title: Evaluation of carbopol-methyl cellulose based sustained-release ocular delivery system for pefloxacin mesylate using rabbit eye model.
abstract: The major purpose of this study was to develop and characterize a series of carbopol- and methyl cellulose-based solutions as the in situ gelling vehicles for ophthalmic drug delivery. The rheological properties, in vitro release as well as in vivo pharmacological response of a combination of polymer solutions, including carbopol and methyl cellulose, were evaluated. It was found that the optimum concentration of carbopol solution for the in situ gel-forming delivery systems was 0.3% (w/w), and that for methyl cellulose solution was 1.5% (w/w). The mixture of 0.3% carbopol and 1.5% methyl cellulose solutions showed a significant enhancement in gel strength in the physiological condition; this gel mixture was also found to be free flowing at pH 4.0 and 25 degrees C. The rheological behaviors of carbopol/methyl cellulose solution were not affected by the incorporation of the drug. Drug levels in the aqueous humor of the rabbits were well above the MIC-values of relevant bacteria after 12 hours, the results of an optimized formulation containing 0.18% of pefloxacin mesylate compared well with the 0.3% marketed eye drop formulation, indicating our formulation to be significantly better considering that a similar effect was obtained at half the concentration. Both the in vitro release and in vivo pharmacological studies indicated that the carbopol/methyl cellulose solution had better ability to retain drug than did the carbopol or methyl cellulose solutions alone. The results demonstrated that the carbopol/methyl cellulose mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability of pefloxacin mesylate.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, Hamdard Nagar, New Delhi, India. yas2312003@yahoo.com
authors.forename: Yasmin
authors.initials: Y
authors.lastname: Sultana
authors.forename: M
authors.initials: M
authors.lastname: Aqil
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
authors.forename: Shadaab
authors.initials: S
authors.lastname: Zafar
mesh_terms: D000180:Acrylic Resins; D000818:Animals; D003692:Delayed-Action Preparations / Q000008:administration & dosage*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D024841:Fluoroquinolones / Q000008:administration & dosage*; D008297:Male; D008747:Methylcellulose / Q000737:chemistry*; D008954:Models, Biological; D009883:Ophthalmic Solutions / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry*; D011817:Rabbits; D013997:Time Factors; D015366:Pefloxacin
chemical_list: D000180:Acrylic Resins; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D024841:Fluoroquinolones; D008747:Methylcellulose; D009883:Ophthalmic Solutions; D011145:Polyvinyls; D015366:Pefloxacin; C006912:carboxypolymethylene