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本文通过将无环鸟苷(acyclovir,简称ACV)2’位羟基分别与月桂酰氯或棕榈酰氯进行酯化反应,制得亲脂性前体药物无环鸟苷月桂酸酯和无环鸟苷棕榈酸酯(分别简称为C_(12)-ACV和C_(16)-ACV),使脂质体包封率从ACV的29.9％提高到C_(12)-ACV的95.6％和C_(16)-ACV的97.1％;漏泄实验表明在4℃透析60h后,一半以上的ACV从脂质体中漏泄,而C_(12)-ACV和C_(16)-ACV的滞留率分别为70％和80％;体外抗疱疹病毒的试验中,在最低试验浓度0.044μmol/L时,ACV不显示抗病毒活性,而C_(16)-ACV脂质体抑制细胞病变率达75％,说明前体药物通过与脂质体脂膜的结合增加了药物的进入细胞能力,从而提高了ACV的抗病毒能力。
In this paper, acyclovir acyclovir (acvclovir acyclovir, referred to as 2’-hydroxy) with lauric acid chloride or palmitic acid chloride esterification reaction to obtain the lipophilic prodrug acyclovir laurate and acyclovir palmitic acid (C_ (12) -ACV and C_ (16) -ACV, respectively) increased the encapsulation efficiency of liposomes from 29.9% of ACV to 95.6% of C_ (12) -ACV and C_ (16) The leakage test showed that more than half of the ACV leaked from the liposomes after 60 h of dialysis at 4 ℃, while the retention rates of C_ (12) -ACV and C_ (16) -ACV were 70% and 80%, respectively. In vitro anti-herpes virus test, ACV did not show antiviral activity at the lowest test concentration of 0.044μmol / L, whereas C_ (16) -ACV liposomes inhibited the rate of cytopathic effect by 75% The combination of plastid lipid membranes increases the ability of the drug to enter the cell, thereby increasing the antiviral ability of ACV.