载紫杉醇脂质微泡的改良制备研究

Optimization in preparation of paclitaxel-loaded lipid microbubbles

目的探讨加入三醋酸甘油酯改良制备载紫杉醇脂质微泡的可行性,及其对载药微泡质量、载药量、包封率的影响。方法采用冷冻干燥法制备携带紫杉醇的脂质微泡,分别于制备过程中加入或不加入三醋酸甘油酯,测定载药微泡的包封率、载药量、粒径大小、分布和Zeta电位、pH值。结果改良法(加入三醋酸甘油酯)制备的载紫杉醇脂质微泡与常规冻干法制备的载药微泡相比较,微泡粒径显著减小,二者的平均粒径分别是(1.1±0.4)μm和(2.8±0.4)μm,P<0.01;其表面电位显著增高(19.1±0.3)mV和(-5.9±0.2)mV,P<0.01;包封率和载药量显著增高,包封率分别为(95.0±1.2)%和(36.1±4.7)%,载药量为(5.60±0.10)%和(0.50±0.04)%,P<0.01。结论制备过程中加入三醋酸甘油酯可显著提高载药微泡的包封率和载药量。

Objective To optimize the preparation of paclitaxel- loaded lipid microbubbles （PLMs） by adding triacetin, and to assess the related quality, encapsulation and drug- loading ratio of PLMs. Methods PLMs were prepared by lyophilization with or without triacetin. Then microbubble size, distribution, surface potential, pH value were measured. The encapsulation and drug- loading ratio of microbubbles were detected with reversed phase high - performance liquid chromatography （ RP - HPLC）. Results Compared to the PLMs prepared without triacetin, PLMs using triacetin were featured with a significantly smaller mean diameter were [ （ 1.1 ± 0.4） tan and （2.8 ± 0.4） μm, P 〈 0.01 ], the higher surface potential were [ （ 19.1± 0.3） mV and （ - 5.9 ± 0.2） mV, P 〈 0.01 ], markedly increased encapsulation were [ （ 95± 1.2） % and （ 36.1± 4.7） %, P 〈 0.01 ] and drug - loading ratio were [（5.60±0.10）% and（0.50±0.04）%, P〈0.01]. Conclusion By addingtriacetin in the preparation of PLMs, it can significantly increase the drug encapsulation and loading capabihty of microbubbles.