复方莪术油脂质体的制备及质量评价

摘要

目的:制备复方莪术油脂质体(ZTOC-LPS)并对其质量进行评价.方法:以复方莪术油中莪术油(以吉马酮表征)和维A酸的包封率及载药量等为考察指标,筛选ZTOC-LPS的制备方法及处方中大豆卵磷脂(SPC)的加入量、脂质中SPC-胆固醇(CH)质量比、莪术油-脂质质量比、维A酸-脂质质量比、水浴温度;并对最优处方制备工艺所制脂质体进行质量评价和初步稳定性考察.结果:优选的制备方法为乙醇注入法;最优处方制备工艺为每1 mL脂质体中SPC4 mg、SPC-CH质量比3:1、莪术油-脂质质量比1:9、维A酸-脂质质量比1:70、水浴温度55 ℃.所制3批脂质体中莪术油和维A酸的平均包封率分别为(64.63±1. 00)％和(90. 33±0. 72)％, 载药量分别为(9. 09±0. 14)％和(1. 43±0. 02)％,粒径为(257. 41±7. 58) nm,Zeta电位为(-38. 77±0. 81) mV,多分散系数为0. 10±0. 04;离心加速试验结果显示脂质体具有良好的物理稳定性;脂质体样品在(4±2)℃条件下放置1个月时各项考察指标均未发生明显变化.结论:建立的制备方法简单可行,所制脂质体质量符合要求,可为后续复方莪术油新剂型的研究提供参考.%OBJECTIVE: To prepare zedoary turmeric oil compound liposomes (ZTOC-LPS) and evaluate its quality.METHODS: The preparation method of liposome, the addition amount of soybean phosphatidylcholine (SPC), ratio of SPC to cholesterol (CH) in lipid, drug-lipid ratio of zedoary turmeric oil (ZTO), drug-lipid ratio of tretinoin in formulation, and water bath temperature were screened using encapsulation efficiency and drug-loading amount of ZTO (represented by germacrone) and tretinoin as investigation indexes. Quality evaluation and primary stability investigation were conducted for liposomes prepared by optimal preparation technology. RESULTS: The optimal preparation method was ethanol injection method; The optimal preparation technology were SPC 4 mg in 1 mL lipid, the mass ratio of SPC to CH 3:1, the ratio of ZTO to lipid 1:9, the ratio of tretinoin to lipid 1:70, water bath temperature of 55 ℃. Encapsulation efficiencies of ZTO and tretinoin were (64. 63 ± 1. 00)％ and (90. 33 土 0. 72)％ in 3 batches of ZTOC-LPS, respectively. Drug-loading amount of ZTO and tretinoin were (9. 09 ± 0. 14)％ and (1. 43 ± 0. 02)％, respectively. Particle size was (257. 41 ± 7. 58) nm, Zeta potential was (-38. 77 ± 0. 81) mV,PDI was 0. 10 ± 0. 04; the results of centrifugal acceleration test showed that the liposomes had good physical stability. No obvious change was found in each investigation index of ZTOC-LPS that stored at (4 ± 2) ℃ for 1 month. CONCLUSIONS: Established preparation technology is simple and feasible, the quality of the prepared ZTOC-LPS conforms to the requirements, and it can provide reference for the following research of ZTOC-LPS.