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___________________________________________Review Paper
Uttarakhand
ABSTRACT
There are many eye ailments which affected to eye and one can loss the eye sight also. Therefore many
ophthalmic drug delivery systems are available. These are classified as conventional and non-conventional
drug delivery systems. Most commonly available ophthalmic preparations are eye drops and ointments about
70% of the eye dosage formulations in market. But these preparations when instilled into the cul-de-sac are
rapidly drained away from the ocular cavity due to tear flow and lachrymal nasal drainage. Only a small
amount is available for its therapeutic effect resulting in frequent dosing. So overcome to these problems
newer pharmaceutical ophthalmic formulation such as in-situ gel, nanoparticle, liposome, nanosuspension,
microemulsion, intophoresis and ocular inserts have been developed in last three decades increase the
bioavailability of the drug as a sustained and controlled manner. Major improvements are required in each of
the technologies discussed in this review. Some approaches are relatively easy to manufacture, but are limited
in their ability to provide sustained drug release.
KEY WORDS: ocular, drug delivery, ocuserts, ophthalmic.
INTRODUCTION
Eye is a unique and very valuable organ. This is
considered a window hinge. We can enjoy it and
look at the world body. There are many eye
diseases that can affect the body and loss of vision
as well. Therefore, many eyes in drug delivery
systems are available. They are classified as
traditional and new drug development system.
Topical application of drugs to the eye is the most
popular and well-accepted route of administration
for the treatment of various eye disorders. The
bioavailability of ophthalmic drugs is, however,
very poor due to efficient protective mechanisms of
the eye. Blinking, baseline and reflex lachrymation,
and drainage remove rapidly foreign substances,
including drugs, from the surface of the eye [1].
There are many eye ailments which affected to eye
and one can loss the eye sight also. Therefore many
ophthalmic drug delivery systems are available.
These are classified as conventional and nonconventional (newer) drug delivery systems. Most
commonly available ophthalmic preparations are
eye drops and ointments about 70% of the eye
dosage formulations in market. But these
preparations when instilled into the culde-sac are
rapidly drained away from the ocular cavity due to
tear flow and lachrymal nasal drainage. Only a
small amount is available for its therapeutic effect
________________________________________
*Address for correspondence:
E-mail: prianshu_tangri@yahoo.co.in
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OCULAR PHARMACOKINETICS[16-18]
The drug pharmacokinetics from the eye follows
the following paths
Transcorneal permeation from the lacrimal
fluid into the anterior chamber.
Non-corneal drug permeation across the
conjunctiva and sclera into the anterior
uvea.
Drug distribution from the blood stream
via blood-aqueous barrier into the anterior
chamber.
Elimination of drug from the anterior
chamber by the aqueous humor turnover
to the trabecular meshwork and sclemm's
canal.
Drug elimination from the aqueous humor
into the systemic circulation across the
blood-aqueous barrier.
Drug distribution from the blood into the
posterior eye across the blood-retina
barrier.
Intravitreal drug administration.
Drug elimination from the vitreous via
posterior route across the blood-retina
barrier.
Drug elimination from the vitreous via
anterior route to the posterior chamber.
BARRIERS TO OCULAR DRUG 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 l/min the excess volume of the
instilled fluid is flown to the nasolacrimal duct
rapidly in a couple of minutes [18]. 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 [19,20].
Anyway, most of small molecular weight drug dose
is absorbed into systemic circulation rapidly in few
minutes. This contrasts the low ocular
bioavailability of less than 5% [18]. Drug
absorption into the systemic circulation decreases
the drug concentration in lacrimal fluid extensively.
Therefore, constant drug release from solid
delivery system to the tear fluid may lead only to
ocular bioavailability of about 10%, since most of
the drug is cleared by the local systemic absorption
anyway [21].
Lacrimal fluid-eye barriers:
Corneal epithelium limits drug absorption from the
lacrimal fluid into the eye [22]. The corneal barrier
is formed upon maturation of the epithelial cells.
They migrate from the limbal region towards the
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Sprays:
Although 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
cycloplegics examination.
Contact lenses:
Contact lenses can absorb water-soluble drugs
when soaked in drug solutions. These drugsaturated contact lenses are placed in the eye for
releasing the drug for a long period of time. The
hydrophilic contact lenses can be used to prolong
the ocular residence time of the drugs. In humans,
the Bionite lens which was made from hydrophilic
polymer (2-hydroxy ethyl methacrylate) has been
shown to produce a greater penetration of
fluorescein. [72]
Artificial tear inserts:
A rod shaped pellet of hydroxy propyl cellulose
without preservative is commercially available
(Lacrisert). This device is designed as a sustained
release artificial tear for the treatment of dry eye
disorders. It was developed by Merck, Sharp and
Dohme in 1981. [73]
Filter paper strips:
Sodium fluorescein and rose Bengal dyes are
commercially available as drug-impregnated filter
paper strips. These dyes are used diagnostically to
disclose corneal injuries and infections such as
herpes simplex and dry eye disorders.
Microemulsion:
Due to their intrinsic properties and specific
structures, microemulsions are a promising dosage
form for the natural defense of the eye. Indeed,
because they are prepared by inexpensive processes
through auto emulsification or supply of energy
and can be easily sterilized, they are stable and
have a high capacity of dissolving the drugs. The in
vivo results and preliminary studies on healthy
volunteers have shown a delayed effect and an
increase in the bioavailability of the drug. The
proposed mechanism is based on the adsorption of
the nanodroplets representing the internal phase of
the microemulsions, which constitutes a reservoir
of the drug on the cornea and should then limit
their drainage. [74-76]
Ocular inserts:
Ocular inserts are solid dosage forms and can
overcome the disadvantage reported with
traditional ophthalmic systems like aqueous
solutions, suspensions and ointments. The ocular
inserts maintain an effective drug concentration in
the target tissues. Limited popularity of ocular
inserts has been attributed to psychological factors,
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Description
Soluble ocular
drug Insert
Small oval wafer, composed of soluble copolymers consisting of actylamide, N-venyl pyrrolidone and ethyl acetate,
soften on insertion
New
ophthalmic
drug delivery
system
Medicated solid polyvinyl alcohol flag that is attached to a paper- covered with handle. On application, the flag
detaches and gradually dissolves, releasing the drugs
Collagen
shields
Ocusert
Flat, flexible elliptical insoluble device consisting of two layers, enclosing a areservior, use commercially to deliver
Pilocarpine for 7 days
Minidisc
or
ocular
therapeutic
Lacrisert
Bioadhesive
ophthalmic
eye insets
Adhesive rods based on a mixture of Hydroxy propyl cellulose, ethyl cellulose, Poly acrylic acid cellulosephthalate
Dry drops
A preservative free of hydrophilic polymer solution that is freeze dried on the tip of a soft hydrophobic carrier strip,
immediately hydrate in tear strip
Gelfoam
Slabs of Gelfoam impregnated with a mixture of drug and cetyl ester wax in chloroform
Rose-shape device made from Hydroxy propyl cellulose use for the eye syndrome as an alternative to tears
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