利福平纳米脂质载体的制备及质量评价

发布时间：2018-04-24 12:50

本文选题：利福平 + 纳米脂质载体　；参考：《中国药房》2017年34期

【摘要】：目的:制备利福平(RFP)纳米脂质载体(RFP-NLCs),提高其水溶性,并评价其质量。方法:以液固脂质材料油酸及单硬脂酸甘油酯为脂质材料,大豆卵磷脂为乳化剂,泊洛沙姆188为非离子型表面活性剂,采用熔融-超声乳化法制备RFP-NLCs。以粒径和包封率的综合评分为指标,以脂质材料的用量、液态脂质材料比例、投药量和大豆卵磷脂-泊洛沙姆188质量比为因素,采用正交试验优化处方。测定最优处方所制脂质载体的形态、粒径、多分散指数(PDI)、Zeta电位、包封率、载药量和体外释放度。结果:最优处方中脂质材料用量为150 mg,液态脂质比例为30%,RFP用量为10 mg,大豆卵磷脂-泊洛沙姆188的质量比为1:3。所制RFP-NLCs的外观较圆整,粒径为(124.07±3.25)nm,PDI为0.104±0.010,Zeta电位为(-31.07±2.94)mV,包封率为(80.90±2.59)%,载药量为(4.81±0.68)%(n=3)。与RFP原料药比较,RFP-NLCs体外释放度明显减缓,12 h内的累积释放度为63.2%,释药行为符合Weibull方程。结论:筛选处方可成功制备RFP-NLCs;所制RFP-NLCs粒径小、包封率较高,具有体外缓释特征。
[Abstract]:Aim: to prepare rifampicin RFP (RFP) nanometer lipid carrier RFP-NLCsN, improve its water solubility and evaluate its quality. Methods: RFP-NLCswere prepared by melt-phacoemulsification using liquid-solid lipids such as oleic acid and glycerol monostearate as lipid materials, soybean lecithin as emulsifier and Poloxamer 188 as non-ionic surfactant. Based on the comprehensive score of particle size and encapsulation efficiency, the dosage of lipid material, the proportion of liquid lipid material, the dosage of soybean lecithin to Poloxamer 188 as factors, orthogonal test was used to optimize the formulation. The morphology, particle size, polydispersity index (PDI), Zeta potential, encapsulation efficiency, drug loading capacity and in vitro release of the lipids prepared by the optimal formulation were determined. Results: the dosage of lipid material was 150 mg, the ratio of liquid lipid to liquid lipid was 30 mg and the dosage of RFP was 10 mg. The mass ratio of soybean lecithin to Poloxamer 188 was 1: 3. The diameter of the RFP-NLCs was 124.07 卤3.25nmPDI, the Zeta potential was -31.07 卤2.94mV, the entrapment efficiency was 80.90 卤2.59mV, and the drug loading was 4.81 卤0.68nmV.The results showed that the diameter of the RFP-NLCs was 124.07 卤3.25nmPDI = 0.104 卤0.010nmV, the entrapment efficiency was 80.90 卤2.59mV, and the drug loading was 4.81 卤0.68nmV. Compared with RFP, the in vitro release rate of RFP-NLCs was significantly decreased by 63.2%, and the drug release behavior was in accordance with Weibull equation. Conclusion: RFP-NLCs can be successfully prepared by screening the formulation, and the prepared RFP-NLCs has the characteristics of small particle size, high entrapment efficiency and in vitro sustained release.
【作者单位】：宁波大学医学院附属医院药剂科;
【分类号】：R943

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