盐酸吉西他滨隐形脂质体的制备及工艺优化

发布时间：2018-04-25 23:07

本文选题：盐酸吉西他滨 + 隐形脂质体　；参考：《中国抗生素杂志》2017年05期

【摘要】：目的应用响应面分析法优化盐酸吉西他滨隐形脂质体的制备条件。方法结合改良薄膜法和冻融法制备盐酸吉西他滨隐形脂质体,利用Plackett-Burman实验设计法确定显著影响药物包封率的因素,即脂药比(W/W),HSPC/DSPE-PEG2k(W/W),脂质比(W/W),并对其进行3因素5水平的中心组合实验,筛选最佳处方工艺,并绘制体外释药曲线。结果最优处方工艺条件为磷脂:药物:胆固醇:DSPE-PEG2k为60:3:20:4.8(W/W),PBS浓度0.1mmol/L,水化时间1h,探头超声时间3min(80W,3s/3s),冻融4次;在此优化条件下,包封率为65.85%±0.48%,较优化前提高近25%。体外释放动力学符合双指数方程,具有一定缓释作用。结论响应面分析法可有效平衡各因素之间的相互影响,适用于脂质体制备工艺及处方筛选。
[Abstract]:Objective to optimize the preparation conditions of gemcitabine hydrochloride stealth liposomes by response surface analysis. Methods Gemcitabine hydrochloride stealth liposomes were prepared by the combination of modified membrane method and freeze-thaw method. The factors that significantly affected the encapsulation efficiency of gemcitabine hydrochloride were determined by Plackett-Burman experimental design. In other words, the ratio of lipids to lipids was compared with that of HSPC / DSPE-PEG2kW / WN, and the ratio of lipids to lipids was W / WN, and a central combination experiment of 3 factors and 5 levels was carried out to screen the best prescription technology and draw the in vitro release curve. Results the optimum prescription conditions were as follows: cholesterol: DSPE-PEG2k: 60: 3: 20: 4.8W / W PBS 0.1 mmol / L, hydration time 1 h, probe ultrasonic time 3 min ~ (80) W ~ (3) s / 3 s ~ (-1), freeze-thaw 4 times, and the encapsulation efficiency was 65.85% 卤0.48%, which was about 25.5% higher than that before optimization. The kinetics of release in vitro accords with the double exponential equation and has a certain sustained release effect. Conclusion response surface analysis can effectively balance the interaction of various factors and is suitable for the preparation of liposomes and the screening of their prescriptions.
【作者单位】：抗生素研究与再评价四川省重点实验室四川抗菌素工业研究所成都大学;
【分类号】：R943

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