Bioadhesive ophthalmic drug insert Presentation Transcript
Bioadhesive ophthalmic drug insert
What are the conventional
ophthalmic preparation ?
What are the non conventional
Phase transition systems.
Microspheres and nanoparticles
Q/ what are the problem with the
conventional ophthalmic dosage
form? That lead to the
innovation of ocular inserts
1. rapid precorneal drug loss due to nasolacrimal
2. tear turnover and drug dilution resulting in
3. binding of the lacrimal proteins
4. limited corneal area and poor corneal
5. nonproductive absorption /adsorption
6. Pulsed dosing of drug.
Way this problem is a lot in this
type of dosage forms?
• The anatomy, physiology and biochemistry of
the eye render this organ exquisitely
impervious to foreign substances.SO The
introduction of ophthalmic insert solves many
problems present with conventional ocular
So we should concentrate on two things:
1) To prolong the contact time
2) To enhance corneal permeability
either by mild or transient structural alteration
of corneal epithelium or by modification of
chemical structure of the drug molecules.
Define “Bioadhesive” and by which
intervention we can obtain
• Bioadhesive can be defined as a state in which
two components, of which one is of biological
origin, are held together for extended periods by
the help of interfacial forces. In case of
bioadhesive drug delivery, the term bioadhesion
is used to describe the adhesion between
polymers, either synthetic or natural and soft
• So by the use of certain polymer matrix we can
what are the Bioadhesive ophthalmic
drug inserts(BODI) ?
BODIs are soluble type of “ocular insert” .
Ocular inserts: are
-thin, mono or multilayered,
-drug-impregnated or not,
-solid or semisolid devices placed into the cul-de-sac
or conjuctival sac, whose size and shape are
especially designed for ophthalmic application.
“They are composed of a polymeric support that
may or may not contain a drug.”
What are the advantage of BODI over the
other types of conventional ocular insert?
• overcome the main problems with
conventional ophthalmic inserts, which
include their site of application and the risk of
expulsion from the site.
• BODI are totally eliminated
• do not need to be removed,
• thus limiting manipulations to insertion only.
what are the Criteria for Successful
• Comfort and noninterference with vision
• Biocompatibility and stability
• Reproducibility of release kinetics
• Applicability to a variety of drugs
• Ease of sterility and nontoxicity
• Ease of handling ( insertion and removal)
• Ease of manufacture and low cost.
What are the advantage of ocular
• Increased contact time
• prolonged drug release
• Reduction in dosage frequency
• an accurate dose
• Reduction of systemic side effect .
• Reproducibility of release kinetics.
• Increased shelf life with comparison to
aqueous solutions due to absence of water.
So what are the disadvantages?
• Perceived by the patient as a foreign body.
• Movement around the eye.( not the case with
• Occasionally lose during sleep or while
• Interference with vision
• Difficulty in placement and removal ( BODI
need no removal )
what are the considerations of
• 1. Thickness of Insert
• 2. Surface pH determination
• 3. Mechanical strength
• 4. Bioadhesive strength
• 5. Sterility
• 6. Pattern and rate of the release of drug and
accuracy of the dose
• 7. Dissolution rate
• 8. Type of the polymer used and its swelling
What are the Components Of
Drug polymer Additives
By which methods preparation is
Various methods used in preparation.
1. Solvent casting method
2. Glass substrate technique
3. Melt extrusion technique
Solvent casting method
Poured in glass petridishEvaporation
dried films thus
Solvent casting method
• using different ratios of drug and polymer
• The polymer is dissolved in distilled water.
• A plasticizer is added under stirring conditions.
• The weighed amount of drug was added
• the casting solution was poured in clean glass
petridish and covered with an inverted funnel to
allow slow and uniform evaporation at room
temperature for 48 h.
• The dried films thus obtained
• The ocular inserts were then stored in an airtight
container (desiccator) under ambient condition
examples of drugs that can be
incorporated in the BODI ?
• BODI are sterile polymeric drug
• Soluble type of ocular insert
• Have many advantage the most important is
increase contact time and controlled release
• prepared by polymerization technique
• Applicable with many drugs