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Abstract #27264 Published in IGR 12-4
Preparation and evaluation of in situ gelling ophthalmic drug delivery system for methazolamide
Qian Y; Wang F; Li R; Zhang Q; Xu QDrug Development and Industrial Pharmacy 2010; 36: 1340-1347
Purpose: In this study, a thermosensitive in situ gelling vehicle was prepared to increase the precorneal resident time and the bioavailability of methazolamide (MTA). Method: Poloxamer analogs were used as the gelling agents, and the in situ gel was obtained by using a cold method. The gelation temperature, rheological properties, in vitro release as well as in vivo evaluation (the elimination of MTA in aqueous humor and intraocular-lowering effect) of the optimized formulations were investigated. Results: The optimum concentrations of poloxamer analogs for the in situ gel-forming delivery system were 21 (ww) poloxamer 407 and 10 (ww) poloxamer P188. This formulation was able to flow freely under nonphysiological conditions and underwent solgel transition in the cul-de-sac upon placement into the eye. In vitro release studies demonstrated a diffusion-controlled release of MTA from the poloxamer solutions over a period of 10 hours. In vivo evaluation indicated that the poloxamer solutions had a better ability to retain drug than MTA eyedrops did. Conclusion: These results suggested that in situ gelling ophthalmic drug delivery system may hold some promise in ocular MTA delivery. (copyright) 2010 Informa UK, Ltd.
Q. Xu. School of Pharmacy, Nanjing Medical University, 140, Hanzhong Road, Nanjing 210029, China. qunweixu@163.com
Classification:
11.16 Vehicles, delivery systems, pharmacokinetics, formulation (Part of: 11 Medical treatment)
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)