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用于甲磺酸帕珠沙星控释的戊二醛交联 O-羧甲基壳聚糖微球的制备与表征

Preparation and characterization of glutaraldehyde cross-linked O-carboxymethylchitosan microspheres for controlled delivery of pazufloxacin mesilate.

作者信息

Liu Yan-Fei, Huang Ke-Long, Peng Dong-Ming, Ding Ping, Li Gui-Yin

机构信息

College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China.

出版信息

Int J Biol Macromol. 2007 Jun 1;41(1):87-93. doi: 10.1016/j.ijbiomac.2007.01.003. Epub 2007 Jan 19.

Abstract

O-carboxymethylchitosan (OCMC) microspheres containing an antibiotic drug pazufloxacin mesilate (PM) have been successfully prepared by emulsion cross-linking using glutaraldehyde (GA). Various manufacturing parameters, including amount of cross-linking agent and OCMC:PM ratios were altered to optimize process variables during the microspheres production. The structure and morphology were characterized by Fourier transform infrared (FT-IR), wide-angle X-ray diffraction (WXRD) and scanning electron microscopy (SEM). The swelling and releasing behaviors of the microspheres at pH 1.2 and 7.4 media were investigated. The results revealed that the microspheres had a spherical, rough morphology and with a narrow size distribution. The degree of swelling of microspheres at pH 7.4 media was higher than that at pH 1.2 media. The microspheres proved to be successful in prolonging drug release. The release of PM was found to depend upon the extent of matrix cross-linking and drug loading. The release profiles of PM from OCMC microspheres were found to be biphasic with a burst release followed by a gradual release phase, and followed the Higuchi matrix model.

摘要

采用戊二醛(GA)通过乳液交联法成功制备了载有抗生素甲磺酸帕珠沙星(PM)的O-羧甲基壳聚糖(OCMC)微球。在微球生产过程中,改变了包括交联剂用量和OCMC:PM比例在内的各种制造参数,以优化工艺变量。通过傅里叶变换红外光谱(FT-IR)、广角X射线衍射(WXRD)和扫描电子显微镜(SEM)对其结构和形态进行了表征。研究了微球在pH 1.2和7.4介质中的溶胀和释放行为。结果表明,微球呈球形,表面粗糙,粒径分布窄。微球在pH 7.4介质中的溶胀度高于在pH 1.2介质中的溶胀度。微球被证明能够成功延长药物释放。发现PM的释放取决于基质交联程度和药物载量。PM从OCMC微球中的释放曲线呈双相,先是突释,然后是缓释阶段,且符合Higuchi基质模型。

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