[关键词]
[摘要]
目的 优化马钱子碱纳米结构脂质载体(B-NLC)处方与制备工艺。方法 溶剂乳化超声法制备B-NLC,以单因素考察法结合星点设计-效应面法(CCD-RSM)优化处方与制备工艺。结果 所制备的B-NLC为淡蓝色乳光的透明液体。最优条件为药物用量为1.28 mg,泊洛沙姆188质量浓度为1.08%,固态脂质与液态脂质的比例为1.45:1,平均粒径为(136.89±4.23) nm,多分散指数(PDI)为0.289±0.005,Zeta电位为(-34.46±0.31) mV,包封率为(68.98±2.06)%,载药量为(1.90±0.06)%。结论 溶剂乳化超声法制备的B-NLC包封率高,粒径小,分布均匀,该方法操作简单方便,可以用于B-NLC制备与处方的优化,为马钱子碱的进一步体内研究奠定了基础。
[Key word]
[Abstract]
Objective To optimize the prescription and preparation technology of brucine nanostructured lipid carriers (B-NLC).Methods The method of "the solvent emulsification ultrasound" was used to prepare B-NLC. The prescription and preparation was optimized using a single factor method combined with central composite design-response surface methodology (CCD-RSM).Results The resultant B-NLC was transparent liquid with light blue opalescence. The optimal conditions were that the dosage of drugs was 1.28 mg, the mass concentration of poloxamer 188 was 1.08%, and the ratio of solid lipid to liquid lipid was 1.45:1. The obtained NLC showed the average particle size of (136.89 ±4.23) nm with a polydispersity index of 0.289 ±0.005 and a zeta potential of (-34.46 ±0.31) mV. The entrapment efficiency was calculated to be (68.98 ±2.06)%, and the drug loading content was (1.90 ±0.06)%.Conclusion B-NLC prepared by solvent emulsification ultrasound had a high entrapment efficiency and a narrow particle size distribution. The method was easy and simple and can be used to optimize the prescription and preparation of B-NLC, which provides a foundation for the further in vivo research of brucine.
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[基金项目]
黑龙江省自然科学基金面上项目(H2016076);黑龙江中医药中青年科技攻关项目(ZQG-039);黑龙江省教育厅科学技术研究项目(12531624);哈尔滨市应用技术研究与开发项目(青年后备人才A类)(2017RAQXJ090)