Box-Behnken效应面法优化黄芩素纳米胶束制备工艺研究

Preparation Optimization of Baicalein Nano-micelles by Box-Behnken Design-Response Method

    摘要
  • 摘要: 目的 采用Box-Behnken效应面法优化工艺，制备黄芩素-聚乙二醇12羟基硬脂酸酯-磷脂纳米胶束，以改善其溶解性。方法 采用薄膜分散法制备黄芩素-solutol HS15-磷脂复合纳米胶束（BA-Sol-Pls），分别以乙醇用量（X1）、solutol质量浓度（X2）、磷脂质量（X3）浓度为考察因素，采用B-B试验进行设计，粒度测定仪考察纳米胶束粒径和Zeta电位，超速离心法考察胶束的包封率及载药量；效应面法筛选载药纳米胶束的最佳处方。结果 优化处方制备的载药纳米胶束粒径分布均匀，平均粒径为(410±5.98)nm，Zeta电位为-(21±0.92) mV，包封率为90.38%，载药量为5.35%。结论 采用Box-Behnken效应面法优化黄芩素纳米胶束制备工艺是有效可行的。

     

    Abstract: OBJECTIVE To prepare the Nanomicelles of Baicalein-polyethylene glycol-12 hydroxy stearic acid ester-phospholipids for improving its solubility， and to optimize its technology. METHODS Baicalein-solutol HS15- phospholipid (BA-Sol-Pls) were prepared by film-dispersion method. Box-behnken design was employed， with the amount of ethanol (X1)， concentration of solutol (X2) and phospholipids (X3) as the investigation object. Particle size analyzer was used to investigate the particle size and Zeta potential of Nanomicelles. The encapsulation efficiency and drug loading of micelles were determined by Ultracentrifugation. RESULTS The BA-Sol-Pls prepared by optimal formulation were well-distributed. The average particle diameter was (410±5.98) nm， Zeta potential was -(21±0.92) mV. The encapsulation efficiency was 90.38% and the drug-loading rate was 5.35%. CONCLUSION The box-behnken design was effective and suitable for optimization the preparation technology of baicalein nano micelles.

     

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