OCULAR DRUG

DELIVERY SYSTEM
Submitted by: Pratiksha Srivastava
M.Pharm
(1st year)
Galgotias university

INTRODUCTION:

Ocular administration of drug is

primarily associated with the need to
treat ophthalmic diseases.
Meant for local therapy and not for
systemic action.
Applied topically to the cornea, or
instilled in the space between the
eyeball and lower eyelid

ANATOMY OF THE EYE

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%.

MECHANISM OF OCCULAR DRUG ABSORPTION

DRUG IN TEAR FLUID

Ocular Absorption
(5% of the dose)
Corneal
Route:
-Primary Route.
-Small Lipophilic
Drugs.

Conjunctival
and Sclera
Route:
-Secondary Route.
-Large Hydrophilic
Drugs.

Aqueous
Humor

Ocular Tissue

Systemic Absorption
(50-100% of the dose)
Major Routes:
-Conjuctiva of eye
-Nose
Minor Routes:
-Lacrimal Drainage
-Pharynx
-Aqueous Humor
-Inner Ocular Tissues

Elimination
5

IDEAL CHARACTERISTIC
Sterility
Isotonicity:

e.g.: 1.9% boric acid, 0.9% NaCl

Buffer/pH
Less

adjustment

drainage tendency

Minimum

protein binding

CLASSIFICATION
OCDDS
SOLUTION

OF

SUSPENTION
EMULSION
OINTMENT
INSERT
GELS

LIPOSOMES
NIOSOMES
DISCOMES
CONVENTIONA
L

IMPLANTS
IONTOPHORESIS
DENDRIMER
MICROEMULSION

VESICULAR

OCULAR DELIVERY
SYSTEMS
CONTROL
RELEASE

PARTICULATE

NANOSUSPENSION
MICRONEEDLE

MICROPARTICLES

MUCOADHESIVE
POLYMERS

NANOPARTICLES

CONVENTIONAL
EYE DROPS:
Drugs

which are active at eye or eye surface are widely

administered in the

form of Solutions, Emulsion and

Suspension.
Various

properties of eye drops like hydrogen ion

concentration, viscosity and instilled volume can influence

retention of a solution in the eye.

Less than 5 % of the dose is absorbed after topical

administration into the eye.

The

dose is mostly absorbed to the systemic blood

circulation via the conjunctival and nasal blood vessels.

ADVANTAGES AND DISADVANTAGES OF

EYE DROPS:
Dosage
form

Advantages

Disadvantages

Solutions

1. Convenience
2. Usually do not
interfere with vision
of patient.

1. Rapid precorneal
elimination.
2. Non sustained action.
3. To be Administered at
frequent intervals.

Suspension

1. Patient compliance.
2. Best for drug with
slow dissolution.
3. Longer contact time

1. Drug properties decide

performance loss of
both solutions and
suspended particles.
2. Irritation potential due
to the particle size of
the drug.

Emulsion

1. Prolonged release of
drug from vehicle

1. Blurred vision.
2. patient non
compliance.

OINTMENT:

Prolongation of drug contact time with the

external ocular surface can be achieved using
ophthalmic
ointment
. filtered while molten to remove
Ointment base
is sterilizedvehicle
by heat and

10

Advantages:

1.

Longer contact time and greater storage

stability.
Flexibility in drug choice.
Improved drug stability.

2.
3.

.Disadvantages:
1.
2.
3.
4.

Sticking of eyes lids.

Blurred vision.
Poor patient compliance.
Matting of eyelids.

VESICULAR:
LIPOSOMES: Liposomes

are biocompatible and biodegradable lipid vesicles

made up of natural lipids and about

25 100 nm in diameter.
They

are having an intimate contact with the corneal and

conjunctival surfaces which is desirable for drugs that are

poorly absorbed, the drugs with low partition coefficient, poor
solubility or those with medium to high molecular weights
and thus increases the probability of ocular drug absorption.
Vesicle

composed of phospholipid bilayer enclosing aqueous

compartment in alternate fashion.

It

is Biodegradable, Non-toxic in nature.


Drugs

ADVANTAGES
delivered intact to

They need many

various body tissues.

Liposomes

both

can be used for

hydrophilic

modification for drug

delivery to special

and organs.

hydrophobic drug.
Possibility

DISADVANTAGES

Stability problem and

of targeting and oxidative degradation.

decrease drug toxicity.

The

Requires special
packaging and storing

size, charge and other facility.

characteristics
can
be Costly.
altered according to drug
and desired tissue.

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.

ADVANTAGES:

The vesicles can act as a depot to release the

drug slowly and offer a controlled release.

They are osmotically active and stable.

They increase the stability of the entrapped drug.

Improves therapeutic performance of the drug

by protecting it from the biological environment and
restricting effects to target cells, thereby reducing
the clearance of the drug.

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NON ERODIBLE INSERTS:

OCUSERT:

The Ocusert therapeutic system is a flat, flexible,

elliptical device designed to be placed in the inferior culde-sac between the sclera and the eyelid and to release
Pilocarpine continuously at a steady rate for 7 days.

The device consists of 3 layers.

1. Outer layer - ethylene vinyl acetate copolymer layer.
2. Inner Core

- Pilocarpine gelled with alginate main

polymer.
3. A retaining ring - of EVA impregnated with titanium
dioxide.

ADVANTAGES

Reduced local side effects and toxicity.

Around the clock control of drug.

Improved compliance.

DISADVANTAGES

Retention in the eye for the full 7 days.

Periodical check of unit.

Replacement of contaminated unit

Expensive.

CONTACT LENS:

Contact lenses can be a way of providing extended

release of drugs into the eye.

Conventional hydrogel soft contact lenses have the

ability to absorb some drugs and release them into the
post lens lachrymal fluid, minimizing clearance through
the conjunctiva.

Their ability to be a drug reservoir strongly depends on

the water content and thickness of the lens, the
molecular weight of the drug, the concentration of the
drug loading solution and the time the lens remains in
it.

ERODIBLE INSERTS:

The solid inserts absorb the aqueous tear fluid and

gradually erode or disintegrate. The drug is slowly
leached from the hydrophilic matrix.

They quickly lose their solid integrity and are

squeezed out of the eye with eye movement and
blinking.

Do not have to be removed at the end of their use.

LACRISERTS

Sterile

rod shaped device made up of hydroxyl

propyl cellulose without any preservative.
For the treatment of dry eye syndromes.
It weighs 5 mg and measures 1.27 mm in diameter
with a length of 3.5 mm.
It is inserted into the inferior fornix.

SODI

Soluble

ocular drug inserts.

Small oval wafer.
Sterile thin film of oval shape.
Weighs 15-16 mg.
Use glaucoma.

Lacriserts

Minidisc

Countered disc with a convex front and a concave

back surface.

Diameter 4 to 5 mm.

Composition

Silicone based prepolymer (4-methacryloxy)-butyl poly

di methyl siloxane. (M2DX)

M-Methyl a cryloxy butyl functionalities.

D Di methyl siloxane functionalities.

Pilocarpine, chloramphenicol.

Advantages And Disadvantages Of

Ocular Inserts
Type
Erodible
inserts

Non-erodible
inserts

Advantages

Disadvantages

Effective.
Flexiblility in drug
Patient
type & dissolution
discomfort.
rate.
Requires patient
Need only be
insertion.
introduced into
eye & not
removed.
Controlled rate of
release.
Prolonged
Patient
delivery.
discomfort.
Flexibility for type Irritation to eye.
of drug selected. Tissue fibrosis.
Sustained
release.

1. Implants

1.

Implants have been widely employed to extend the

release of drugs in ocular fluids and tissues
particularly in the posterior segment.

2.

Implants can be broadly classified into two

categories based on their degradation properties:
(1) Biodegradable
(2) Nonbiodegradable

Implants can be solids, semisolids or particulate-based

delivery systems.

For chronic ocular diseases like cytomegalo virus

(CMV) retinitis, implants are effective drug delivery
system. Earlier non biodegradable polymers were
used but they needed surgical procedures for
insertion and removal.

Presently biodegradable polymers such as Poly

Lactic Acid (PLA) are safe and effective to deliver
drugs in the vitreous cavity and show no toxic
signs.

EVALUATION OF OCDDS
. 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