姜黄素炎症靶向自微乳的制备及质量评价

Preparation and Quality Evaluation of Negatively Charged Self-Microemulsifying Drug Delivery System of Curcumin

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±0.29 m V,外观澄清、透明,粒径分布均匀,平均粒径为14.08±0.082 nm,姜黄素载药量为26.48 mg·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。

The aim of the study was to prepare and evaluate the quality of negatively charged self-microemulsifying 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±0.29 m V 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±0.082 nm, the drug loading of curcumin was 26.48 mg·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.