The document discusses ocular inserts, which are thin, solid or semi-solid drug-impregnated devices placed in the eye to provide prolonged drug delivery. It defines ocular inserts and describes different types including soluble, insoluble, and erodible inserts. Applications include treatments for glaucoma, infections, and inflammation. Advantages are prolonged contact time and drug release, while disadvantages include potential loss or irritation. The document outlines manufacturing methods and innovations in ocular insert technologies and drug delivery to the eye.

1. OCULAR INSERTS
Pharmaceutics 2nd semester

2. GROUP MEMBERS:
 Amina Tariq 19623
(types)
 Sidra Munir 18978
(methods of manufacturing)
 Sadia Ayaz 20050
(innovations)
 Saba Inayat 20036
(drug dosage forms)
 Mehwish Saleem 20110
(adv. & disadv.)
 Wardah Tariq 20063
(def. & applications)

3. OCULAR INSERTS

4. CONTENTS:
 Definition
 Types of ocular inserts
 Significance/Applications
 Advantages and disadvantages
 Methods of manufacturing
 Available drug dosage forms in market
 Innovations
 References

5. DEFINITION:
“Ocular inserts are defined as sterile, thin,
mono or multilayered , drug-impregnated,
solid or semi-solid consistency devices
placed into the cul-de-sac or conjuctival sac,
whose size and shapes are especially
designed for ophthalmic application. They
are composed of a polymeric support that
may or may not contain a drug.”

6. Annual ring
(surrounds
reservoir opaque
white for visibility
in handling and
inserting system)
Drug
reservoir
Transparent
rate
controlling
membrane

7. INTRODUCTION:
 Ocular inserts represent a significant
advancement in therapy of eye diseases.
 Ocular inserts offer an attractive alternative
approach to the difficult problem of limited pre-
corneal drug residence time.
 Main objective of ocular inserts is to increase its
contact time with the corneal surface. For
increasing the contact time viscosity-enhancers are
added in preparations.

8. CHALLENGING TASK:
 Ocular drug delivery is one of the most
challenging tasks faced by Pharmaceutical
researchers.
 Major barriers in ocular medication are the
ability to maintain a therapeutic level of the
drug at the site of action for a prolonged
duration.

9.  The anatomy, physiology, and
biochemistry of the eye is such that it
is impervious to foreign substances,
therefore, it is a challenge for the
formulator to pass through the
protective barriers of the eye without
causing any permanent tissue
damage.

11. ABSORPTION OF DRUGS IN THE EYE.
 Topical delivery into the cul-de-sac is, by far, the
most common route of ocular drug delivery,
absorption from this site by.
 1. Corneal
 2. Non-corneal routes.
 Maximum absorption takes place through the
cornea, which leads the drug into aqueous humor.
 The non-corneal route involves absorption across
the sclera and conjunctiva, this route is not
productive as it restrains the entry of drug into the
intraocular tissues

13. TYPES OF OCULAR INSERTS ON THE BASIS OF
SOLUBILITY:
 The foreign-body sensation leads to discomfort,
which causes poor-patient compliance, excessive
lacrimation that accompanies irritation, dilutes the
drug, and reduces its concentration.
 A properly designed ocular insert will minimize the
sensation caused by its insertion .

14. TYPES OF OCULAR INSERTS ON THE BASIS OF
SOLUBILITY:

15. TYPES:
Soluble ocular inserts
Insoluble ocular inserts
Erodible ocular inserts

16. SOLUBLE INSERTS:
 Soluble inserts correspond to the oldest
class of ocular inserts. These types of
inserts are entirely soluble so that they do
not need to be removed from their site of
application

17. CONTI…..
 The release of the drug takes place when
tears penetrate into the insert. This induces
drug release by diffusion and forms a layer
of gel around the core of the insert.
 This gelification causes further release of
the drug, but it is still controlled by diffusion.
 Example is lacrisert

18. INSOLUBLE OPHTHALMIC INSERTS:
 Diffusional Inserts.
 Osmotic Inserts.
 Contact Lenses.

19.  The first two classes (Diffusion and osmotic
systems) are reservoir type of systems. The
reservoir contain either a liquid/ gel/ colloid/ solid
matrix or a carrier – containing drug homogenously
or heterogeneously dispersed or dissolved there in.
 The third class includes contact lenses.

20. DIFFUSIONAL INSERTS:
 The diffusional inserts are composed of a
central reservoir of drug enclosed in
specially designed semi permeable, which
allow the drug to diffuse from the reservoir
at precisely determined rate. The lacrimal
fluid permeating through the membrane until
the sufficient internal pressure is reached to
drive the drug out of reservoir controls the
drug release from such a system.

21. OSMOTIC INSERTS:
 The osmotic inserts are composed of two
distinct compartments.
 One compartment contains drug and other
contains osmotic solute, which is
sandwiched between the rate controlling
membrane.
 The tears diffuse into osmotic compartment
inducing an osmotic pressure due to which
drug diffuses.

23. CONTACT LENSES:
 Contact lenses are covalently cross-linked
hydrophilic or hydrophobic polymer that
forms a three-dimensional network capable
of retaining water aqueous drug solution or
solid components.

24. ERODIBLE OCULAR INSERTS:
 The biodegradable inserts are composed of
material homogeneous dispersion of a drug
included or not into a hydrophobic coating which is
substantially impermeable.
 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.
 Sodi and minidiscs are the examples of erodible
inserts.

25. APPLICATIONS:
 Ocular inserts are widely used as:
 SODI (soluble ocular drug insert)
 Collagen shields
 Ocusert
 Lacrisert
 Dry drops
 Minidisc or ocular therapeutic
 Bioadhesive ophthalmic eye insert
 Gelfoam
 New ophthalmic drug delivery system

26. ADVANTAGES OF OCUSERTS:
 Increased contact time and thus improved bio-
availability.
 Possibility of providing a prolonged drug release
and thus a better efficacy.
 Administration of an accurate dose in the eye and
thus a better therapy.
 Reduction of systemic side effects and thus
reduced adverse effects.
 Reduction of the number of administrations and
thus better patient compliance, comfort.

27. CONTI….
 Lack of explosion.
 Ease of handling and insertion.
 Non-interference with vision and oxygen
permeability.
 Reproducibility of release kinetics.
 Sterility.
 Stability.
 Exclusion of preservatives
 Increased shelf life with comparison to aqueous
solutions due to absence of water.

28. DISADVANTAGES:
 The insert may be lost immediately.
 Sometimes the insert twists to form ‘a figure eight’,
which diminishes the delivery rate.
 A leakage may occur.
 Dislocation of the device in front of the pupil.
 Irritation to eye
 Expensive
 Periodical check of unit
 Retention in the eye for full 7 days

30. METHOD OF MANUFACTURING:
 Casting method:
 Polymer solution of different composition is
prepared in boiling water.
 Keep aside for 20-24 hrs to get clear solution &
then 10% w/w plasticizer is added & stirred for 3
hrs.
 Weighed amount of drug is added & stirred for 4 hrs
to get uniform dispersion.
 Dispersion is disgassed & cast on glass substrate &
dry for at 50C for 18-20 hrs.
 Dried films are carefully removed & inserts of
required dimensions are punch out ,wrap
individually in Al. foil.

31. AVAILABLE DRUG DOSAGE FORMS IN MARKET:
 The therapeutic efficacy of an ocular drug can be
improved by increasing its contact time with the
corneal surface.
 For increasing the contact time viscosity-enhancers
are added in preparations or the drug is formulated
in a water-insoluble ointment formulation, to sustain
the duration of drug-eye contact.

32. THE CONVENTIONAL OCULAR DOSAGE FORMS :
 Eye drops (solution, suspension)

33. OPHTHALMIC OINTMENTS

34.  Unfortunately, conventional dosage forms give only
a marginally sustained drug-eye contact like eye
drop solutions and do not yield constant drug
bioavailability.
 These dosage forms are easy to administer, but
have inherent drawback that most of the instilled
volume is eliminated from the pre-corneal area
resulting in poor bioavailability, ranging from 1 –
10% of the total administered dose.

35.  This occurs mainly due to:
 Conjunctival absorption
 Rapid solution drainage by gravity
 Induced lachrymation
 Blinking reflex
 Low corneal permeability
 Normal tear turnover.
 To overcome this, many ocular drugs are used in
high concentrations. This causes both ocular and
systemic side-effects

36. RECENT TRENDING DRUG DOSAGE FORMS IN
THE MARKET:
 Membrane-bound ocular inserts (biodegradable
and non-biodegradable)

37. MUCOADHESIVE DOSAGE FORMS:
 (ocular films or sheath, ophthaCoil, polymer rods,
HEMA hydrogel, Dispersion, polysulfone capillary
fiber)

38.  Collagen shields, cyclodextrine based system,
ophthalmic rods.
 Filter paper strips (drug-impregnated filter paper
strips for staining agent- sodium fluorescent,
lissamine green and rose Bengal)

39. CONTACT LENSES:
 Soft contact lenses, implants, flexible coils and
cotton pledgets (Drug presoaked hydrogel type,
polymeric gels)

40. IONTOPHORESIS:
 Nanoparticles (Microspheres, nanosuspension,
Amphiphilogels, Niosomes, Liposomes, Dendrimers
and Quantom dots)
 Iontophoresis

41. INNOVATIONS IN EYE DISEASE THERAPY:
 The ocular insert represents a significant
advancement in the therapy of eye:
 Punctal plug

42. OPHTHALMIC IONTOPHORESIS

43. EYE GENE THERAPY

44. NANO TEARS:

45. CONCLUSION:
 In conclusion, an ideal ocular insert as a
therapeutic system should be bio stable,
biocompatible with minimal tissue-implant
interaction, stable, nontoxic, non carcinogenic,
retrievable and should release the drug at a
constant programmed rate for a predetermined
duration of medication.
 . Different categories of drugs like antiglaucoma,
antibacterials, antivirals, anaesthetics, NSAIDs can
be loaded through the ocular inserts for the
treatment of eye disorders.

46. REFERENCES:
 www.thepharmajournal.com
 http://ijpsr.com/bft-article/an-insight-into-ocular-
insert/?view=fulltext
 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3255
407/
 http://www.authorstream.com/Presentation/bhasker
reddy1149-982436-0cular-inserts/
 http://dx.doi.org/10.1155/2014/861904