FORMULATION AND IN-VITRO EVALUATION OF MOXIFLOXACIN OCULAR INSERTS
Objectives: Most ocular diseases are treated with topical applications of eye drops. After instillation of an eye drop, typically less than 5 % of the applied drug penetrates the cornea and reaches intraocular tissues, while a major fraction of the instilled dose is absorbed and enters the systemic circulation. The objective of present work is to improve ocular bioavailability and corneal contact time of a Moxifloxacin for better permeation through cornea.
Methods: Five formulations were prepared by film casting method. Polyvinyl pyrrolidene, methyl cellulose and hydroxyl propyl methyl cellulose were used as polymers. PEG 400 was used as plasticizer.
Results: The release from the ocular inserts may be considered to follow zero order as evidenced from the regression coefficient (r2) value which is higher for MF4 (.9991).Â The release from formulation code MF1 was found to be 80 % upto 24 hrs. The release from formulations MF2 and MF3 was 91.7 % and 92.10 % respectively within 24 hrs. The release from formulation 4 was 95.23% within 24 hrs. The release from MF5 was upto 60.73% within 24 hrs. The ocular inserts of formulation MF5 were hard and brittle.
Conclusion: The formulation MF4 has the potential to formulate moxifloxacin ocular inserts. However in-vivo studies in animals and antimicrobial studies are required before this could be evaluated as an alternative to moxifloxacin eye drops.
Keywords: Ocular inserts, Moxifloxacin, Ophthalmic, STF, Release, In-vitro.
2. Karlgard CC, Wong NS, Jones LW, Moresoli C. In Vitro uptake and release studies of ocular pharmaceutical agents by silicon-containing and p-HEMA hydrogel contact lens materials. Int J Pharm 2003;257(1-2):141â€“51.
3. Allen LV, Popovich NG, Ansel HC. Special solutions and suspensions. In: Anselâ€™s Pharmaceutical dosage forms and drug delivery systems. 8th ed. Lippincott Williams & Wilkins; 2008. p. 540-1.
4. Sharma J, Majumdar DK. Moxiflocain laded contact lens for ocular delivery-An in Vitro study. Int J Pharm Pharm Sci 2012;4(1):605-9.
5. Onlen y, Tamer C, Oksuz H, Duran N, Altug ME, Yakan S. Comparative trail of different anti-bacterial combinations with propolis and ciprofloxacin on Pseudomaonas kratitis in rabbits. Microbiol Res 2007;162:62-8.
6. Ophthalmic Preparations by John C Lang, Robert E Roehrs, Rajni Jani in Remington-The Science and Practice of pharmacy. Ed 21(1):857.
7. Saski H, Tei C, Nishida K, Nakamura J. Drug release from an ophthalmic insert of a betaâ€“blocker as an ocular drug delivery system. J Cont Rel 1993;24(27):127-37.
8. Oâ€™Neil MJ, editor. The Merck Index: An encyclopedia of chemicals, drugs, and biologicals. 14th ed. Whitehouse Station,NJ,USA: Merck & Co. Inc; 2006.
9. British Pharmacopoeia, Vol 1, London: The Stationary Office; 2008.
10. Sweetman SC, editor. Martindale: The complete drug reference. 35th ed. The pharmaceutical Press; 2007.
11. Takamura A, Ishii F, Hidaka H. Drug release from poly(vinyl alcohol) gel prepared by freeze-thaw procedure. J Control Rel 1992;20:21â€“7.
12. Thanoo BC, Sunny MC, Jaikrishnan A. Controlled release of oral drugs from cross-linked polyvinyl alcohol microspheres. J Pharm Pharmacol 1993;45(1):16-20.
13. Deamin RD, Seymour RB. Addatives of plasticizers Academic press: Newyork; 1978. p. 203.