[关键词]
[摘要]
目的:制备负电荷的姜黄素炎症靶向自微乳给药系统(NC-CUR-SMEDDS),并对其进行质量评价。方法:在前期姜黄素自微乳(CUR-SMEDDS)的研究基础上,以乳剂的粒径、Zeta电位、包封率和载药量为评价指标,通过单因素试验筛选电荷调节剂的最佳用量,制备NC-CUR-SMEDDS。通过观察微乳外观和微观形态并测定其粒径、Zeta电位、包封率及载药量对其进行质量评价。结果:当加入处方量4%的丁二酸二辛酯磺酸钠时,所形成的微乳Zeta电位可以达到-43.43±0.29mV,外观澄清、透明,粒径分布均匀,平均粒径为14.08±0.082nm,姜黄素载药量为26.48mg·g-1,包封率为94.12%。结论:NC-CUR-SMEDDS包封率高,带负电,粒径分布均匀,符合结肠炎症靶向要求。
[Key word]
[Abstract]
The aim of the study was to prepare and evaluate the quality of negatively charged selfmicroemulsifying drug delivery system of curcumin(NC-CUR-SMEDDS).Based on the CUR-SMEDDS,the optimum amount of excipients was confirmed by the single-factor design experiment taking mean particle size,Zeta potential,drug entrapment efficiency and the drug loadings of curcumin as the evaluation indices for the preparation of NC-CUR-SMEDDS.The quality of NC-CUR-SMEDDS was evaluated by observing its appearance status,transmission electron microscope micrographs and determining particle diameter,Zeta electric potential,drug entrapment efficiency and drug loading.As a result,it was found that the Zeta potential reached -43.43±0.29mV when 4% docusate sodium was added.The appearance of NC-CUR-SMEDDS remained clarified and transparent,and the microemulsion droplets appeared spherical without aggregation with uniform particle size distribution.The mean particle size was 14.08±0.082nm,the drug loading of curcumin was 26.48mg·g-1 and the drug entrapment efficiency was 94.12%.It was concluded that NC-CUR-SMEDDS with high entrapment efficiency and uniform particle size distribution met the requirement of inflammatory target binding in the colon.
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[基金项目]
北京中医药大学自主选题项目(2016-JYB-XS072):姜黄素炎症靶向自微乳治疗溃疡性结肠炎研究,负责人:刘乐环。