PLGA-Trail微球制备及评价

发布时间：2019-05-22 17:33

【摘要】：微球作为一种缓控释放药物载体成为国内外研究热点,改变传统药物治疗给药方式成为肿瘤药物的一个发展趋势。本文以复乳挥发法制备PLGA-Trail微球,所制备的载药微球进行载药量、包封率、理化性质及形态、体外释药等实验进行考察,以期获得最优制备方法,满足进一步研究需求。本文第一部分对PLGA微球制备方法及国内外研究进展进行综述,对当前微球制备方法进行全面了解和分析,以此为基础,确定本研究使用复乳挥发技术制备PLGA-Trail微球。第二部分对PLGA-Trail微球制备工艺进行全面优化,并对其理化性质进行考察,以包封率及载药量作为微球评价指标,最终确定PLGA-Trail微球制备工艺为:内水相与油相比例为1:20,油相与外水相比例为1:20,PLGA的浓度为120mg/ml、PVA的添加量为5%、漩涡时间为90s、漩涡速度为3000rpm/min、剪切时间为30s、剪切速度为10000rpm/min。再此条件下制备的PLGA-Trail微球具有良好的可重复性,包封率达到51.7%,平均直径为9.3±4μm。第三部分对PLGA-Trail微球进行体外释药测定及动物体内疗效确定,结果表明,体外释药结果显示PLGA-Trail微球释药周期为25d;荷瘤小鼠体内实验证明,PLGA-Trail微球具有明显抑制肿瘤生长作用,单次注射PLGA-Trail微球后21d内,肿瘤生长可受到抑制。综上所述,本文所述PLGA-Trail微球制备工艺合理,载药微球具有稳定包封率,药物缓释作用明显,具有进一步研究和开发价值。
[Abstract]:As a kind of slow release drug carrier, the microsphere has become a hot spot at home and abroad, and changes the traditional medicine treatment mode to become a development trend of the tumor drug. In this paper, PLGA-Trail microspheres were prepared by the method of complex emulsion evaporation, and the drug-loaded microspheres prepared were tested with drug-carrying amount, encapsulation rate, physical and chemical properties and morphology, and in vitro release, so as to obtain the optimal preparation method and meet the further research requirements. The first part of this paper reviews the preparation of PLGA microspheres and the research progress at home and abroad. in the second part, the preparation process of the PLGA-Trail microsphere is comprehensively optimized, the physical and chemical properties of the PLGA-Trail microsphere are researched, the encapsulation rate and the drug loading amount are used as the evaluation indexes of the microspheres, and finally, the preparation process of the PLGA-Trail microsphere is as follows: the ratio of the internal water phase to the oil phase is 1:20, the proportion of the oil phase and the external water phase is 1:20, The concentration of PLGA was 120 mg/ ml, the addition of PVA was 5%, the vortex time was 90 s, the speed of the vortex was 3000 rpm/ min, the shear time was 30 s, and the shear rate was 10,000 rpm/ min. The PLGA-Trail microballoon prepared under this condition has good repeatability, the encapsulation rate reaches 51.7%, the average diameter is 9.3-4.mu. m, and the third part is used for the in-vitro drug release determination of the PLGA-Trail microsphere and the determination of the curative effect of the in vivo. The results show that the release period of the PLGA-Trail microsphere is 25d in vitro. The experimental results of the tumor-bearing mice showed that the PLGA-Trail microsphere has the effect of inhibiting the growth of the tumor, and the growth of the tumor can be inhibited in 21 days after a single injection of the PLGA-Trail microsphere. In conclusion, the preparation process of the PLGA-Trail microsphere is reasonable, the drug-loaded microsphere has a stable encapsulation rate, the drug sustained-release effect is obvious, and the drug-loaded microsphere has further research and development value.
【学位授予单位】：吉林大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：R943

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