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脂质体载水溶性药物出现的共同问题是药物的包封量低、稳定性差。本文以甲硝唑(Ⅰ)为水溶性药物模型,进行疏水性结构修饰,得其肉豆蔻酸酯(Ⅱ)前体药物,分别进行Ⅰ和Ⅱ的脂质体研究,结果表明Ⅱ在脂质体中的包封率较Ⅰ提高10倍以上,渗漏速率降至十分之一,制成含Ⅱ的脂质干膜,经超声分散,可得合乎要求的重组型脂质体,为解决脂质体载药的稳定性问题提供有效途径。体外抗阿米巴原虫试验,镜检观察到载药脂质体进入阿米巴原虫的细胞内,且100%抑制原虫所需剂量Ⅱ脂质体是Ⅰ游离药的二分之一。因此药物疏水化修饰是解决脂质体载水溶性药物稳定性问题的理想途径。
The common problem that liposomes contain in water-soluble drugs is their low encapsulation and poor stability. In this paper, Imidazole (I) as a water-soluble drug model, hydrophobic structure modification, its myristate (Ⅱ) prodrugs, respectively, Ⅰ and Ⅱ liposomes, the results show that Ⅱ in lipid The entrapment efficiency of the body is more than 10 times higher than that of I, and the leakage rate is reduced to one tenth. Lipid dry membrane containing II is prepared and dispersed by ultrasound to obtain the desired recombinant liposome. In order to solve the problem Liposome drug stability problems provide an effective way. In vitro anti-amoeba test, microscopic examination of the drug-loaded liposomes was found in the cells of the amoebae, and the dose required for 100% inhibition of the protozoal II liposomes was one-half that of the free drug. Therefore, drug hydrophobic modification is an ideal way to solve the stability problem of liposome-loaded water-soluble drugs.