this is a presentation show controlled release new ocular delivery systems and problems of conventional ocular delivery systems

1. Outline
1.Introduction
2.Why there is a need for such dosage forms
3.Technologies used
4.Examples from the market
5.Special considerations while manufacturing
6.Conclusion
7.References Remon Maged Agaiby

2. • The new drug development system is the most popular and well accepted route.
• BV is very poor Efficient protective mechanism Blinking
Barrier prop. of the Cornea Reflex lacrimation
Low tear volume (7-30 μl) Nasolacrimal Drainage
Low capacity of conjunctival sac
Poor retention of applied drug on surface of the eye
• A small amount is available for its therapeutic effect need frequent dosing
tc several systemic side effects excipients local drug concentration
• Ideal ophthalmic drug delivery must be able to sustain the drug release for
prolong period of time.
• So the challenge in front of formulator is to circumvent the protective barriers
of the eye without causing permanent tissue damage.
<1 %

3. • The ocular BV must be increased from
less than 1% to 15-20% of dose.
• To improve ocular BV
viscosity
mucoadhesive polymers
• But these approaches to prolong corneal contacts time level led to
improvement in ocular BV.
Goal
Effective
drug
For a
extended
period of
time
With less
frequent
dosing
At intended
site of
action
To avoid
risk of eye
damage
For
enhance
patient
compliance

4. 1. Increased accurate dosing to overcome the side effects.
2. Increase the ocular BV of drug by increasing the corneal contact time.
3. Provide targeting within the ocular globe.
4. Provide sustained and controlled drug delivery.
5. Provide comfort, better compliance to the patient and to improve therapeutic
performance of the drug
6. Provide better housing of delivery system
7. Circumvent the protective barriers like drainage, lacrimation and conjunctival
absorption.

5. 8. prolonging precorneal residence time
9. Minimizing precorneal loss
10. Minimizing the preservative burden and other excipients
11. Decreasing the effect of washout when insilling multiple drops
12. Better patient compliance
13. Increased shelf life

6. Ocular
insert Collagen
shield
Polymeric gels
Colloidal
delivery system
Polymeric drug
delivery
Vascular
delivery
liposomes
Niosomes
Mucoadhesive
dosage forms
Ocular
iontophoresis
Contact
lenses
soluble
insoluble
In-situ activated gel
forming systems
Performed or bio-
adhesive hydrogels
microemulsion
nanosuspension
microparticle
nanoparticles

7. Ocular insert
Ocusert
lacrisert
Alza crop
Merk
In situ gel timoptic Merk
liposomes ocusoft ocusoft
Viscosity
enhancer/muco
adhesive
Viscotrears
Nyogel
Novartis
Novartis
Collagen shield proshield Alcon

8. 1. IN-VIVO study:
- dosage form is applied to one eye of animals and the other eye
serves as control removed at regular time analyzed the drug content
2. IN-VITRO evaluation method:
- Bottle method : placed in the bottle containing dissolution medium at sp. Temp. and pH shaked
sample of medium is taken analyzed for the drug content
- Diffusion Method: placed in donor comp. buffer medium is placed bet. Donor and receptor comp.
drug diffused in receptor comp. is measured at time interval
- Modified rotating basket method:
- Modified rotating paddle apparatus:
3. Accelerated stability studies
- predict the breakdown that may occur over prolonged period of storage at normal shelf condition
- Temp. Humidity intensity of light or oxygen
- analyzed the drug content at interval time
- determine shelf life and expiry date

9. • Ideal system should be able to achieve an effective drug concentration at the
target tissue for an extended period of time while minimizing systemic
exposure .
• The system should be both comfortable and easy to use.
• Patient acceptance will continue to be emphasized in the design future ocular
drug selivery system
• Novel delivery technologies are needed to overcome the anatomical and
physiological constrains of the eye.
• Improve BV by increasing ocular drugs residence time
• Diminish side effects due to systemic absorption and reducing dose regimen
• Improve patient compliance by reducing the frequency of dosing

10. 1. Nanjawade BK, Manvi FV, Manjappa AS. Insitu-forming hydrogels for
sustained ophthalmic drug delivery. J Control Release 2007;126:119-34.
2.Khar RK et al, “Targeted and Controlled drug delivery novel carrier systems”
1 st ed. New Delhi; CBS Publishers and Distributors; 2002.
3.Davis JL, Gilger BC, Robinson MR. Novel approaches to ocular drug delivery.
Curr Opin Mol Ther.2004;6:195–205.
4. Lee VHL, Robinson JR: Topical ocular drug delivery: recent developments
and future challenges. Journal of Ocular Pharmacology
1986; 2: 67–108