for the treatment of bacterial conjunciivitis: Invitro –Invivo
studies.J.Pharm.sci.,Vol-92,No-2,2003,407-413Samuel H. Yalkowsky, Yang –chi Lee. Ocular
devices for the controlled systemic delivery of insulin : In vitro in vivo dissolution ,
Inter.J.Pharm,181(1999),71-77.
• Samuel H. Yalkowsky, yag-chilee, Jeffrey W. millard. Gera; K. Negvesky, Salim I.

Butrai.Formulation and in vivo evaluation of ocular insert containing phenylephrine and
tropicamide.Inter.J.Pharm,182(1999),121-126.

• 150485 e : In-vitro and in-vivo evaluation of gellan gum based ocular
inserts of phenylephrine. ; C.A., vol:147 : number 7 : august 13; 2007.
• 344379 y : Regenerating pharmaceutical composition : C.A. :vol: 146 ;
number 17 : april 23 ; 2007.
• 79232 n : sustained opthalmic delivery of gatifloxacin from in-situ
gelling system: C.A. : vol 147: july 23 :2007.
• 196937 g : piroxicam nanoparticles for ocular delivery. :C.A. : vol 147 :
august 27 :2007.

MODEL QUESTIONS:-
• EXPLAIN THE VARIOUS DEVICES FOR PROVIDING
SUSTAINED RELEASE OF DRUG TO THE EYE.
• EXPLAIN THE PHASE – TRANSITION SYSTEM FOR

ODDS.
• EXPLAIN THE ROLE OF PENETRATION ENHANCERS

IN ODDS.


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Seminar on

Ocular Drug Delivery Systems

Department of Pharmaceutics and Pharmaceutical Technology,

ROUTES FOR OCULAR DRUG DELIVERY

CONVENTIONAL EYE PREPARARIONS

RECENT TRENDS IN ODDS

24 / 10 / 07 L. M. COLLEGE OF PHARMACY : PAPER – 421 : M. PHARM - II 2 / 78

 SOLIDS : OCULAR INSERTS FILTER PAPER STRIPS

 MISCELLANEOUS : OCULAR IONTOPHORESIS,

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Diffusion Dissolution Erosion Absorption

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EARLY APPROACH:- RECENT APPROACH:-

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1 . ION DEPENDENT GELLING:-

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2. CARBOXYLATE- - - - - -K+ - - - - - - CARBOXYLATE

 CELLULOSE ACETATE PTHALATE

24 / 10 / 07 L. M. COLLEGE OF PHARMACY : PAPER – 421 : M. PHARM - II 16 / 78

4 .ENZYME DEPENDENT GELLING:-

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MATP : Mono Amine Terminated poloxamer

W/O MICRO LIQUID PROVIDE

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ANIONIC EMULSION CATIONIC EMULSION

CONFOCAL LASER SCANNING MICROSCOPY PHOTOGRAPHS

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Not commonly used.

Some practitioners use mydriatics or

These sprays are used in the eye for dilating

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4. PROSERT® 9. Collagen Shields

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Avoid the side effects of pulsed drug delivery.

Maintain an effective drug concentration in the

Limited popularity due to unnoticed expulsion from

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METHOD OF DRUG LOADING :-

DISADVANTAGE :-The drug is not bound to the matrix.

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LIMIIATION OF CONVENTIOAL EYE INSERTS:-

 TO AVOID SUCH LIMITATION,

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DRUG LOADING :-BY SOAKING IN DRUG SOLUTION.

STRUCTURE :- 0.1 MM THICKNESS

ADVANTAGES:- 1) BIOLOGICAL INERTNESS

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• PROSERT® is an ophthalmic placebo insert which is

• It is having a matrix able to contain one or several active

It is indicated in pre surgical

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BEFORE 2 MONTHS AFTER