July 2013, Vol-4, Issue -3

Review Article ISSN NO:0976-6723

REVIEW ON OPHTHALMIC INSERTS

Geeta Rajput*, Shaweta Sharma, Shalini Chaudhury, Banshraj
T.M.U College of Pharmacy, Moradabad- U.P, India
Abstract
The purpose of this review is to provide an update on the current knowledge within this field of
ocular drug delivery. Ocular route of drug delivery is one of the most interesting and challenging
endeavors facing the pharmaceutical scientist. One of the major barriers of ocular medication is to
obtain and maintain a therapeutic level at the site of action for prolonged period of time. Therefore
many ophthalmic drug delivery systems are available. These are classified as conventional and non-
conventional drug delivery systems. The main purpose of preparing ocular insert is to increase ocular
bioavailability of drug. Ocular inserts maintain the drug concentration within a desired range. Fewer
administrations are required so they increase patient compliance. In the present update, the
advantages, disadvantages and requirement for success of ocular inserts, and examine the few inserts
which are available on the market or are being developed by pharmaceutical companies for drug
delivery. In this review, we have focused on the present area of ocuserts helps in treating eye
diseases.

Keywords: Ocuserts, ocular drug delivery system, eye diseases

INTRODUCTION required for the instillation to achieve an

Ocular drug delivery is one of the most adequate level of therapeutic effect. Polymeric
challenging and interesting tasks for the film ocular drug delivery systems/ocular inserts,
Pharmaceutical researchers. One of the major which are gaining worldwide accolade, release
barriers of ocular medication is to maintain and drugs at a pre-programmed rate for a longer
obtain a therapeutic level at the site of action for period by increasing the pre-corneal residence
desired period of time. The anatomy, time with increase. [2, 3]
biochemistry and physiology of the eye render The advantage of ocular inserts, which are solid
this organ exquisitely impervious to foreign devices placed in the cul-de-sac of the eye in
substances [1]. comparison with liquid formulations are
The eye as a portal for drug delivery is generally numerous. Because of the prolonged retention of
used for local therapy against systemic therapy to the devices and a controlled release, the effective
avoid the risk of eye damage due to high blood drug concentration in the eye can be ensured
concentrations of the drug, which is not intended. over an extended time period. Dosing of the drug
The ocular organ impervious to foreign is also more accurate and the risk of systemic
substances due to unique anatomy, physiology side effects is decreased. Furthermore, solid
and biochemistry of the eye, thus presenting a devices have an increased shelf life and the
constant challenge to the pharmaceutical presence of additives such as preservatives is not
formulator to circumvent the protective barriers required. Ocular delivery systems like inserts,
of the eye without causing permanent tissue biodegradable polymeric systems, and collagen
damage. Therefore, the target tissue absorbs a shields are being developed in order to attain
very less fraction of drug. Due to this reason, better ocular bioavailability and sustained action
concentrated solutions and frequent dosing are of ocular drugs.

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A basic concept in ophthalmic review and posterior route across the blood-retina barrier.
development is that the therapeutic efficacy of an • Drug elimination from the vitreous via anterior
ophthalmic drug can be greatly improved by route to the posterior chamber. [5]
prolonging its contact with the corneal surface. MECHANISM OF OCULAR DRUG
Ophthalmic inserts offer many advantages over ABSORPTION [6, 7]
conventional dosages forms, like increased Topical delivery into the cul-de-sac is, by far, the
ocular residence, possibility of releasing drug at most common route of ocular drug delivery.
a slow and constant rate, accurate dosing, and Absorption from this site may,
exclusion of preservatives and increased shelf 1. Corneal
life. Design, construction and technology of 2. Non-corneal
ocular insert in a controlled and sustained ocular CLASSIFICATION OF OPHTHALMIC
delivery device are gaining rapid improvement to INSERTS
overcome this constraint. [4] Ophthalmic inserts are aimed at remaining for a
ADVANTAGES OF OCULAR DRUG long period of time in front of the eye. These
DELIVERY SYSTEMS solid devices are intended to be placed in the
1. Accurate dosing is possible. To overcome the conjunctival sac and to deliver the drug at a
side effects of pulsed dosing produced by comparatively slow rate. Ophthalmic inserts are
conventional systems. defined as sterile preparations, with a thin,
2. To provide sustained and controlled drug multilayered, drug-impregnated, solid or
delivery. semisolid consistency devices placed into cul-de-
3. To increase the ocular bioavailability of drug sac or conjuctival sac and whose size and shape
by increasing the corneal contact time. This can are especially designed for ophthalmic
be achieved by effective adherence to corneal application. They are composed of a polymeric
surface. support containing or not drug (s), the latter
4. To provide targeting within the ocular globe being incorporated as dispersion or a solution in
so as to prevent the loss to other ocular tissues. the polymeric support. The inserts can be used
5. To circumvent the protective barriers like for topical or therapy.
drainage, lacrimation and conjunctival The advantages of these systems are:
absorption. 1. Ocular contact time is increased.
6. To provide comfort, better compliance to the 2. Accurate dosing is possible. Constant and
patient and to improve therapeutic performance predictable rate of drug release can be achieved.
of drug. 3. Systemic absorption can be reduced and side
7. To provide better housing of delivery system. effects can be reduced.
OCULAR PHARMACOKINETICS 4. Increased shelf life can be achieved
The drug pharmacokinetics from the eye follows 5. Better patient compliance.
the following paths 6. Targeting to internal ocular tissues can be
• Transcorneal permeation from the lacrimal done. [8]
fluid into the anterior chamber. CLASSIFICATION OF OPHTHALMIC
• Non-corneal drug permeation across the INSERTS
conjunctiva and sclera into the anterior uvea. 1. Non-erodible ocular insert: The Non-
• Drug distribution from the blood stream via erodible ocular inserts include Ocusert, and
blood-aqueous barrier into the anterior chamber. Contact lens.
• Elimination of drug from the anterior chamber Ocusert was one of the earlier ocular inserts in
by the aqueous humor turnover to the trabecular use. The technology used in this is an insoluble
meshwork and sclemm's canal. delicate sandwich technology. In ocusert the drug
• Drug elimination from the aqueous humor into reservoir is a thin disc of pilocarpine-alginate
the systemic circulation across the blood- complex sandwiched between two transparent
aqueous barrier. discs of micro porous membrane fabricated from
• Drug distribution from the blood into the ethylene-vinyl acetate copolymer. The micro
posterior eye across the blood-retina barrier. porous membranes permit the tear fluid to
• Intra vitreal drug administration. penetrate into the drug reservoir compartment to
• Drug elimination from the vitreous via E.g. dissolve drug from the complex.

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Alza-ocusert: In this Pilocarpine molecules are solutions and delivers the drug for about
then released at a constant rate of 20 or 40 μg/h 24hours. [10]
for 4 to 7 days. Used in the management of c. Minidisc: The minidisc consists of a
glaucoma The use of pre-soaked hydrophilic contoured disc with a convex front and concave
contact lenses was used for ophthalmic drug back surface in the contact with the eyeball. It is
delivery. Therapeutic soft lenses are used to aid like a miniature contact lens with a diameter of
corneal wound healing in patients with infection, 4-5mm. The minidisc is made up of silicone
corneal ulcers, which is characterized by marked based prepolymer-α-ψ-bis (4-methacryloxy)
thinning of the cornea. butyl polydimethyl siloxane. Minidisc can be
An alternative approach to pre-soaked soft contact hydrophilic or hydrophobic to permit extend
lenses in drug solutions is to incorporate the drug release of both water soluble and insoluble drugs.
either as a solution or suspension of solid particles in [11]
the monomer mix. The polymerization is then carried Classification of Patented Ocular Inserts
out to fabricate the contact lenses. This technique is
(Based upon their solubility behavior)
promising longer release up to 180 h as compared to
pre-soaked contact lenses.
Disadvantages of these non-erodible ocular 1) Insoluble inserts
inserts are 2) Soluble inserts
1.Complexity and difficulty of usage is noticed 3) Bio-erodible inserts
particularly in self administration.
2.Tolerability in the eye is poor, due to rigidity, Insoluble ophthalmic inserts
size or shape. The insoluble inserts have been classified into
3.Foreign body sensation and they are to be three groups:-
removed at the end of the dosing period. [9] i. Diffusion systems
ii .Osmotic systems
2. Erodible ophthalmic insert: The marketed iii. Hydrophilic contact lenses.
devices of erodible drug inserts are Laciserts, The first two classes include a reservoir in
SODI, and Minidisc. contact with the inner surface of the rate
controller and supplying drug thereto. The
a. Lacisert: It is a sterile rod shaped device reservoir contains a liquid, a gel, a colloid, a
made up of hydroxyl propyl cellulose without semisolid, a solid matrix or a carrier-containing
any preservative is used for the treatment of dry drug homogeneously or heterogeneously
eye syndromes. It weighs 5 mg and measures dispersed or dissolved therein. Carriers can be
12.7 mm in diameter with a length of 3.5 mm. made of hydrophobic, hydrophilic, organic,
Lacisert is useful in the treatment of keratitis inorganic, naturally occurring or synthetic
whose symptoms are difficult to treat with material.The third class includes the contact
artificial tear alone. It is inserted into the inferior lenses. The insoluble of these devices is their
fornix where it imbibes water from the main disadvantages, since they have to be
conjunctiva and cornea, forms a hydrophilic film removed after use.
which stabilizes the tear film and hydrates and
lubricates the cornea. It dissolves in 24 hours. Diffusion inserts: The diffusion systems are
b. Sodi: Soluble Ocular Drug Insert is a small compared of a central reservoir of drug enclosed
oval wafer developed for cosmonauts who could in specially designed semi permeable or micro
not use eye drops in weightless conditions. It is porous membranes, which allow the drug to
sterile thin film of oval shape made from diffuse the reservoir at a precisely determined
acrylamide, N-vinylpyrrolidone and ethylacrylate rate.
called as ABE. It weighs about 15-16 mg. It is The drug release from such a system is
used in the treatment of glaucoma and trachoma. controlled by the lachrymal fluid permeating
It is inserted into the inferior cul-de-sac and gets through the membrane until a sufficient internal
wets and softens in 10-15 seconds. After 10-15 pressure is reached to drive the drug out of the
min the film turns into a viscous polymer mass, reservoir. The drug delivery rate is controlled by
after 30-60 minutes it turns into polymer diffusion through the membrane, which one can
be controlled. [12]

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Soft contact lenses
These are shaped structure made up of a
covalently crosslinked hydrophilic or
hydrophobic polymer that forms a three-
dimensional network or matrix capable of
retaining water, aqueous solution or solid
components.
When a hydrophilic contact lens is soaked in a
drug solution, it absorbs the drug, but does not
give a delivery as precise as that provided by
other non-soluble ophthalmic systems. The drug
Osmotic inserts [13] release from such a system is generally very
The osmotic inserts are generally compared of a rapid at the beginning and then declines
central part surrounded by a peripheral part. The exponentially with time. The release rate can be
first central part can be composed of a single decreased by incorporating the drug
reservoir or of two distinct compartments. homogeneously during the manufacture or by
In first case, it is composed of a drug with or adding a hydrophobic component. Contact lenses
without an additional osmotic solute dispersed have certainly good prospects as ophthalmic drug
through a polymeric matrix, so that the drug is delivery systems.
surrounded by the polymer as discrete small Soluble Ophthalmic inserts
deposits. In the second case, the drug and the Soluble inserts correspond to the oldest class of
osmotic solutes are placed in two separate ophthalmic inserts. They offer the great
compartments, the drug reservoir being advantage of being entirely soluble so that they
surrounded by an elastic impermeable membrane do not need to be removed from their site of
and the osmotic solute reservoir by a semi application thus, limiting the interventions to
permeable membrane. The second peripheral part insertion only.
of these osmotic inserts comprises in all cases a Types
covering film made of an insoluble semi a) Based on natural polymers e.g. collagen.
permeable polymer. The tear fluid diffuse into b) Based on synthetic or semi synthetic
peripheral deposits through the semi permeable polymers.
polymeric membrane wets them and induces The therapeutic agents is preferably absorbed by
their dissolution. The solubilized deposits soaking the insert in a solution containing the
generate a hydrostatic pressure against the drug, drying and rehydrating in before use on the
polymer matrix causing its rupture under the eye. The amount of drug loaded will depend
form of apertures. Drug is then released through upon the amount of binding agent, upon the
these apertures from the deposits near the surface concentration of the drug solution into which the
of the device which is against the eye, by the sole composite is soaked, as well as the duration of
hydrostatic pressure. This corresponds to the the soaking.
osmotic part characterized by zero order drug The soluble ophthalmic inserts containing
release profile. synthetic/semi synthetic polymers
Offers the additional advantages of being
generally of a simple design.
a) Based on products well adopted for
ophthalmic use.
b) Easily processed by conventional methods –
slow evaporating extrusion, compression or
injection molding.
The release of the drug from such system is by
penetration of tears into the insert which induces
release of the drug by diffusion and forms a gel
layer around the core of the insert, this external
gelification induces the further release, but still

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controlled by diffusion. The release rate, J, is polymers. Successful biodegradable materials for
derived from Fick’s law yields the following ophthalmic use are the poly (orthoesters) and
expression. poly (orthocarbonates). The release of the drug
from such a system is the consequence of the
contact of the device with the tear fluid inducing
a superficial diversion of the matrix.
A- Surface area of the membrane The use of solid ophthalmic devices will
K – Diffusion coefficient of the drug certainly increase owing to the development of
L – Membrane thickness new polymers, the emergence of new drugs
CS – Drug solubility in water having short biological half lives or systemic side
D- Diffusion coefficient of the ocuserts effects and the need to improve the efficacy of
membrane. ophthalmic treatment by ensuring an effective
Since all the terms on the right hand side of the drug concentration in the eye over an extended
[12, 14]
above equation are constant, so is the release rate period of time.
of the device. The other factors affecting drug OCUSERTS USING IN VARIOUS EYE
release from these Ocuserts include: DISEASES:
• Penetration of the inclusion. 1. Glaucoma: Glaucoma refers to a group of eye
• Swelling of the matrix. conditions that lead to damage to the optic nerve.
• Dissolution of the drug and the polymers. This nerve carries visual information from the
The soluble insert made of cellulose derivatives eye to the brain. In most cases, damage to the
can be sterilized by exposure to gamma radiation optic nerve is due to increased pressure in the
without the cellulose components being altered. eye, also known as intraocular pressure (IOP).
A decreased release rate is obtained by using a Medication available but having side effects:
component of the matrix a polymer normally Ophthalmic pilocarpine is used to treat
used for enteric coatings or by introducing a glaucoma, a condition in which increased
suitable amount of hydrophobic polymer capable pressure in the eye can lead to gradual loss of
of diminishing the tear fluid penetration and thus vision. Pilocarpine is in a class of medications
of decreasing the release of the drug without called miotics. It works by allowing excess fluid
modifying the solubility of the insert when added to drain from eye.
in proper proportion. The amount of the drug administered in
pilocarpine eye drops is substantially in excess of
that needed for IOP control. The need to avoid
this problem and the inconvenience of
administering drops are leading to the
development of a variety of alternative methods
for drug delivery to the eye. Pilocarpine needs to
be administer four times a day which do not
provide a constant therapeutic effect of the
medication while leading the side effects of
blurred or fluctuating vision and also not been
tolerated by patients under the age of 40 and
leeds to the fluctuation of intraocular pressure.
Other Side Effects:
1. Prostaglandin Analogs: possible changes in
eye color and eyelid skin, stinging, blurred
vision, eye redness, itching, burning.
Biodegradable ophthalmic inserts 2. Beta Blockers: low blood pressure, reduced
The biodegradable inserts are composed of pulse rate, fatigue, shortness of breath; rarely:
material homogeneous dispersion of a drug reduced libido, depression. 3. Alpha Agonists:
included or not into a hydrophobic coating which burning or stinging, fatigue, headache,
is substantially impermeable to the drug. They drowsiness, dry mouth and nose, relatively
are made of the so-called biodegradable higher likelihood of allergic reaction.

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4. Carbonic Anhydrase Inhibitors: in eye drop a day in the eye. The poor therapeutic response
form: stinging, burning, eye discomfort; in pill exhibited by conventional ophthalmic ointments
form: tingling hands and feet, stomach upset, due to rapid pre corneal elimination of the drug.
memory problems, depression, frequent New advanced ocusert system
urination. Acyclovir ocular inserts: They were prepared
New advanced ocusert system using solvent casting method said promising
Ocular inserts of Timolol maleate: Controlled formulation would be able to offer benefits such
release of timolol maleate ocusert avoids the as increase residence time, prolonged drug
pulse-entry with which side-effects are release, reduction in frequency of administration
associated. These systems can be based on any of and thereby may help to improve the patient
several different mechanisms, and include both compliance.
erodible and nonerodible matrices, wafers. 1. Eye Allergies: Eye allergies often are
Timolol maleate was the first β-blocker to be hereditary, and occur due to processes associated
used as an anti-glaucoma agent and to date with other types of allergic responses. When an
remains as the standard because none of the allergic reaction takes place, your eyes may be
newer beta blockers were found to be more overreacting to a substance perceived as harmful,
effective. Timolol maleate has the longest record even though it may not be. These substances are
of safety and efficacy to lower IOP and is called allergens. For example, dust that is
administered via eye drops one or more times per harmless to most people can cause excessive
day. They lengthen the extent of drug action by production of tears and mucus in eyes of overly
enhancement of corneal absorption. sensitive, allergic individuals.
Pilocarpine ocusert: A matrix-dispersed Medication available but having side effects:
pilocarpine soluble insert avoids some of the The disadvantage with Systane eye drops, use in
problems of administration of pilocarpine by eye allergies, especially with the gel formula, is
drops. It has shown an effective lowering of the that when first applied the eyes, people may
IOP with a duration of at least 24 hours.The experience a blurry vision for about 20 to 30
insert is, in effect, a device for prolonging the seconds. It can also cause a little feeling of
contact time of the dispersed drug with the burning and stinging sensations around the eyes
corneal tear film. It is therefore analogous to the but not to the point that it will cause redness and
use of agents which increase tear film viscosity, further irritations to the eyes. Additionally,
such as methylcellulose and polyvinyl alcohol, although it s a very rare case, at the initial
without the disadvantage inherent in the removal application of the Systane eye drops, some
of a drug- soaked carrier such as the cotton pled- people may experience pain in the eyes, changes
get. Since there is a limit to the effectiveness of in vision orientation and swelling and irritation.
increasing viscosity on drug penetration, the Blurred vision, headache, and increased tear
duration of effect seen with these inserts can be production; swelling of the cornea and iris;
attributed to prolonged release with the slow temporary burning, irritation, pain, redness,
dissolution of the device. stinging, or swelling of the eye are the side
1. Herpes Simplex Eye Disease: The most effects.
common herpes simplex eye disease caused is an New advanced ocusert system: Ketorolac
infection of the cornea, which can potentially tromethamine ocuserts were prepared using
threaten sight. The infection varies in duration, different polymers such as hydroxy propyl
severity and response to treatment, depending in methylcellulose, ethyl cellulose, methylcellulose
part on which of several different strains of HSV and polyvinyl pyrrolidone in different
type I caused the original infection. It can be proportions. [15]
considered a "cold sore" or "fever blister" of the 1. Blepharitis: An infection of lid tructures
eye.Herpes simplex keratitis (HSK) remains a (usually by staphylococcus aureus) with
common cause of unilateral corneal disease. concomitant seborrhoea, rosacea, a dry eye
Medication available but having side effects: and abnormalities in lipid secretions.
Acyclovir, an antiviral is effective against human Medication available but having side effects:
Herpes Simplex viruses, commercially available The poor bioavailability and therapeutic response
as a 3 % w/w eye ointment to be applied 5 times exhibited by Ofloxacin conventional ophthalmic

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solutions due to rapid pre-corneal elimination of may not be affected, depending upon the location
the drug. and extent of the corneal lesion. You may see a
New advanced ocusert system: Ocular inserts vesicular skin rash and follicular conjunctivitis
were prepared with prolonged release of drug with the initial infection, but these are less
and minimum swelling within cul-de-sac common with recurrent HSV. A more common
using Ofloxacin. [16] sign is secondary uveitis.
1. Ocular Hypertension: The term ocular Medication available but having side effects:
hypertension usually refers to any situation in Adverse events associated with the use of
which the pressure inside the eye, called ganciclovir ophthalmic gel may include, but are
intraocular pressure, is higher than normal. Eye not limited to, the following:
pressure is measured in millimeters of mercury 1. Blurred Vision
(mm Hg). Normal eye pressure ranges from 10- 2. Eye Irritation
21 mm Hg. Ocular hypertension is an eye 3. Punctate Keratitis
pressure of greater than 21 mm Hg. 4. Conjunctival Hyperemia
2. Medication available but having side New advanced ocusert system
effects: Idoxuridine ocular insert therapy: use in
treatment of herpes simplex keratitis: Therapy
of acute herpes simplex keratitis in rabbits with
idoxuridine-releasing ocular inserts showed that
an application rate of 30µg/hr gave significantly
better results than conventional treatment with
idoxuridine drops and ointment while exposing
the eye to 40% less drug. Delivery rates lower
than this were equal or not as effective as drop
New advanced ocusert system and ointment therapy and rates up to 100µg/hr
Pilocarpine ocusert system for sustained did not produce significantly better results than
control of ocular hypertension: A number of rates of 30µg/hr. Serial viral cultures
excellent drugs are available that are effective in demonstrated the persistence of virus beyond the
reducing IOP. These drugs are typically applied period of clinical resolution of disease in all
as eye drops. However, patient adherence can be treatment groups, indicating that therapy should
poor, thus reducing the clinical efficacy of the be continued longer than apparent resolution of
drugs. Several novel delivery systems designed disease.
to address the issue of adherence and to ensure 1. Dry Eye Syndrome: Dry eye is a disorder of
consistent reduction of IOP are currently under the tear film due to tear deficiency or excessive
development. A pilocarpine-containing, tear evaporation which causes damage to the
polymermembrane unit (Ocusert) was evaluated interpalpebral ocular surface (i.e. exposed eye
in 29 patients with open-angle glaucoma.Their surface) and is associated with symptoms of
potential is dependent on developing suitable ocular discomfort. This definition of dry eyes
delivery systems that can provide the drugs in a was adopted by the National Eye Institute
sustained, local manner to the retina and optic workshop on dry eyes. The eye becomes dry
nerve. Drug delivery systems have the potential either because there is not enough tears being
to improve patient adherence, reduce side effects, produced or because there is abnormally high
increase efficacy, and ultimately, preserve sight rate of evaporation of tears.
for glaucoma patients. New advanced ocusert system
1. Herpes Simplex Keratitis: Herpes Simplex Hydroxypropyl cellulose ophthalmic inserts
keratitis (HSK) is a viral infection that if left for treatment of dry eye: There are various
untreated can have devastating ocular treatment modalities for dry eye syndrome
consequences25. The keratitis caused by the available to eye care professionals, which can be
herpes simplex virus (HSV) typically presents as used as monotherapy or in combination.
a unilateral "red eye" with a variable degree of There is evidence to suggest that with proper use
pain or ocular irritation. Photophobia and and adequate patient education, hydroxypropyl
epiphora are common; however, vision may or cellulose ophthalmic inserts are an effective and

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safe treatment choice for dry eye syndrome. for the treatment of fungal blepharitis,
Most patients showed significant improvement in conjunctivitis and keratitis. Natamycin when
ocular symptoms and clinical signs, and many formulated as eye drops suffered the
patients continued using hydroxypropyl cellulose disadvantage of instillation of the dye drops for
ophthalmic inserts for several years alone or in every 3-4 h and hence maximized patient non
conjunction with other dry eye therapies. There compliance, leading to ineffective therapy.
was no significant worsening in symptoms or 1. Corneal Ulcers: A corneal ulcer is an erosion
any major long-term side effects of the or open sore on the surface of the cornea. The
medication. The inserts may be particularly cornea is the transparent area at the front part of
helpful in patients who cannot tolerate the eye that serves as a window through which
preservatives or immunosuppressant drops, do we see. It also refracts light and offers protection
not want to instill multiple artificial tears to other parts of the eye. If the cornea becomes
throughout the day, or still have an insufficient inflamed due to infection or injury, an ulcer may
tear film despite other therapies. However, it is develop. A corneal ulcer is a serious condition
worth noting that several of the studies excluded that must be treated promptly to avoid lasting
patients with meibomian gland disease or vision problems.
blepharitis. It remains to be seen if the inserts Medication available but having side effects
help patients with evaporative aqueous tear loss Treatment for corneal ulcers needs to be
due to meibomian gland dysfunction or aggressive, as some ulcers lead to vision loss and
blepharitis. One would think that both of these blindness. Treatment usually involves antibiotics
disease groups would benefit from using the as well as antiviral or antifungal medications.
inserts because there is often overlap of patients Steroid eye drops may also be given to reduce
who also have dry eye syndrome. Nonetheless, inflammation but having side effects like White
hydroxypropyl cellulose ophthalmic inserts can precipitate and ocular discomfort (stinging and
be used effectively as monotherapy, or in burning may occur upon application). For e.g. In
conjunction with other therapies, and should be patients with corneal ulcer or frequent
considered in the treatment of dry eye syndrome. administration of the drug, white precipitates
1. Conjunctivitis: Conjunctivitis is the have been observed, which resolved
inflammation of the conjunctiva (the membrane spontaneously with continued application The
that lines the eyelids and covers the exposed precipitate does not preclude continued use of
surface of the eyeball).Conjunctivitis can be CILOXAN Eye drops or CILOXAN Eye
caused by allergies, bacteria, viruses, chemicals, ointment, nor does it adversely affect the clinical
or underlying health conditions. The eyes are course of the ulcer or the recovery process. [17]
susceptible to infection because they are not New advanced ocusert system
sterile. They rely on lysozyme (an enzyme found Ocular inserts of Ofloxacin: Ocular inserts of
in the tears) to destroy bacteria. Bacteria line the ofloxacin were prepared with objectives of
surface of the eyelids (all the way down into the reducing the frequency of administration,
shaft of the eyelashes), which makes the obtaining controlled release and greater
conjunctiva predisposed to germs and therapeutic efficacy in the treatment of corneal
conjunctivitis. ulcers. Ofloxacin ocular inserts were prepared to
Medication available but having side effects overcome the problem of the excretion and low
Moxifloxacin hydrochloride ophthalmic solution retention time into the eye. The prepared ocular
used. Serious side effects are not expected to inserts show the more retention time and less
occur during treatment with this medication. excretion through the eye secretions. The ocular
Some eye burning, stinging, irritation, itching, inserts prepared were smooth and passed all the
dryness, redness, tearing; or blurred vision may evaluation tests. Formulations show a
occur. maximum cumulative percentage drug release of
Polymeric Controlled Release Natamycin 91.27 % at the end of 24 hours. Ocuserts
Ocular Inserts: Ocular drug delivery system for formulated also passed the test for sterility. They
Natamycin; a polyene antibiotic is highly useful showed zero-order release of the drug in the in
for the treatment of conjunctivitis and keratitis. vitro and in vivo release studies. The drug in the
Natamycin, a polyene antibiotic is highly useful films was found to be active against selected

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microorganisms as was proved by microbial 6.Sahane NK et al, “ Ocular Inserts: A Review”,
efficacy studies. A high correlation coefficient Drug Invention Today, 2010,2(1):pp- 57-64.
was found between in vitro and in vivo release 7.Zaffaroni A et al, “ Osmotic releasing device
rate studies. Shelf-life of the product was found having a plurality of release rate patterns”, U.S.
to be more than one year. [18] Patent: 1977,4, 036, 227.
Conclusion: Ocular drug delivery systems 8.Robinson, J.C.,“ Ocular Anatomy and
provide local as well as systemic delivery of the Physiology Relevant to Ocular Drug Delivery
drugs. The limitations of existing medical chapter 2, In: Ophthalmic Drug Delivery
therapies for ocular disorders include low drug systems. Volume-58,Marcel Dekker, New
bioavailability, no specificity, side effects, and York,1993:29.9.Venkata Ratnam G et al, ‟
poor treatment adherence to therapy. These Ocular Drug Delivery: an update review ”, IJPBS
limitations may be overcome through the use of Volume 1, Oct-Dec, 2011, pp.437-446.
sustained- release intraocular drug delivery 10.S.A. Menqi et al,“ Controlled and Novel drug
systems. In the area of topical ocular delivery systems, CBS Publishers, New
administration, important efforts concern the Delhi,2004,pp-82-96.
design and the conception of new ophthalmic 11.D.M.Brahmankar et al,“ Biopharmaceutics
drug delivery systems able to prolong the and Pharmacokinetics a treatise, Vallabh
residence time. The use of inserts, which are Prakashan,2010,pp-470-475.
solid devices to be placed in the cul-de- sac or on 12.Rathore K.S et al,“ Review on ocular inserts
the cornea, represents one of the possibilities to ”, International Journal of Pharm Tech Research
reach increased residence time. These solid volume 1,pp.164-169.
ophthalmic devices present the advantage of 13.Bloomfield et al,“ Soluble gentamacin
avoiding a pulsed release due to multiple ophthalmic inserts as a delivery system”,
applications. Finally concluded that the present J.Pharm. Sci., 1987, 76: 583.
review work has been reveals that the ophthalmic 14.Mitra, A.K. et al,“ Ophthalamic drug delivery,
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Corresponding Author:
Geeta Rajput
T.M.U College of Pharmacy, Moradabad- U.P, India
E.mail: geetarajput87@gmail.com

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