FORMULATION AND EVALUATION OF IN SITU MUCOADHESIVE OPHTHALMIC HYDROGEL FOR SUSTAINED DELIVERY OF PEFLOXACIN MESYLATE
Keywords:
Ocular drug delivery, Sodium alginate, Hydroxyethyl cellulose, Sustained delivery, Flouroquinolone antibioticAbstract
Objective: The drawback associated with conventional eye drops needs development of novel ophthalmic delivery system with improved bioavailability and patient compliances. The objective of present work was to develop and evaluate mucoadhesive in situ ocular gel of Pefloxacin mesylate based on the concept of ion activated in situ gelation for the prolonged precorneal residence time.
Methods: Formulations were prepared using Sodium Alginate as gelling agent and Hydroxy ethyl cellulose as mucoadhesive agent. Gels were evaluated for gelling capacity, bio adhesion force, rheological property, ex vivo and in vitro release profile for selection of optimized formulation.
Results: Developed formulations with satisfactory clarity, pH, drug content, gelling capacity, viscosity and bio adhesion were selected for ex vivo and in vitro release studies. An optimum formulation which could sustain the release for 12hours was finalized for further evaluations like; antimicrobial efficacy and irritation test. Formulations were found to be non irritant, effective against the test organisms and exhibited Zero order release pattern and pseudoplastic rheology.
Conclusion: The developed system with sodium alginate and hydroxyl ethyl cellulose can be a feasible alternative to conventional eye drops.
Â
Downloads
References
Gupta H, Velpandian T, Jain S. Ion and pH activated novel in-situ gel system for sustained ocular drug delivery. J Drug Target 2010;18:499-505.
Balasubramaniam J, Kant S, Pandit J. K.-In vitro and in vivo evaluation of the Gelrite gellan gum-based ocular delivery system for indomethacin. Acta Pharm 2003;53:251-61.
Nanjawade BK, Manvi FV, Manjappa AS. In situ-forming hydrogels for sustained ophthalmic drug delivery. J Controlled Release 2007;122:119-34.
Manjappa AS, Nanjwade BK, Manvi FV, Murthy RSR. Sustained ophthalmic in situ gel of ketorolac tromethamine: rheology and in vivo studies. Drug Dev Res 2009;70:417-24.
Shastri DH, Prajapati ST, Patel LD. Thermoreversible mucoadhesive ophthalmic in situ hydrogel: Design and optimization using a combination of polymers. Acta Pharm 2010;60:349-60.
Paulsson M, Hägerström H, Edsman K. Rheological studies of the gelation of deacetylated gellan gum [Gelrite] in physiological conditions. Eur J Pharm Sci 1999;9:99-105.
Gonjari ID, Karmarkar AB, Khade TS, Hosmani AH, Navale RB. Use of factorial design in formulation and evaluation of ophthalmic gels of gatifloxacin: Comparison of different mucoadhesive polymers. Drug Discoveries Ther 2010;4:423-34.
Hagerstrom H, Paulsson M, Edsman K. Evaluation of mucoadhesion for two polyelectrolyte gels in simulated physiological conditions using a rheological method. Eur J Pharm Sci 2000;9:301–9.
Mohammed MM, Hoda AE, Magda W. Mucoadhesive liposomes as ocular delivery system: physical, microbiological, and in vivo assessment. Drug Dev Ind Pharm 2010;36:108-18.
Séchoy O, Tissié G, Sébastian C, Maurin F, Driot JY, Trinquand C. A new long acting ophthalmic formulation of Carteolol containing alginic acid. Int J Pharm 2000;207:109-16.
Gonzalez JP, Henwood JM. Pefloxacin: a review of its antibacterial activity, pharmacokinetic properties and therapeutic uses. Drugs 1989;37:628-68.
Blondeau JM. Fluoroquinolones: mechanism of action, classification, and development of resistance. Surv Ophthalmol 2004;49:73-8.
Choi HG, Jung JH, Ryu JM, Yoon SJ, Oh YK, Kim CK. Development of in situ gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm 1998;165:33-44.
Sultana Y, Aqil M, Ali A, Zafar S. Evaluation of carbopolâ€methylcellulose based sustainedâ€release ocular delivery system for pefloxacin mesylate using rabbit eye model. Pharm Dev Technol 2006;11:313â€9.
Gonjari ID, Hosmani AH, Karmarkar AB, Godage AS, Kadam SB, Dhabale PN. Formulation and evaluation of in situ gelling thermoreversible mucoadhesive gel of Fluconazole. Drug Discoveries Ther 2009;3:6-9.
Doijad RC, Manvi FV, Malleswara Rao VSN, Prajakta, Alsae. Sustained ophthalmic delivery of gatifloxacin from in situ gelling system. Indian J Pharm Sci 2006;68:814-8.
Mitjans M, Infante MR, Vinardell MP. Human hemoglobin denaturation as an alternative to the Draize test for predicting eye irritancy of surfactants. Regul Toxicol Pharmacol 2008;52:89-93.
Dharmendra J, Edmund C, Ajit KB, Rinti B. Development of polyvinyl alcohol–gelatin membranes for antibiotic delivery in the eye drug delivery in the eye. Drug Dev Ind Pharm 2011;37:167–77.
Desi HA, Bhalla HL. Preparation and evaluation of new eye drops containing a combination of ciprofloxacin and dexamethasone. Indian Drugs 2000;37:112.
Pandit J, Bharathi D, Srinatha A, Ridhurkar D, Singh S. Long acting ophthalmic formulation of indomethacin: evaluation of alginate gel systems. Indian J Pharm Sci 2007;69:37-40.
Sechoy O, Tissié G, Sébastian C, Maurin F, Driot JY, Trinquand C. A new long acting ophthalmic formulation of Carteolol containing alginic acid. Int J Pharm 2000;207:109-16.
Larsen B, Smidsrød O, Painter TJ, Haug A. Calculation of the nearest-neighbour frequencies in fragments of alginate from the yields of free monomers after partial hydrolysis; Acta Chem Scand 1970;24:726–8.
Mohanambal E, Arun K, Abdul Hasan Sathali A. Formulation and Evaluation of pH-Triggered in situ Gelling System of Levofloxacin. Indian J Pharm Educ Res 2011;45:58-64.
Srividya B, Cardoza RM, Amin PD. Sustained ophthalmic delivery of ofloxacin from a PH triggered in situ gelling system. J Controlled Release 2001;73:205â€11.
Patel PB, shastri DH, shelat PK. Development and evaluation pH triggered in situ gelling ophthalmic gel formulations of ofloxacin. AJPTR 2011;1:430-45.
Suman Y, Nayyar P. A comparative evaluation of 0.3% eye drops and in situ forming gel of pefloxacin mesylate in experimentally induced pseudomonas conjunctivitis. Continental J Pharmacol Toxicol Res 2008;2:1-5.
Sharma P, Sharma JD. In vitro hemolysis of human erythrocytes by plant extracts with antiplasmodial activity. J Ethnopharmacol 2001;74:239–43.