Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

[1]  R. Ladani,et al.  Formulation, evaluation and optimization of stomach specific in situ gel of clarithromycin and metronidazole benzoate , 2010 .

[2]  A. Mishra,et al.  Preparation, characterization, and evaluation of gatifloxacin loaded solid lipid nanoparticles as colloidal ocular drug delivery system , 2010, Journal of drug targeting.

[3]  A. Gorle,et al.  Design and evaluation of polymeric ocular drug delivery system. , 2009, Chemical & pharmaceutical bulletin.

[4]  R. Deveswaran,et al.  Sustained ophthalmic delivery of ofloxacin from an ion-activated in situ gelling system. , 2009, Pakistan journal of pharmaceutical sciences.

[5]  J. Madan,et al.  Fast Dissolving Tablets of Aloe Vera Gel , 2009 .

[6]  Manisha Pandey,et al.  BIODEGRADABLE ORTHOPEDIC IMPLANT: FABRICATION AND EVALUATION , 2009 .

[7]  R. Nema,et al.  An Insight into Ophthalmic Drug Delivery System , 2009 .

[8]  Eaga Chandra Mohan,et al.  Preparation and Evaluation of In-Situ-Gels for Ocular Drug Delivery , 2009 .

[9]  E. S. Ghaly,et al.  Formulation and characterization of nystatin gel. , 2008, Puerto Rico health sciences journal.

[10]  B. K. Gupta,et al.  Characterization Of Glipizide-Loaded Polymethacrylate Microspheres Prepared By An Emulsion Solvent Evaporation Method , 2008 .

[11]  D. Mishra,et al.  DESIGN AND CHARACTERIZATION OF BIOADHESIVE IN-SITU GELLING OCULAR INSERTS OF GATIFLOXACIN SESQUIHYDRATE , 2008 .

[12]  M. S. Srinath,et al.  Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention , 2006, AAPS PharmSciTech.

[13]  M. Mohamed Optimization of chlorphenesin emulgel formulation , 2004, The AAPS Journal.

[14]  Rc Doijad,et al.  Sustained ophthalmic delivery of gatifloxacin from In situ gelling system , 2006 .

[15]  Weisan Pan,et al.  Study of an alginate/HPMC-based in situ gelling ophthalmic delivery system for gatifloxacin. , 2006, International journal of pharmaceutics.

[16]  J. Carlfors,et al.  Rheological evaluation and ocular contact time of some carbomer gels for ophthalmic use , 1996 .

[17]  Raymond C Rowe,et al.  Handbook of Pharmaceutical Excipients , 1994 .

[18]  J W Shell,et al.  Ophthalmic drug delivery systems , 1984, Survey of ophthalmology.