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蓝色葡聚糖2000壳聚糖微球的制备及其体外释放的研究

Preparation and in vitro release of blue dextran 2000-loaded chitosan microspheres
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摘要 目的制备蓝色葡聚糖2000壳聚糖微球,并考察其性质和体外释药特性。方法采用微乳液-离子交联法制备蓝色葡聚糖2000壳聚糖微球,以载药量和包封率为指标、单因素优化处方;考察微球的形态和粒径,及其在3种不同介质中的体外释药情况。结果当药物与壳聚糖比例为1∶5、水油相比为1∶6、壳聚糖浓度为1%时,所制备的微球表面圆整,平均粒径为3.20±0.55μm,平均载药量为15.95%±0.17%,平均包封率为69.09%±0.04%;载药微球在人工肠液中48 h时释放<10%,在人工胃液中24 h时基本释放完全,在p H7.4磷酸盐缓冲液中24 h时释放约30%,此后释药渐缓,72 h时释药约50%。结论所用方法简便可靠,微球在p H7.4磷酸盐缓冲溶液中具明显的缓释效果。 OBJECTIVE To prepare blue dextran 2000- loaded chitosan microspheres and investigate their characteristics and in vitro release. METHODS The microspheres were prepared by microemulsion- ionic crosslinking method,and evaluated with entrapment efficiency and load efficiency. The morphology and mean size of microspheres were evaluated and in vitro drug release was carried out in three different mediums. RESULTS The optimal formulation was the 1∶5 ratio of drug to chitosan,aqueous phase- oil phase( 1∶6),and the content of chitosan of 1%. The microspheres showed good spherical geometry,smooth surface and suitable size. Their mean diameter was 3. 20 ± 0. 55 μm with the drug load efficency of 15. 95% ± 0. 17% and the drug encapsulation efficency of 69. 09% ±0. 04%. Less than 10% release of the drug from the microspheres were observed in the artificial intestinal juice until 48 h. However,the release of blue dextran 2000 increased rapidly in the artificial gastric juice,which was near to 100% at 24 h. The release rate of drug-loaded microspheres in PBS( p H7. 4) was stable,which was close to 30% at 24 h and 50% at 72 h,respectively. CONCLUSION This method is reliable and simple,the microspheres possessed good physical performance and sustained release character in PBS( p H7. 4).
出处 《华西药学杂志》 CAS CSCD 北大核心 2014年第6期616-618,共3页 West China Journal of Pharmaceutical Sciences
基金 国家自然科学基金资助项目(批准号:81202489) 四川省青年基金项目(编号:2011JQ0060)
关键词 蓝色葡聚糖2000 壳聚糖 微球 体外释放 Blue dextran 2000 Chitosan Microspheres In vitro drug release
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