【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 m L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)m V,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。更多还原

【Abstract】 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 m L 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)m V,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.更多还原