title: Formulation optimization of chelerythrine loaded O-carboxymethylchitosan microspheres using response surface methodology.
abstract: The aims of this investigation were to develop a procedure to prepare chelerythrine (CHE) loaded O-carboxymethylchitosan (O-CMCS) microspheres by emulsion cross-linking method and optimize the process and formulation variables using response surface methodology (RSM) with a three-level, three-factor Box-Behnken design (BBD). The independent variables studied were O-CMCS/CHE ratio, O/W phase ratio, and O-CMCS concentration, dependent variables (responses) were drug loading content and encapsulation efficiency. Mathematical equations and response surface plots were used to relate the dependent and independent variables. The process and formulation variables were optimized to achieve maximum drug loading content and entrapment efficiency by the desirability function. The optimized microsphere formulation was characterized for particle size, shape, morphology and in vitro drug release. Results for mean particle size, drug loading content, entrapment efficiency, and in vitro drug release of CHE-loaded O-CMCS microspheres were found to be of 12.18 μm, 4.16 ± 3.36%, 57.40 ± 2.30%, and 54.5% at pH 7.4 after 70 h, respectively. The combination use of RSM, BBD and desirability function could provide a promising application for O-CMCS as controlled drug delivery carrier and help to develop procedures for a lab-scale microemulsion process.
authors: School of Life and Environmental Sciences, Guilin University of Electronic Technology, Guilin, Guangxi 541014, China.
authors: Gui-yin
authors: GY
authors: Li
authors: Ming
authors: M
authors: Zhong
authors: Zhi-de
authors: ZD
authors: Zhou
authors: Yue-dan
authors: YD
authors: Zhong
authors: Ping
authors: P
authors: Ding
authors: Yong
authors: Y
authors: Huang
mesh_terms: D000465:Algorithms; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D053119:Benzophenanthridines / Q000737:chemistry* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D048271:Chitosan / Q000031:analogs & derivatives* / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry* / Q000494:pharmacology; D004339:Drug Compounding / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D015233:Models, Statistical; D009369:Neoplasms / Q000188:drug therapy*; D010316:Particle Size; D012044:Regression Analysis; D013696:Temperature; D014867:Water
chemical_list: D000970:Antineoplastic Agents; D053119:Benzophenanthridines; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; C504164:O-carboxymethylchitosan; D014867:Water; D048271:Chitosan; C016299:chelerythrine