ocdds vaibhav katare
TRANSCRIPT
A Seminar on
OCULAR DRUG
DELIVERY SYSTEM
VAIBHAV KATARE
1st Year M.Pharm
(Pharmaceutics)
1
PRESENTED BY:
GUIDED BY:
Dr.G.S ASANE(Dept. of pharmaceutics)
• Introduction
• Anatomy And Physiology Of Eye
• Mechanism Of Ocular Absorption
• Ophthalmic Dosage Form Introduction And
Classification
• Advanced Ocular Drug Delivery System
• Marketed Ocular Drug Delivery Products
• Evaluation Of OCDDS
• Conclusion And Future Outlook
• References2 2
INTRODUCTION
• Designed to treat ophthalmic diseases.
• Meant for local therapy and not for systemic action.
• Eye - easily accessible site for topical administration.
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IDEAL CHARACTERISTICS OF OCDDS
Sterility
Isotonicity:
e.g.: 1.9% boric acid, 0.9% NaCl
Buffer/pH adjustment
Less drainage tendency
Minimum protein binding
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COMPOSITION OF EYE
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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ANATOMY AND PHYSIOLOGY OF EYE
The Sclera
The Cornea
The Choroid
The Iris
The Lens
The Retina
The Conjunctiva
Vitreous Humor
Aqueous Humor
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ROUTES OF OCULAR DELIVERY
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D R U G I N T E A R F L U I D
Ocular Absorption
(5% of the dose) Systemic Absorption
(50-100% of the dose)
Major Routes:
-Conjuctiva of eye
-Nose
Minor Routes:
-Lacrimal Drainage
-Pharynx
-Aqueous Humor
-Inner Ocular Tissues
Corneal
Route:
-Primary Route.
-Small Lipophilic
Drugs.
Conjunctival
and Sclera
Route:
-Secondary Route.
-Large Hydrophilic
Drugs.
Aqueous
Humor
Ocular Tissue Elimination
MECHANISM OF OCCULAR DRUG ABSORPTION
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OPHTHALMIC DOSAGE FORM
Ophthalmic preparations are sterile products (free
from foreign particles.) that are intended to be applied
topically to cornea or instilled in the space between the
eyeball and lower eyelid (cul-de-sac cavity).
The following dosage forms have been developed to
ophthalmic drugs.
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OCULAR DELIVERY SYSTEMS
CONVENTIONAL VESICULAR
CONTROL RELEASE PARTICULATE
SOLUTION
SUSPENTION
EMULSION
OINTMENT
INSERT
GELS
IMPLANTS
IONTOPHORESIS
DENDRIMER
MICROEMULSION
NANOSUSPENSION
MICRONEEDLE
MUCOADHESIVE
POLYMERS
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MICROPARTICLES
NANOPARTICLES
LIPOSOMES
NIOSOMES
DISCOMES
CLASSIFICATION OF OCDDS
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SELECTED TYPES OF OCDDS:
1. Aqueous eye drops
2. Oily eye drops
3. Eye ointments
4. Eye lotions
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5. Paper strips
6. Ocuserts
and Laciserts
7. Hydro gel contact
lenses
8. Collagen shields
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1) CONVENTIONAL DELIVERY SYSTEMS:
Eye Drops:
Widely administered drugs as liquid dosage form
Only 5 % of the dose is absorbed
Mostly absorbed through systemic circulation.
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Ointment and Gels:
Prolongation of drug contact time.
blurring of vision & matting of eyelids
can limit its use.
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Ocuserts and Lacrisert:
Sterile Preparation
Controlled Release Dosage Form
Treatment Of Dry Eye Syndrome And Keratitis Sicca.
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2) VESICULAR SYSTEM:
Liposomes:
Liposomes are biocompatible and biodegradable lipid vesicles
made up of natural lipids.
They include the drugs with low partition coefficient, poor
solubility. 16 16
Niosomes and Discomes
They are non toxic and do not require special handling
techniques:
• Niosomes are nonionic surfactant vesicles that have
potential applications in the delivery of hydrophobic or
amphiphilic drugs.
• Discomes act as potential drug delivery carriers as they
released drug in a sustained manner at the ocular site.17
3) CONTROL DELIVERY SYSTEMS:
1. Implants
2. Iontophoresis
3. Dendrimer
4. Microemulsion
5. Nanosuspensions
6. Microneedle
7. Mucoadhesive Polymers18 18
4) PARTICULATE SYSTEM :(NANOPARTICLES AND MICROPARTICLES) The maximum permissible size limit for
microparticles is about 5-10 mm for ophthalmic
administration.
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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1. Scleral Plugs Therapy.
2. Gene Therapy.
3. Stem Cell Therapy.
4. Cell Encapsulation.
5. siRNA therapy.
6. Oligonucliotide therapy.
7. Aptamer.
8. Ribozyme therapy.
ADVANCED DRUG DELIVERY SYSTEM (4)
New Ophthalmic Drug Delivery System (NODDS) (7)
Delivers precise amount of drug to the eye.
Device consists of medicated film attached to paper
cover and handled by a short and thin membrane.
All components are packed individually and sterilized by
gamma irradiation.
Membrane dissolves in lacrimal fluid and delivers the drug.
Conclusion: NODS produced 8-fold increase in
bioavailability for pilocarpine with respect to standard eye
drop formulation.21
MARKETED PRODUCTS(3)
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Brand Name Drug Dosage Form Use
DICHOL Carbachol Sterile solution and
prefilled syrings
Used in ophthalmic
surgery
REFRESH
TEARS®
Hydroxypropyl-
methylcelluose
Drops Eye lubricants and
dryness of eye
GELTEAR/
VISCOTEAR
Corbomer Bioadhesive gel Treatment of
soreness, burning
Timolol® XE Timolol maleate In-situ gel Keratoconjuctivitis
PRED
FORTE®
prednisolone
acetate
suspensions Antiallergic and
anti-inflammatory
ACIVIR EYE Acyclovir Ointment Anti-infective
REFRESH®
Classic
Artificial tear fluid convenient single
use vials
Moisturizes and
relieves dry eyes
RESTASIS® Cyclosporine emulsion Chronic dry eye
diseases
EVALUATION OF OCDDS (3)
1. Thickness of film
2. Content uniformity
3. Uniformity of Weight
4. Percentage moisture absorption
5. Percentage moisture loss
6. In-vitro drug release
7. In-vivo drug release
8. Accelerated stability studies.
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CONCLUSION & FUTURE OUTLOOK (8)
Ocular drug delivery systems provide local as well as
systemic delivery of the drugs.
The novel advanced delivery systems offer more protective
and effective means of drug delivery.
The latest available targeted drug delivery systems focus
on the localised delivery of the drugs as well as certain
macromolecular substances like proteins, genes like DNA,
siRNA to the internal parts of the eye.
Further developments are preferable which will eliminate
the disadvantages of these available advanced delivery
systems and will make readily acceptable among the
patients.24
References
1. N.K.Jain, “Advances in Controlled & Novel Drug Delivery”,
CBS Publication, & distributor, New Delhi, pg No. 219-223,
110-120.
2. N. K. Sahane, “Ocular Inserts: A Review” , Drug Invention
Today 2010, 2(1), 57-64.
3. Jitendra, Sharma P.K. Banik A. and Dixit S., “A New Trend:
Ocular Drug Delivery System”, An International Journal Of
Pharmaceutical Sciences, July-2011,Vol-2,Issue-3,ISSN:
0976-7908.
4. Patel Vishal, Agrawal Y K, “Current Status And Advanced
Approaches In Ocular Drug Delivery System”, Journal of
Global Trends in Pharmaceutical Sciences, ISSN: 2230-7346,
Vol.2, Issue 2, April-June 2011, pp -131-148.25 25
5. A.Rajasekaran, K.S.G.Arul Kumaran, J.Padma Preetha And
K.Karthika, “A Comparative Review On Conventional And
6. Advanced Ocular Drug Delivery Formulations”, International
Journal Of Pharmtech Research, ISSN : 0974-4304, Vol.2,
No.1, pp 668-674, Jan-Mar 2010
7. S.L Harikumar, Arora Sonia “Nanotechnological approaches
in Ophthalmic delivery systems”, Int. J. Drug Dev. & Res.,
Oct-Dec 2011, 3(4): 9-19.
8. Venkata Ratnam G, Madhavi S, Rajesh P, “ Ocular Drug
Delivery: An Update Review”, International Journal of
Pharmacy and Biological Sciences (eISSN: 2230-7605),
Volume 1| Issue 4 |OCT-DEC |2011|437-446.
9. www.mims-india.com/date of citation on
03/12/2012/time/12.38pm
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