Development and optimization of gastroretentive mucoadhesive microspheres of gabapentin by Box–Behnken design. (June 2014)

• Record Type: Journal Article
• Authors: Gaur, Praveen Kumar; Mishra, Shikha; Kumar, Avdhesh; Panda, Bibhu Prasad
• Is Part Of: Artificial cells, nanomedicine, and biotechnology. Volume 42:Number 3(2014:Jun.)
• Page Start: 167
• Page End: 177
• Publication Date: 2014-06
• Subjects: Artificial cells -- Periodicals; Nanotechnology -- Periodicals; Blood substitutes -- Periodicals; Tissue engineering -- Periodicals; Molecules -- Periodicals; Biotechnology -- Periodicals; 615.39
• DOI: 10.3109/21691401.2013.800081
• Languages: English
• ISSNs: 2169-1401

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context:</italic> Gabapentin follows saturation kinetics for absorption because of carrier-mediated transport and narrow absorption window in stomach. There is need to develop a gastroretentive formulation to maximize the absorption without crossing the saturation threshold for absorption. <italic>Objective:</italic> The aim was to develop a gastroretentive formulation of gabapentin to increase the fraction of drug absorbed in stomach. <italic>Materials and methods:</italic> Sodium alginate and sodium carboxymethylcellulose were used to formulate the microsphere by ionotropic gelation with calcium chloride. The formulation was optimized using a three-factor, three-level Box–Behnken design. <italic>Results:</italic> The particle size varied from 559.50 to 801.10 μm, entrapment efficiency from 61.29 to 81.00% and in vitro release from 69.40 to 83.70%. The optimized formulation was found using point-prediction, and formulation OF-3 showed optimum results at 608.21 μm size, 79.65% entrapment efficiency and 82.72% drug release and 81% mucoadhesion up to 10 h. The drug release was controlled for more than 12 h. <italic>Discussion:</italic> The particle size was most influenced by sodium alginate while entrapment efficiency and drug release depended upon both polymers. The release followed Higuchi model. <italic>Conclusion:</italic> Gastroretentive formulation was successfully optimized by a three-factor, three-level Box–Behnken design and found to be useful.</p> </abstract>