以 α-氰基丙烯酸异丁酯（iBCA）为原料、泊洛沙姆 188 为乳化剂，以捏合法制得的姜黄素（Cur）/羟丙基-β-环糊精（HP-β-CD）包合物（Cur-HP-β-CD）为负载药物，经一步乳化法制得姜黄素/聚（α-氰基丙烯酸异丁酯）载药微球（Cur-HP-β-CD-PiBCA）。考察乳化剂、负载药物的浓度对微球粒径与分布、微球载药率及包封率的影响，并对载药微球的药物释放进行了研究。结果表明：随着乳化剂浓度从 0.01% 增加到 0.07%，载药微球粒径下降，粒径分布变宽，载药率和包封率均增加，适宜的乳化剂浓度为 0.05%；随着药物浓度从 0.03% 增加到 0.07%，微球载药率升高，包封率下降；载药微球的载药率越高，最终的药物累积释放百分率越低。姜黄素经包合和负载，不仅可以有效改善其亲水性，而且可以提高其溶出度，为提高姜黄素的生物利用度奠定了基础。
Curcumin-loaded poly (α-isobutyl cyanoacrylate) microspheres (Cur-HP-β-CD-PiBCA) were prepared by one-step emulsification with α-isobutyl cyanoacrylate as materials, poloxamer 188 as emulsifier, and curcumin complex with hydroxypropyl-β-cyclodextrin (Cur-HP-β-CD) as drug prepared by kneading method. Effects of emulsifier and drug concentration on microspheres size and distribution, drug loading and encapsulation efficiency were investigated in detail. And the curcumin release of drug-loaded microspheres was also studied. Results showed that as the emulsifier concentration increased from 0.01% to 0.07%, particle size of the drug-loaded microspheres decreased while particle size distribution, drug loading and entrapment efficiency increased. The optimized concentration of surfactant was 0.05%. With increasing the concentration of drug from 0.03% to 0.07%, drug loading of Cur-HP-β-CD-PiBCA increased, but encapsulation efficiency decreased. Additionally, the results of drug release experiments revealed that the higher drug loading of Cur-HP-β-CD-PiBCA was, the lower cumulative release percentage was. Drug-loading of cumulative inclusions in HP-β-CD by PiBCA can improve its wettability, and increase the degree of dissolution and bioavailability.
引用本文： 石淑先, 李庆钊, 陈晓农, 夏宇正. 姜黄素/聚(α-氰基丙烯酸异丁酯)载药微球的制备及其药物释放. 生物医学工程学杂志, 2018, 35(5): 749-753. doi: 10.7507/1001-5515.201701045 复制