title: Preparation and drug release properties of norisoboldine-loaded chitosan microspheres.
abstract: This study aimed to develop injectable norisoboldine (NOR) chitosan microspheres formulated through the emulsion cross-linking method. The formulation was optimized using response surface methodology (RSM) with a three-level, three-factor Box-Behnken design (BBD). The morphology, size, physicochemical characterization and in vitro release behavior of the optimized formulation were evaluated. Scanning electron micrographs (SEM) indicated that the microspheres were spherical with a smooth surface. The encapsulation efficiency and drug loading content of the microspheres were 38.89%±1.72% and 4.25%±0.15%, respectively, with an average size of 105μm. Fourier-transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) revealed the absence of a drug-polymer interaction and the amorphous nature of an entrapped drug. Analysis results of drug release in vitro show the burst release of the microsphere in 2h and a slow progression afterward. In vivo studies using Sprague-Dawley rats revealed that the NOR-loaded chitosan microspheres were biocompatible. This study suggests that the BBD with desired formulation could provide a suitable drug delivery system of chitosan microspheres.
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai 201210, China.
authors.forename: Miao
authors.initials: M
authors.lastname: He
authors.affiliation: The Third People's Hospital of Jinan, Jinan 250132, China.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Wang
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai 201210, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Dou
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai 201210, China.
authors.forename: Guixin
authors.initials: G
authors.lastname: Chou
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai 201210, China. Electronic address: xhweixh@163.com.
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Wei
authors.affiliation: The MOE Key Laboratory for Standardization of Chinese Medicines and the SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China; Shanghai R&D Center for Standardization of Chinese Medicines, Shanghai 201210, China.
authors.forename: Zhengtao
authors.initials: Z
authors.lastname: Wang
mesh_terms: D000470:Alkaloids / Q000737:chemistry*; D000818:Animals; D048271:Chitosan / Q000737:chemistry* / Q000633:toxicity; D004337:Drug Carriers / Q000737:chemistry* / Q000633:toxicity; D065546:Drug Liberation; D008297:Male; D008422:Materials Testing; D008863:Microspheres; D051381:Rats; D017207:Rats, Sprague-Dawley; D012984:Software; D013583:Synovial Membrane / Q000187:drug effects
chemical_list: D000470:Alkaloids; D004337:Drug Carriers; C464745:norisoboldine; D048271:Chitosan
keywords: Chitosan; Microsphere; Norisoboldine; Response surface methodology