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Novel approach of
OPTHALMIC DRUG DELIVERy
SYSTEMS
Under the Esteemed Guidance of
Dr.B.Vasudha
Department of Pharmaceutics
Presented By
P.Jeevan Reddy
Roll no:12H61S0320
Pharmaceutics(Shift-1)
CONTENTS
INTRODUCTION
ANATOMY OF EYE
BARRIERS FOR OCULAR DDS
CLASSIFICATION
TYPES OF OCULAR DDS
GENERAL SAFETY CONCERNS
ADVANCES IN OCULAR DDS
EVALUATION METHODS
CONCLUSION
REFERENCES
INTRODUCTION
 Traditionally used eye drop formulations lacked good
bioavailability and had low patient compliance, hence
most investigations in this field emphasize on the
duration of action and enhancement of corneal
absorption
 Recent developments in ophthalmic drug delivery
systems include use of gelling polymers, prodrugs,
microspheres, nanoparticles, liposomes and
hydrophilic ocular inserts. Protein and peptide
delivery, posterior drug delivery and non-aqueous
vehicles are new areas of interest in ophthalmic drug
delivery.
• The Ophthalmic Drug Delivery Systems (ODDS)
are desired to improve efficacy, minimization of
toxicity, sustained effect or modified drug release.
• Cyclodextrin cyclic oligosaccharides are the
newer carriers in ODDS which have proved to be
useful for controlled release by forming a
complex which is known to show rapid and
quantitative drug release.
RELEVANT ANATOMY AND
PHYSIOLOGY OF THE EYE
• HUMAN EYE : The accessory structures of the
eye are the eyelids, eyelashes, eyebrows, the lachrymal
apparatus and extrinsic eye muscles. The diameter of
eye is 23mm.
General Pathway For Ocular
Absorption
BARRIERS FOR OCULAR DELIVERY
 Drug loss from the ocular surface after instillation, the flow
of lacrimal fluid removes instilled compounds from the
surface of the eye.
 Even though the lacrimal turnover rate is only about 1
μl/min the excess volume of the instilled fluid is flown to
the nasolacrimal duct rapidly in a couple of minutes.
 Another source of non-productive drug removal is its
systemic absorption instead of ocular absorption.
 Systemic absorption may take place either directly from the
conjunctival sac via local blood capillaries or after the
solution flow to the nasal cavity.
Approaches to improve ocular
bioavailability
1) Viscosity enhancers 8) Eye ointments
2) Gel 9) Prodrug
3) Penetration enhancers 10) Liposomes
4) Niosomes 11) Nanosuspension
5) Microemulsion
6) Nanoparticles/nanospheres
7) In situ-forming gel
 Classification Of Ophthalmic
Dosage Form:
1)Based on route of administration:
a)Topical solution
b)Intra ocular solution
c)Opthalmic solution
2)Based on physical form:
a)Aqueous solutions
b)Suspension
c)Ointments
d)Gels
e)Eye lotions
f)Solid inserts
TYPES OF OCULAR DRUG DELIVERY
A)Non-erodible:
1)Ocusert
2)Contact lenses
3)Diffusional inserts
B)Erodible
1)Lacrisert
2)Soluble ocular drug inserts(sodi)
3)Minidisc
4)Nanoparticles
5)Liposomes
Role Of Polymer In ODDS
 Solution Viscosity , Solution Drainage. Polymer
Mucoadhesive Vehicle: Retained in the eye due to non-
covalent bonding between with conjuctival mucine. Mucine
is capable of picking of 40-80 times of weight of water
Polymeric Solution: The addition of polymers like
methylcellulose, polyvinyl alcohol, hydroxypropyl cellulose
and polyvinyl pyrrolidone to the eye drop solution increases
the corneal penetrations of drug.
• This is presumably due to on increases tear viscosity, which
decreases the other wise rapid initial drainage rate, increases
the corneal contact time and thus sustains to some extant the
initial tear concentration of the drug.
Manufacturing Environment:
General safety considerations
a) Sterility:
b) Ocular toxicity and irritation
Preservatives and preservation
LIMITATIONS OF CONVENTIONAL
DRUG DELIVERY
Rapid precorneal elimination
Solution drainage by gravity
Frequent instillation is necessary
Conjuctival absorption
ADVANTAGES OFAVANCED
DUG DELIVERY
Sustained and/or controlled drug release
Site-specific targeting
Protect the drug from chemical or
enzymatic hydrolysis
Increasing contact time and thus
improving bioavailability
Better patient compliance.
16
Advances in Ophthalmic Drug
Delivery Systems
IN-SITU GELS -A NOVEL APPROACH FOR OCULAR DRUG
DELIVERY
• Polymeric gels for improved drug
delivery.-HYDRO GEL
• Ophthalmic inserts :are defined as sterile
solid or semisolid preparations, with a thin, flexible and
multilayered structure, for insertion in the conjunctival sac.
Ocular iontophoresis:
Iontophoresis is the process in which direct current
drives ions into cells or tissues .
Evaluation of ocular drug delivery
systems
Ocular drug delivery systems are evaluated by
various methods. The ocular in-vitro studies include
design of specialised apparatus.
The ocular in-vivo studies were done in rabbits and
include tear pH measurements, pharmacodynamic
studies and scintigraphy to assess precorneal
residence of formulations.
In-vitro evaluation methods :
A number of approaches are used by different
workers to conduct in-vitro evaluation of controlled
ocular drug delivery systems.
(a) Bottle method
(b) Diffusion method
(c) Modified rotating basket method
(d) Modified rotating paddle apparatus
(e) Flow through devices
(2) In – vivo evaluation methods
 The controlled ocular drug delivery systems can be
evaluated for its pharmacokinetic and pharmacodynamic
profiles.
 The main objective of the pharmacokinetic studies is to
determine the drug release from the dosage form to the eye.
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 .
• Equipments:The blow /fill/seal method:
Marketed products
Glucotim LA of Centaur Pharma is an original research
formulation of Timolol .Used to treat Glaucoma.
Combigan contains brimonidine. Combigan is used to
treat glaucoma or ocular hypertension
Conclusion
In the past 2 decades, a considerable amount of
research has been carried out on the development
of ocular drug delivery systems.
 It is appreciated that the topical route is preferred
for delivery of drugs to the eye.
 The primary objective of all the ocular drug
delivery systems developed till date is to increase
ocular drug residence time which leads to
improvement in ocular drug bioavailability,
diminish side effects due to systemic absorption
and diminishing the necessary amount of drug for
a therapeutic response in the eye.
References
1.Hill J M, O' Callaghan R J, Hobden J A, Kaufman H E. Corneal
Collagen shields for ocular delivery. In :Mitra A K, eds. Ophthalmic
drug delivery systems, New York: Marcel Dekker Inc., 1993; 261 – 273.
2.Hughes P M, Mitra A K. Overview of ocular drug delivery and
iatrogenic ocular cytopathologies. In : Mitra A K, eds. Ophthalmic drug
delivery systems, New York: Marcel Dekker Inc., 1993; 1-28.
3.Van Ootegham M. M M. Fomulation of ophthalmic solutions and
suspensions. In : Edman P, eds. Biopharmaceutics of ocular drug
delivery, Boca Raton : CRC press, 1993; 27-42.
4.Mueller W H, Deardroff D L. Ophthalmic vehicles: The effect of
methyl cellulose on the penetration of Homatropine hydrobromide
through the cornea. J. Am. Pharm. Assoc. 1956; 45: 334.
5.Krishna N, Brown F. Polyvinyl alcohol as an ophthalmic vehicle. Am.
J. Ophthalmol. 1964; 57: 99.
6.Swanson AA, Jeter D J, Tucker P. Ophthalmic vehicles II.
Comparison of ointment and polyvinyl alcohol 1.4% . Ophthalmologica.
1970; 160: 265 - 270.
QUERIES…..
“Sight is the sense which is more
valuable than all the rest.” So Take
care of Eyes!!!

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Optalmic dds final ppt ,g1.

  • 1. Novel approach of OPTHALMIC DRUG DELIVERy SYSTEMS Under the Esteemed Guidance of Dr.B.Vasudha Department of Pharmaceutics Presented By P.Jeevan Reddy Roll no:12H61S0320 Pharmaceutics(Shift-1)
  • 2. CONTENTS INTRODUCTION ANATOMY OF EYE BARRIERS FOR OCULAR DDS CLASSIFICATION TYPES OF OCULAR DDS GENERAL SAFETY CONCERNS ADVANCES IN OCULAR DDS EVALUATION METHODS CONCLUSION REFERENCES
  • 3. INTRODUCTION  Traditionally used eye drop formulations lacked good bioavailability and had low patient compliance, hence most investigations in this field emphasize on the duration of action and enhancement of corneal absorption  Recent developments in ophthalmic drug delivery systems include use of gelling polymers, prodrugs, microspheres, nanoparticles, liposomes and hydrophilic ocular inserts. Protein and peptide delivery, posterior drug delivery and non-aqueous vehicles are new areas of interest in ophthalmic drug delivery.
  • 4. • The Ophthalmic Drug Delivery Systems (ODDS) are desired to improve efficacy, minimization of toxicity, sustained effect or modified drug release. • Cyclodextrin cyclic oligosaccharides are the newer carriers in ODDS which have proved to be useful for controlled release by forming a complex which is known to show rapid and quantitative drug release.
  • 5. RELEVANT ANATOMY AND PHYSIOLOGY OF THE EYE • HUMAN EYE : The accessory structures of the eye are the eyelids, eyelashes, eyebrows, the lachrymal apparatus and extrinsic eye muscles. The diameter of eye is 23mm.
  • 6. General Pathway For Ocular Absorption
  • 7. BARRIERS FOR OCULAR DELIVERY  Drug loss from the ocular surface after instillation, the flow of lacrimal fluid removes instilled compounds from the surface of the eye.  Even though the lacrimal turnover rate is only about 1 μl/min the excess volume of the instilled fluid is flown to the nasolacrimal duct rapidly in a couple of minutes.  Another source of non-productive drug removal is its systemic absorption instead of ocular absorption.  Systemic absorption may take place either directly from the conjunctival sac via local blood capillaries or after the solution flow to the nasal cavity.
  • 8.
  • 9. Approaches to improve ocular bioavailability 1) Viscosity enhancers 8) Eye ointments 2) Gel 9) Prodrug 3) Penetration enhancers 10) Liposomes 4) Niosomes 11) Nanosuspension 5) Microemulsion 6) Nanoparticles/nanospheres 7) In situ-forming gel
  • 10.  Classification Of Ophthalmic Dosage Form: 1)Based on route of administration: a)Topical solution b)Intra ocular solution c)Opthalmic solution 2)Based on physical form: a)Aqueous solutions b)Suspension c)Ointments d)Gels e)Eye lotions f)Solid inserts
  • 11. TYPES OF OCULAR DRUG DELIVERY A)Non-erodible: 1)Ocusert 2)Contact lenses 3)Diffusional inserts B)Erodible 1)Lacrisert 2)Soluble ocular drug inserts(sodi) 3)Minidisc 4)Nanoparticles 5)Liposomes
  • 12. Role Of Polymer In ODDS  Solution Viscosity , Solution Drainage. Polymer Mucoadhesive Vehicle: Retained in the eye due to non- covalent bonding between with conjuctival mucine. Mucine is capable of picking of 40-80 times of weight of water Polymeric Solution: The addition of polymers like methylcellulose, polyvinyl alcohol, hydroxypropyl cellulose and polyvinyl pyrrolidone to the eye drop solution increases the corneal penetrations of drug. • This is presumably due to on increases tear viscosity, which decreases the other wise rapid initial drainage rate, increases the corneal contact time and thus sustains to some extant the initial tear concentration of the drug.
  • 14. General safety considerations a) Sterility: b) Ocular toxicity and irritation
  • 16. LIMITATIONS OF CONVENTIONAL DRUG DELIVERY Rapid precorneal elimination Solution drainage by gravity Frequent instillation is necessary Conjuctival absorption ADVANTAGES OFAVANCED DUG DELIVERY Sustained and/or controlled drug release Site-specific targeting Protect the drug from chemical or enzymatic hydrolysis Increasing contact time and thus improving bioavailability Better patient compliance. 16
  • 17. Advances in Ophthalmic Drug Delivery Systems IN-SITU GELS -A NOVEL APPROACH FOR OCULAR DRUG DELIVERY
  • 18. • Polymeric gels for improved drug delivery.-HYDRO GEL
  • 19. • Ophthalmic inserts :are defined as sterile solid or semisolid preparations, with a thin, flexible and multilayered structure, for insertion in the conjunctival sac.
  • 20. Ocular iontophoresis: Iontophoresis is the process in which direct current drives ions into cells or tissues .
  • 21.
  • 22. Evaluation of ocular drug delivery systems Ocular drug delivery systems are evaluated by various methods. The ocular in-vitro studies include design of specialised apparatus. The ocular in-vivo studies were done in rabbits and include tear pH measurements, pharmacodynamic studies and scintigraphy to assess precorneal residence of formulations. In-vitro evaluation methods : A number of approaches are used by different workers to conduct in-vitro evaluation of controlled ocular drug delivery systems.
  • 23. (a) Bottle method (b) Diffusion method (c) Modified rotating basket method (d) Modified rotating paddle apparatus (e) Flow through devices (2) In – vivo evaluation methods  The controlled ocular drug delivery systems can be evaluated for its pharmacokinetic and pharmacodynamic profiles.  The main objective of the pharmacokinetic studies is to determine the drug release from the dosage form to the eye. 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 .
  • 24. • Equipments:The blow /fill/seal method:
  • 25. Marketed products Glucotim LA of Centaur Pharma is an original research formulation of Timolol .Used to treat Glaucoma. Combigan contains brimonidine. Combigan is used to treat glaucoma or ocular hypertension
  • 26. Conclusion In the past 2 decades, a considerable amount of research has been carried out on the development of ocular drug delivery systems.  It is appreciated that the topical route is preferred for delivery of drugs to the eye.  The primary objective of all the ocular drug delivery systems developed till date is to increase ocular drug residence time which leads to improvement in ocular drug bioavailability, diminish side effects due to systemic absorption and diminishing the necessary amount of drug for a therapeutic response in the eye.
  • 27. References 1.Hill J M, O' Callaghan R J, Hobden J A, Kaufman H E. Corneal Collagen shields for ocular delivery. In :Mitra A K, eds. Ophthalmic drug delivery systems, New York: Marcel Dekker Inc., 1993; 261 – 273. 2.Hughes P M, Mitra A K. Overview of ocular drug delivery and iatrogenic ocular cytopathologies. In : Mitra A K, eds. Ophthalmic drug delivery systems, New York: Marcel Dekker Inc., 1993; 1-28. 3.Van Ootegham M. M M. Fomulation of ophthalmic solutions and suspensions. In : Edman P, eds. Biopharmaceutics of ocular drug delivery, Boca Raton : CRC press, 1993; 27-42. 4.Mueller W H, Deardroff D L. Ophthalmic vehicles: The effect of methyl cellulose on the penetration of Homatropine hydrobromide through the cornea. J. Am. Pharm. Assoc. 1956; 45: 334. 5.Krishna N, Brown F. Polyvinyl alcohol as an ophthalmic vehicle. Am. J. Ophthalmol. 1964; 57: 99. 6.Swanson AA, Jeter D J, Tucker P. Ophthalmic vehicles II. Comparison of ointment and polyvinyl alcohol 1.4% . Ophthalmologica. 1970; 160: 265 - 270.
  • 29. “Sight is the sense which is more valuable than all the rest.” So Take care of Eyes!!!