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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SPC 4 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±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.
莪术油维A酸脂质体包封率载药量制备工艺质量评价
Zedoary turmeric oilTretinoinliposomesEncapsulation efficiencyDrug-loading amountPreparation technologyQuality evaluation
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