摘要
目的 优化注射用七叶皂苷钠脂质体的制备工艺。方法 采用单因素考察法及Box-Behnken设计-响应曲面法,考察磷脂种类选择、药物与磷脂比例(W/W)、磷脂与胆固醇比例(W/W)、DSPE-mPEG2000用量、无水乙醇用量(W/V)、水相pH等因素对注射用七叶皂苷钠脂质体包封率的影响,优化其制备工艺,并通过透射电镜、粒径分布以及电位对脂质体进行质量评价。结果 药物在水合介质的质量浓度为2.5 mg·mL-1,磷脂选用EPCS,药物与磷脂比例为1∶20,磷脂与胆固醇比例为3∶1,DSPE-mPEG2000用量为0.1%、无水乙醇用量为15%(W/V),水相pH为3.5。制备得到的注射用七叶皂苷钠脂质体具有高包封率(99.33%),粒径均一为(107.33±0.84) nm,多分散系数(PDI)为(0.130±0.017);Zeta电位为(-30.34±0.23) mv。结论 优化筛选的脂质体制备工艺简便、包封率高、稳定性好,适用于注射用七叶皂苷钠脂质体的制备。
OBJECTIVE To optimize the technology preparation of sodium aesculin liposome for injection.METHODS Firstly,a single factor test was used to investigate the influence of the formulation process on the preparation of liposomes with the encapsulation efficiency and particle size as evaluation indicators.The effects of phospholipid type selection,ratio of drugs to phospholipids(W/W),ratio of phospholipids to cholesterol(W/W),dosage of DSPE-mPEG2000,dosage of anhydrous ethanol(W/V)and aqueous pH on the encapsulation rate of sodium aesculin liposome for injection were investigated.Finally,the Box-Behnken effect surface method was used to further optimize the prescription process.RESULTS The mass concentration of the drug in the hydration medium was 2.5 mg·mL-1,the phospholipid was selected as EPCS,the ratio of drug to phospholipid was 1∶20,the ratio of phospholipid to cholesterol was 3∶1,the dosage of DSPE-mPEG2000 was 0.1%,the amount of anhydrous ethanol was 15%(W/V),and the aqueous pH was 3.5.The liposome of sodium aescinate(SA-Lip)were successfully prepared,with an encapsulation efficiency of 99.33%;The particle size was(107.33±0.84)nm,polydispersity index(PDI)was(0.130±0.017),Zeta potential was(-30.34±0.23)mV.CONCLUSION The optimized liposome has simple preparation process,high encapsulation rate and good stability,and is suitable for the preparation of sodium aescinate for injection.
作者
蔡晓惠
刘梦梦
陈行
许幼发
陈玉燕
CAI Xiao-hui;LIU Meng-meng;CHEN Hang;XU You-fa;CHEN Yu-yan(Zhangzhou Hospital of Traditional Chinese Medicine,Zhangzhou 363000,China;Shanghai Wei Er Lab,Shanghai 201712,China)
出处
《海峡药学》
2023年第8期4-10,共7页
Strait Pharmaceutical Journal
基金
福建中医药大学高层次人才科研启动资金项目(X2019006-人才)
上海青浦区产学研合作发展资金项目资助(青产学研2021-7)。
