顺铂\|聚己内酯微球的研制及其缓释性能测试
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1.福建医科大学 药学院药物化学系 福州 350122; 2.福建省皮肤病性病防治院,福州 350009; 3.福建医科大学 药学院实验中心,福州 350122

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R318.08; R944.9

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基金项目: 福建省自然科学基金(2015J01316; 2016J01686); 福建省科技创新联合资金(2016Y9053)作者简介: 林爱珠,女,福建医科大学2016级硕士研究生 通讯作者: 林 媚. Email: linmei79@126.com收稿日期: 2018-09-13


Preparation of Cisplatin-loaded Polycaprolactone Microspheres and Their Sustained Release Performance
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1. Department of medicinal chemistry, School of Pharmacy, Fujian Medical University, Fuzhou 350122, China; 2. Fujian Provincial Institute of Dermatology and Venereology, Fuzhou 350009, China; 3. Center for Comprehensive Experimental Pharmacy, Fujian Medical University, Fuzhou 350122, China

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    摘要:

    目的 制备顺铂-聚己内酯微球,探讨该微球载药量、粒径大小及体外释放的影响因素。 方法 采用水包油(O/W)乳化法和溶剂挥发相结合的方法制备微球,利用紫外分光光度计测定载药率和包封率,采用偏光显微镜及扫描电镜观察其粒径大小和表面形态。 结果 当聚乙烯醇浓度为3.5%、乳化搅拌速度为800 r/min时,采用高分子量的聚己内酯负载顺铂,可制得粒径约为54 μm的顺铂微球,其载药率为7.8%、顺铂包封率为75%。药物释放速率与微球粒径大小有关,且遵循Fickian扩散定律。 结论 通过优化条件制得的顺铂-聚己内酯微球形态良好,粒径均一,有良好的缓释行为。

    Abstract:

    Objective To prepare cisplatin-loaded polycaprolactone microspheres and investigate the influencing factors on drug-loading rate, particle size and sustained release property. Methods The microspheres were fabricated by oil-in-water(O/W)emulsion and solvent evaporation technique. The drug loading rate and encapsulation efficiency of microspheres were investigated by using ultraviolet spectro-photometry(UV)and the shape and particles size of microspheres were characterized by polarizing microscope and scan electron microscope(SEM). Results The results showed that cisplatin-loaded microspheres of 54 μm size were prepared with high molecular weight of polycaprolactone when the concentration of polyvinyl alcohol was 3.5% and the speed of emulsification was 800 r/min. The drug loading rate could reach 7.8% and the encapsulation efficiency of cisplatin could reach about 75%. The drug release behavior of microspheres was related to the size of microspheres and fitted well with the Fickian diffusion model. Conclusion The resulting cisplatin-loaded microspheres has good shape, homogeneous particle size and good sustained release properties under the optimized conditions.

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林爱珠, 方芳, 吴宏霞, 刘天惠, 柯方, 林媚.顺铂\|聚己内酯微球的研制及其缓释性能测试[J].福建医科大学学报自然版,2019,(4):219-223

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