Preparation and drug release properties of norisoboldine-loaded chitosan microspheres

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• 作者：Miao He^a ; ^b ; Haiyan Wang^c ; Wei Dou^a ; ^b ; Guixin Chou^a ; ^b ; Xiaohui Wei^a ; ^b ; ^{xhweixh@163.com" class="auth_mail" title="E-mail the corresponding author} ; ^{xhwei2000@hotmail.com" class="auth_mail" title="E-mail the corresponding author} ; Zhengtao Wang^a ; ^b
• 关键词：Chitosan ; Norisoboldine ; Microsphere ; Response surface methodology
• 刊名：International Journal of Biological Macromolecules
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：91
• 期：Complete
• 页码：1101-1109
• 全文大小：3703 K

文摘

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 105 μm. 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 2 h 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.