Li Guozhuan, Yao Liang, Li Jing, Qin Xiaoyan, Qiu Zhen, Chen Weidong
Anhui University of Chinese Medicine, Xiangshan Road, Hefei 230012, China.
Hefei First People's Hospital, Hefei, 230038, China.
Asian J Pharm Sci. 2018 Jan;13(1):82-90. doi: 10.1016/j.ajps.2017.09.002. Epub 2017 Oct 10.
The aim of the present study was to develop a novel long-acting Poly (lactic-co-glycolic acid) (PLGA)-based microspheres formulation of Bisdemethoxycurcum (BDMC) by emulsion-solvent evaporation method. Meanwhile, the effects of the volume ratio of the dispersed phase and continuous phase, the concentration of PLGA and PVA, the theoretical drug loading and stirring speed were investigated. The mean diameter of the microspheres was 8.5 µm and the size distribution was narrow. The encapsulation efficiency (EE) and drug loading efficiency (DLE) of BDME loaded PLGA microspheres (BDMC-PLGA-MS) was 94.18% and 8.14%, respectively. In an study of drug release, it can be concluded that the BDMC-PLGA-MS exhibited sustained and long-term release properties for 96 h. Stability studies suggested that the microspheres we prepared had a very good stability. Furthermore, the results of an study indicated that the BDMC-PLGA-MS had sustained release effect and was mainly distributed in the lung tissue, and less distribution in other tissues, which indicated that microspheres could be an effective parenteral carrier for the delivery of BDMC in lung cancer treatment.
本研究的目的是通过乳液-溶剂蒸发法开发一种新型的基于聚乳酸-乙醇酸共聚物（PLGA）的双去甲氧基姜黄素（BDMC）长效微球制剂。同时，研究了分散相和连续相的体积比、PLGA和PVA的浓度、理论载药量和搅拌速度的影响。微球的平均直径为8.5 µm，粒径分布狭窄。载有BDME的PLGA微球（BDMC-PLGA-MS）的包封率（EE）和载药效率（DLE）分别为94.18%和8.14%。在药物释放研究中，可以得出结论，BDMC-PLGA-MS具有96小时的持续和长期释放特性。稳定性研究表明，我们制备的微球具有非常好的稳定性。此外，一项研究结果表明，BDMC-PLGA-MS具有缓释作用，主要分布在肺组织中，在其他组织中的分布较少，这表明微球可能是BDMC在肺癌治疗中有效的非肠道给药载体。
