Eye is the organ of human body having main function of vision. Ocular drug delivery is the alternative route for the systemic treatment of disease and also a route for the treatment of eye diseases such as conjunctivitis, keratitis etc. Ocular inserts are the one of the most useful and innovative technique for the treatment of eye diseases by increase contact time and providing control release of drug. This review is generated to provide an overview of ocular drug delivery including role of ocular inserts in treatment of eye disorders.
Eye diseases are commonly encountered in day to day life, which are cured or prevented through the conventionally used dosage forms. Delivery to the internal parts of the eye still remains troublesome due to the anatomical and protective structure of the eye. Drugs may be delivered to the eye through the application of four primary modes of administration: topical, systemic, intravitreal, and periocular.
Eye diseases are commonly encountered in day to day life, which are cured or prevented through the conventionally used dosage forms. Delivery to the internal parts of the eye still remains troublesome due to the anatomical and protective structure of the eye. Drugs may be delivered to the eye through the application of four primary modes of administration: topical, systemic, intravitreal, and periocular.
This presentation discusses about the recent drug delivery systems for targeting posterior segment of eye
For detailed information, please go through the reference
Introduction
Anatomy and physiology of human eye
Ocular delivery system
Optimum characters of ophthalmic drugs
Routes of ophthalmic drugs
Mechanism of ocular drug absorption
Barriers and fate of ocular drug delivery
Formulation consideration of ocular dosage forms
Evaluation tests
References
This presentation discusses about the recent drug delivery systems for targeting posterior segment of eye
For detailed information, please go through the reference
Introduction
Anatomy and physiology of human eye
Ocular delivery system
Optimum characters of ophthalmic drugs
Routes of ophthalmic drugs
Mechanism of ocular drug absorption
Barriers and fate of ocular drug delivery
Formulation consideration of ocular dosage forms
Evaluation tests
References
Routes of Ocular Delivery.
COMPOSITION OF EYE.
MECHANISM OF OCULAR ABSORPTION.
Barriers of Drug Permeation.
Anatomical Barrier.
CORNIAL CROSS SECTION.
Physiological Barrier.
Blood-Occular Barriers.
Routes of Ocular Drug Delivery.
Topical Route & Novel Route ocular drug delivery.
Methods to Overcome Barriers.
Bioavailability Improvement & Controlled Ocular Drug Delivery
Slide 1: Title Slide
- Title: Ocular Drug Delivery Systems:
- Presenter Name and Affiliation
Slide 2: Introduction
- Importance of efficient drug delivery to the eye for the treatment of ocular diseases.
- Challenges with conventional eye drops and the need for improved drug absorption and residence time.
- Objectives of ocular drug delivery systems: enhancing drug bioavailability, prolonging drug release, and providing targeted delivery.
Slide 3: Overview of Ocular Drug Delivery Systems
- Definition of ocular drug delivery systems as specialized techniques and formulations for drug administration to the eye.
- Importance of improving drug delivery to achieve therapeutic efficacy.
- Goals: enhancing drug bioavailability, prolonging drug release, and providing targeted delivery.
Slide 4: Types of Ocular Drug Delivery Systems
- Topical Formulations:
- Eye Drops: Traditional method with limited drug absorption.
- Ointments and Gels: Improved residence time but may cause blurred vision.
- Sprays and Aerosols: Effective for certain medications but challenging for accurate administration.
Slide 5: Types of Ocular Drug Delivery Systems (continued)
- Solid Drug Delivery Systems:
- Inserts and Implants: Sustained release of drugs over an extended period.
- Microparticles and Nanoparticles: Enhanced drug stability, bioavailability, and targeted delivery.
Slide 6: Types of Ocular Drug Delivery Systems (continued)
- Contact Lenses:
- Drug-Eluting Lenses: Act as reservoirs to release drugs gradually.
- Mucoadhesive Lenses: Improve drug retention and bioavailability.
Slide 7-45: Advantages of Ocular Drug Delivery Systems
- Increased Bioavailability: Enhanced drug absorption and residence time for improved therapeutic efficacy.
- Targeted Delivery: Localized treatment of ocular tissues, minimizing systemic side effects.
- Prolonged Drug Release: Controlled release systems reduce the frequency of administration.
- Patient Compliance: Convenience and ease of use improve patient adherence to treatment regimens.
Slide 46: Challenges and Future Perspectives
- Barrier Properties: Overcoming the ocular barriers for effective drug penetration.
- Biocompatibility: Ensuring the drug delivery system is well-tolerated by ocular tissues.
- Manufacturing and Regulatory Considerations: Meeting quality standards and regulatory requirements for commercial production.
- Future Developments: Nanotechnology, biomaterials, and gene therapy for advancing ocular drug delivery systems.
Slide 47: Conclusion
- Recap of the importance of ocular drug delivery systems for improving treatment outcomes.
- Potential benefits of enhanced drug bioavailability, targeted delivery, and prolonged drug release.
- Acknowledgment of challenges and the promising future of ocular drug delivery systems.
Slide 48: Thank You
- Contact
ocular drug delivery systems in drug delivery systemsArun Pandiyan
DEFENITION:
Drug delivery systems are designed to enhance the targeted delivery of medications, improving their effectiveness while minimizing side effects. Various approaches include nanoparticles, liposomes, and implantable devices, offering controlled release or targeted delivery to specific tissues. These systems aim to optimize therapeutic outcomes and patient compliance.
CLASSIFICATION OF DRUG DELIVERY SYSTEM
Oral Drug Delivery:- Tablets, capsules, and liquids are commonly used for systemic drug delivery. Controlled-release formulations provide sustained drug release over time
Injectable Drug Delivery:- Intravenous, intramuscular, and subcutaneous injections allow rapid drug delivery into the bloodstream. Depo injections provide sustained release over weeks or months.
Transdermal Drug Delivery:- Patches and topical formulations deliver drugs through the skin. Ensures a controlled and prolonged release of medication.
Inhalation Drug Delivery:- Aerosolized medications for respiratory conditions. Rapid absorption through the lung's extensive surface area.
Implantable Drug Delivery:- Devices like pumps or reservoirs placed under the skin for continuous drug release. Common for long-term conditions requiring a steady dosage.
Nanoparticle-based Drug Delivery:- Nanocarriers (liposomes, micelles, nanoparticles) enhance drug solubility and improve targeted delivery. Effective for delivering drugs to specific cells or tissues.
Targeted Drug Delivery:- Ligand-based systems use specific molecules to target drugs to particular cells or tissues. Minimizes side effects by focusing on diseased areas.
Gastrointestinal Drug Delivery:- Drug formulations designed for specific release in different parts of the gastrointestinal tract. Examples include enteric-coated capsules.
Intrathecal Drug Delivery:- Direct delivery of drugs into the spinal canal. Often used for pain management or neurological conditions.
Ocular Drug Delivery:- Eye drops, ointments, or implants for treating ocular conditions. Ensures targeted drug delivery to the eyes.
These systems cater to diverse medical needs, offering tailored solutions for optimal therapeutic outcomes.
A Review of Potential Effect of Nanotechnology and Control Drug Delivery Syst...ijtsrd
Nanotechnology is a positive concept which will soon improved the field of medical science and technology. In this process used nano meters to penetrate and has improved the medicine and avenues of science. The various types of eye diseases will treated by this nanotechnology, and also enhance the positive effect of the medicated dose. Various aspect of treatment and diagnosis in eye disease are expected to be in future. It will not improved our approach to current therapeutic challenges, but enable to address currently unsolved problems Nanotechnology is the conducted to special treatment process to minimized the drug adverse effect and their accurate dosage form. The technology is being explore as a means of drug delivery, not only the systemic medication, but also for ocular application as many of the condition. Madhusudan Das | Ms Ankita Sharma | Mr. Kaushal K. Chandrul ""A Review of Potential Effect of Nanotechnology and Control Drug Delivery System Introduce Into Ocular Drug Delivery System"" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-3 | Issue-4 , June 2019, URL: https://www.ijtsrd.com/papers/ijtsrd23563.pdf
Paper URL: https://www.ijtsrd.com/pharmacy/pharmacognosy-/23563/a-review-of-potential-effect-of-nanotechnology-and-control-drug-delivery-system-introduce-into-ocular-drug-delivery-system/madhusudan-das
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AN OVERVIEW OF OCULAR DRUG DELIVERY SYSTEM INCLUDING ROLE OF OCULAR INSERTS IN EYE DISORDER TREATMENT
1. Sriram N et al, ICJPIR 2014, 1(2), 32-40
www.icjpir.com
~32~
Available online at www.icjpir.com ISSN: 2349-5448
Intercontinental journal of pharmaceutical
Investigations and Research
ICJPIR |Volume 1 | Issue 2 | Oct–Dec- 2014 Research Article
AN OVERVIEW OF OCULAR DRUG DELIVERY SYSTEM INCLUDING
ROLE OF OCULAR INSERTS IN EYE DISORDER TREATMENT
N. Sriram1
, Dr. S.Jeevanandham2
*, K. Ashok2
1
Holy Mary Institute of Technology and Science-College of Pharmacy, Bogaram, Keesara, R.R, District,
Telangana, India.
2
A.K.R.G College of Pharmacy, Nallagerla, West Godavari District, Andhra Pradesh –534112, India.
Corresponding Author: Dr.S.Jeevanandham
Email: spjeeva1983@gmail.com
ABSTRACT
Eye is the organ of human body having main function of vision. Ocular drug delivery is the alternative route for the
systemic treatment of disease and also a route for the treatment of eye diseases such as conjunctivitis, keratitis etc.
Ocular inserts are the one of the most useful and innovative technique for the treatment of eye diseases by increase
contact time and providing control release of drug. This review is generated to provide an overview of ocular drug
delivery including role of ocular inserts in treatment of eye disorders.
Keywords: Ocular drug delivery, Ocular insert, Conjunctivitis.
I NTRODUCTION
The human eye can be classified into two segments:
anterior and posterior segments. The cornea,
conjunctiva, iris, ciliary body, aqueous humor and
lens are includes in the anterior segment and sclera,
choroid, retina, vitreous humor are includes in the
posterior segment. The outermost transparent
membrane of the eye is cornea such are the corneal
epithelium, bowman's membrane, stroma, descemet's
membrane, and endothelium. The anterior segment is
a fluid of the eye which contains the source of
nutrition to the crystalline lens and cornea. The iris
sphincter and dilator muscles are help full to adjust
the pupil size which regulates the amount of light
entering to the eye.[1, 2]
A ring-shaped muscle attached to the iris called
ciliary muscles. It is important because contraction
and relaxation of the ciliary muscle controls the shape
of the lens. The choroid layer is located behind the
retina and absorbs unused radiation.[3]
The retina is a multi-layered sensory, light sensitive
tissue contains millions of photoreceptors or
photosensitive elements that capture light rays and
convert them into electrical impulses. These impulses
travel along the optic nerve to the brain, where they
are converted into an image. A jelly-like substance
known as vitreous humor, distribute between retina
and lens.[1, 2]
2. Sriram N et al, ICJPIR 2014, 1(2), 32-40
www.icjpir.com
~33~
Fig. 1: Anatomy of Eye
MANAGEMENT OF EYE DISEASES
Conjunctivitis
Bacterial conjunctivitis is an inflammation of the
conjunctiva caused by bacteria.[4, 5]
Fluoroquinolones
Ciprofloxacin or Ofloxacin, Levofloxacin,
Moxifloxacin, Gatifloxacin or Besifloxacin
Aminoglycosides
Tobramycin or Gentamicin
Macrolides
Erythromycin [6, 7]
Keratitis
Bacterial keratitis is an infection and inflammation of
the cornea that cause pain, reduced vision, light
sensitivity and tearing or discharge from the eye that
can, in severe cases cause loss of vision. Treatment
will include third-generation quinolone drops
(ciprofloxacin and ofloxacin) or fourth generation
drops (gatifloxacin or moxifloxacin).[8]
OCULAR DRUG DELIVARY
Ocular drug delivery system is a system to deliver
active pharmaceutical ingredient to ophthalmic route
for local or systemic effect.
TYPES OF OCULAR DRUG DELIVARY
A multitude of ocular dosage forms are available for
delivery of drugs to the eye. These can be classified as
follows:
1. Liquids: Solutions, Suspensions, Sol to gel systems,
Sprays
2. Solids: Ocular inserts, Contact lenses, Artificial
tear inserts, Filter paper strips
3. Semi-solids: Ointments, Gels
4. Miscellaneous: Ocular iontophoresis,
Mucoadhesive dosage forms.[9]
Liquids
It is most popular and desirable state of dosage forms
for the eye and drug absorption rate is fastest from
this state then the other.
Solution and suspensions
Solutions are widely used to administer drugs that
must be active on the eye surface or in the eye after
passage through the cornea or the conjunctiva. The
drug in the solution is in the solved state and may be
immediately active. To increase the corneal contact
time of a drug substance and provide a more sustained
action we use ophthalmic suspensions.
Sol to gel system
It is a new concept of producing a gel in situ (eg. in
the cul-de-sac of the eye) and widely accepted that in
the precorneal region when viscosity of a drug
formulation increased so the bioavailability will also
increased, due to slower drainage from the cornea.
These systems can be triggered by pH, temperature or
by ion activation.
Spray
These sprays are used in the eye for dilating the pupil
or for cycloplegic examination.
Solids
The concept of using solids for the eye is based on
providing sustained release characteristics.[9]
Ocular Inserts
Ophthalmic inserts are defined as sterile preparations,
with a solid or a semi solid consistency, whose size
and shape are especially designed for ophthalmic
application. A number of ocular inserts were prepared
utilizing different techniques to make soluble,
erodible, non erodible, and hydrogel inserts.[10]
Contact lenses
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Contact lenses can absorb water soluble drugs when
soaked in drug solutions.
Artificial tear inserts
This device is designed as a sustained release artificial
tear for the treatment of dry eye disorders.
Filter paper strips
These strips are used to disclose corneal injuries and
infections such as herpes simplex, and dry eye
disorders. The example of filter paper strips are
Sodium fluorescein and rose Bengal dyes.
Semisolids
To provide sustained effects Semi-solids dosage
forms are used. Ophthalmic ointment is used to
prolong drug contact time with the external ocular
surface.Ophthalmic gels are composed of
mucoadhesive polymers that provide localized
delivery of an active ingredient to the eye.
Miscellaneous
Ocular iontophoresis
Iontophoresis is the process in which direct current
drives ions into cells or tissues. When iontophoresis is
used for drug delivery, the ions of importance are
charged molecules of the drug.If the drug molecules
carry a positive charge, they are driven into the tissues
at the anode; if negatively charged, at the cathode.
Mucoadhesive dosage forms
Mucoadhesive polymers are usually macromolecular
hydrocolloids with numerous hydrophilic functional
groups such as carboxyl-, hydroxyl-, amide and
sulphate, capable of establishing electrostatic
interactions. The bioadhesive dosage form showed
more bioavailability of the drug as compared to
conventional dosage forms.[9]
OCULAR INSERTS
Ophthalmic inserts are sterile preparations with a
solid or a semisolid consistency, and whose size and
shape are especially designed for topical or systemic
treatment ophthalmic inserts.[11]
Advantages over other ocular drug delivery system
Increased ocular residence, hence a prolonged
drug activity and a higher bioavailability with
respect to standard vehicles
Possibility of releasing drugs at a slow, constant
rate
Accurate dosing
Reduction of systemic absorption
Better patient compliance, resulting from a
reduced frequency of administration and a lower
incidence of visual and systemic side-effects
Possibility of targeting internal ocular tissues
through non-corneal routes
Increased shelf life with respect to aqueous
solutions
Exclusion of preservatives, thus reducing the
risk of sensitivity reactions
Possibility of incorporating various novel
chemical/technological approaches [12]
Characteristics required for drug
The necessary characteristics for the material
used to fabricate the ocular insert and obtain the
desired drug metering effect are dependent on
the particular drug used.
Hydrophobic polymeric materials having a
relatively high affinity for the drug should be
used in forming the ocular insert. Otherwise, the
drug will be rapidly released from the ocular
insert and the objective of continuous and
sustained release defeated.
However, many hydrophobic polymers having
the desired drug retention and release
characteristics tend to be irritating to the eye and
surrounding tissues.
To provide compatibility with the eye and
surrounding tissues. Since hydrophilic materials
do not have the drug retention characteristics
needed for many drugs, it has been necessary at
times in the past to select materials which
compromise the desired comfort and tissue
compatibility with the desired retention and
release characteristics for the drug.
Should be compatible with eye and surrounding
tissues.
In most cases hydrophobic polymers are used
due to which sustain release of drug is achieved.
Should not irritate ocular tissues.
The surface of the ocular insert in contact with
the eye and surrounding tissues should be soft
and hydrophilic.
Half life should not more.
Protein binding should be low.
Considerable bioavailability should be there.
Characteristics of ocular inserts
Ocular inserts should not produce immunogenic
& mutagenic reactions
Ocular inserts are bio stable in nature &
Biocompatible with tissue of eye
They should have good mechanical strength
Easily sterilizable
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They should not produce toxic & carcinogenic
reactions
Should be free from drug leakage
They should be Retrievable & Release at a
constant rate
Non-interference with vision
Successful oxygen permeability
Ease of manufacture and low cost
Sterility[9,13, 14, 15]
CLASSIFICATION OF OPHTHALMIC
INSERTS [14, 15, 16, 17]
Based upon their solubility behavior
1. Insoluble inserts;Diffusion, osmotic and contact
lens etc.
2.Soluble; Natural polymers (eg. collagen), synthetic
or semi synthetic polymers (eg. cellulose derivatives)
3.Bioerodible
Fig.2. Classification of Ocular inserts
Insoluble ocular inserts
Diffusion
In diffusion inserts, the release of drug is based on
diffusion mechanism. The diffusion systems are
designed of a central reservoir of drug enclosed in a
special semi permeable or micro porous membranes,
which allow the drug to diffuse the reservoir at a
precisely determined rate.
Osmotic
The osmotic inserts are generally divided into two
types, in the first case the central part of the insert is
surrounded by a peripheral part. The central part can
be composed of a single reservoir, which is composed
of the drug with or without an osmotic solute
dispersed through a polymeric matrix, so that the drug
is surrounded by the polymer as discrete small
deposits.[18]
In the second case, the drug and the
osmotic solutes are placed in two separate
compartments, the drug reservoir is surrounded by an
elastic impermeable membrane and the osmotic solute
reservoir surrounded by a semi-permeable membrane.
The peripheral part of these osmotic inserts is
comprised of a film covering made of an insoluble
semi-permeable polymer.[19]
The release of drug
through the osmotic insert follows the zero-order drug
release profile.[20]
Contact lenses
When contact lenses soaked in drug solutions it
absorbs water-soluble drugs. Contact lenses are used
to provide extended release of drugs into the eye. In
ophthalmic drug delivery systems, Contact lenses
have certainly good prospects. The contact lenses are
sub-divided into five groups; rigid, semi-rigid,
elastomeric, soft hydrophilic and bio-polymeric.[9, 14,
21]
Soluble ocular inserts
Soluble ocular inserts are divided into two types
Natural polymer
The first type of soluble inserts is based on natural
polymer. Natural polymer used to produce soluble
ophthalmic inserts is preferably collagen. The amount
of drug loaded will depend on the amount of binding
agent present, the concentration of the drug solution
into which the composite is soaked as well as the
duration of the soaking.
Synthetic and semi-synthetic polymer
The second type of soluble insert is usually based on
semi-synthetic polymers (e.g., cellulose derivatives)
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or on synthetic polymers such as polyvinyl alcohol. A
decrease of release rate can be obtained by using
Eudragit, a polymer normally used for enteric coating,
as a coating agent of the insert. Ethyl cellulose, a
hydrophobic polymer, can be used to decrease the
deformation of the insert and thus to prevent blurred
vision.[17]
Bioerodible
The bioerodible inserts are composed of metrical
homogeneous dispersion of a drug included or not
into a hydrophobic coating which is substantially
impermeable to the drug. These inserts are formed by
bio-erodible polymers (e.g., cross-linked gelatin
derivatives, polyester derivatives) which undergo
hydrolysis of chemical bonds and hence dissolution.
The great advantage of these bio-erodible polymers is
the possibility of modulating their erosion rate by
modifying their final structure during synthesis and by
addition of anionic or cationic surfactants. They are
two in types; insoluble inserts and soluble inserts.[15,
17]
METHOD OF PREPARATION
Solvent casting method
In this method using different ratio of drug and
polymer and prepare no. of batches. Firstly, in
distilled water the polymer is dissolved. In stirring
condition a plasticizer is added to this solution. The
weighed amount of drug was added to this solution
and stirred to get a uniform dispersion. After mixing
this solution poured in Petridish and covered with
funnel to allow slow evaporation at room temperature
for 48 h. The dried films thus obtained then cut into
circular pieces of definite size containing drug. The
ocular inserts were stored in a desiccators (air tight
container) under ambient condition.[22]
Gelfoam disc
A gelfoam disc which diameter is ≈4 mm and 0.5 mm
thickness was punched from a slab of gelfoam sponge
with a common hole punch and phenylephrine HCL
1.7 mg and tropicamide 0.6 mg were dissolved in a
solution (25 µl) of 50% (v/v) ethanol in water. The
solution was placed on the Gelfoam disc. Under
vacuum for at least 72 h, the wet matrics were dried.
By this method placebo devices were also prepared
but without drug. The dose of phenylephrine and
tropicamide are equal to two drops each of
Mydriacyl.[23]
Mould preparation
Using appropriate amounts of polymer, drug and
exicipients we prepare, polymethylsiloxane rod-
shaped silicone inserts. Into the aluminiummoulds
(diameter 0.9 mm, length 22.0 mm), the mixtures
were injected, and were allowed to cure at 45°C for
24 h. The resulting rubbery cylinders (diameter 0.9
mm, length 22.0 mm) were appropriately cut to give a
drug content of specific amount. The final lengths and
weights were in the range 4-12 mm and 2.7-8.0 mg,
depending on insert type. The rod shaped silicon
inserts were used, as such and after poly- acrylic acid
or polymethacrylic acid coating, for hydration tests
and for in vitro/in vivo drug release studies.[24]
EVALUATION PARAMETERS
Sterility study
The inserts were sterilized using gamma radiation
before carrying out the eye irritancy and in vivodrug
release study. No microbial or fungal growth was seen
in any of the formulations, which indicate that the
films were sterilized completely.[25]
Surface pH determination
The pH of solutions, drops, suspensions, and in situ
gels is most often determined using a potentiometric
method. In this method, the pH value is determined by
measuring potential difference between
electrodes placed in examined and reference solutions
of known pH or between measurement electrode and
reference (calomel or silver chloride) electrode, both
placed in examined preparation.[26-28]
Clarity examination
Clarity examination involves the visual assessment of
formulation in suitable lighting on white and black
background. It is performed for liquid forms, with the
exception of suspensions. This examination applies to
eye drops and in situ gels before and after gelling.[29,
30]
Another method of clarity examination involves
transmittance measurement using a UV-Vis
spectrophotometer. This method can be employed in
research on contact lenses filled with active
ingredients. The lenses are hydrated in physiological
saline and placed on the surface of quartz cuvette. The
transmittance is measured afterwards from 200 to
1000 nm wavelength.[31]
Examination of size and morphology of particles
For examination of particles’ size multiple methods
are employed: optical microscopy (microscopic
particle count test), light obscuration particle count
test, dynamic imaging analysis, laser diffraction
particle analyzers, electron microscopy, dynamic light
scattering, coulter counter test and nanoparticle
tracking analysis.[32]
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In-vivo characterization
Eye Irritancy Test (Draize Eye Test)
There are many modifications of eye toxicity/irritancy
test (Draize eye test) performed for dosage forms, that
is, solutions, emulsions, ointments, solids, for
example, inserts, and so forth. The most often used
animal subspecies are albino (eg. New Zealand)
rabbits, which are examined and weighed before the
test and then placed in specifically adapted cages,
designed so as to avoid accidental injuries. The
examined preparations are introduced to conjunctival
sac or applied directly on the cornea. At first, about
0.1mL of analyzed drug was being applied on the
eyeball, but many later examinations pointed to
reducing the amount, for example, to 0.01 mL, which
more reflects real situations. In the test, one eyeball,
usually the left one, is used as a control. After
introducing a drug form on the eyeball, the eyelids are
usually kept closed for a few seconds, although it is
not required. Sometimes sterile solutions are
additionally used for rinsing the eyeball surface. An
assessment of eyeball condition before and after
introducing the formulation is done by observation of
the eyeball in suitable light, often using magnifying
glass or a slit lamp, which ensures more precise
evaluation. Auxiliary procedures which simplify
visualization of changes include dyeing with
fluorescein and taking photos of eyeball. Moreover,
the discomfort level after application may be
indicated by the number of blinkings or rubbings of
the eye. The evaluation takes place usually after 1 h,
24 h, 48 h, and 72 h from introducing a drug form on
the eyeball and, if essential, also after 7 or 21 days.
Duration of examination, as well as its scheme, is
individually adapted to the analyzed formulation.[34-36]
Transcorneal Permeation Study
For transcorneal permeation study, as in the Draize
eye test, healthy albino rabbits are chosen in the
number which is suitable for obtaining reliable
results. The amount of active substance in aqueous
humor after introducing the formulation to
conjunctival sac is marked in specified time intervals.
Using a syringe with needle, after intramuscular or
intravenous anaesthetic injection which may contain,
depending on application, ketamine hydrochloride,
xylazine hydrochloride, or pentobarbital sodium, a
sample of aqueous humor is taken in the amount of
about 150–200 𝜇L and stored at negative temperature,
for example, −20∘C, before HPLC analysis.[37-41]
At
times, additional inhalation anaesthesia is used, for
example, in the form of mixture of 4%
isofluraneoxygen, shortly before or during
paracentesis.[38]
Regional anaesthesia, for example, in
the form of xylocaine solution, may also be
applied.[40]
Noomwong with associates, during
performed tests, added suitable amount of 2% ZnSO4
⋅ 7H2O solution to the taken samples in order to salt
out proteins contained in aqueous humor and then
centrifuged the sample at the speed of 10000 rpm for
1 h at the temperature of −10∘C. They used HPLC
method to examine the amount of active ingredient in
the obtained supernatant [38]
. On the other hand, El-
Laithy et al. and associates examined obtained
samples using a spectrofluorometric method, which
could have been employed due to natural fluorescence
of used drug from fluoroquinolone group,
moxifloxacin.[39]
Table: Marketed ophthalmic products[42]
Brand name Drug Dosage form Use
Dichol Carbahol Sterile solution/injection In ophthalmic surgery
Dexcin Dexamethasone Eye drop In eye infection
Ocupol Polymixin-B Eye drop/Ointment Corneal ulcer
Acivir eye Acyclovir Ointment Eye infection
Chloromycetin Chlorampthenicolpalmitate Ointment Conjunctivitis
Pred forte Prednisolone acetate Suspension Anti allergic
Ciplox Ciprofloxacin Eye drop Conjunctivitis
Restasis Cyclosporine Emulsion Dry eye
Refresh classic Artificial tear fluid Single use vials Dry eye
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Betnisol N Betamethasone Eye drop Eye infection
Refresh tears Hydroxypropyl methylcellulose Eye drops Eye lubricant
Geltear Carbomer Bioadhesive gel Lubricant
Timololxe Timolol maleate In-situ gel Keratoconjuctivitis
CONCLUSION
Ocular delivery based formulations have great
applications for local treatment of eye disease with
relatively lesser side effects as compared to other
route of drug delivery. Progress in the field of ocular
drug delivery has been established recently with
controlled loading and sustained release. Ocular
formulations could be more acceptable and excellent
drug delivery systems if prepared by using the
biodegradable and water soluble polymers. Ocular
inserts might be an alternate for the traditional system
with many of benefits and best system for the
treatment of eye disease as well as systemic disease.
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