【摘要】 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。更多还原

【Abstract】 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.更多还原