阿昔洛韦脂质体的制备及其体外抗乙肝病毒的研究

Study on preparation of acydovir liposomes and its role in inhibiting hepatitics B in vitro

目的制备阿昔洛韦脂质体并进行体外抗乙肝病毒作用研究。方法以反相蒸发法制备阿昔洛韦脂质体,同时考察其包封率的影响因素。以HPLC测定阿昔洛韦含量,透射电镜观察其形态,激光散射法测定其粒径大小,HepG2 2.2.15细胞模型检测阿昔洛韦脂质体对乙肝病毒HBs Ag和HBe Ag的抑制率。结果反相蒸发法中4℃时的包封率高于37℃时的包封率; 在本实验的PBS缓冲液离子强度范围内,随着离子强度升高,阿昔洛韦脂质体的包封率降低。脂质体中阿昔洛韦质量浓度为10.0,20.0,40.0,80.0 mg·L-1时对HBs Ag和HBe Ag的抑制率分别达到(7.5±1.2)%,(18.2±2.1)%,(52.6±2.7)%,(60.3±1.9)%和(8.3±0.8)%,(40.5±3.2)%,(47.4±1.2)%,(50.4±0.6)%。结论反相蒸发法可以制备阿昔洛韦脂质体;阿昔洛韦脂质体时HBs Ag和HBeAg有较好的抑制作用且明显优于游离阿昔洛韦。

OBJECTIVE To prepare acyclovir hposomes and study its ability to inhibit hepatitis B virus HBs Ag and HBe Ag. METHODS Acyclovir liposomes were prepared by reverse phase evaporation. Acyclovir was determined by HPLC and its partical size was determined by laser light scattering instrument. Transmission electron microscopy （TEM） was used to examine the morphology of liposomes. Its ability to inhibit hepatitis B virus HBs Ag and HBe Ag in vitro was studied by a HBV-transfectted cell line （ HepC2 2.2.15）. RESULTS The encapsulation efficiency of liposomes prepared at 4℃was higher than that at 37 ℃. With the increase of PBS buffer ion strength, the encapsulation efficiency of liposomes decreased. The acyclovir concentrations of liposomes that inhibited HBs Ag in vitro by （7.5± 1.2） %, （ 18.2±2.1）% ,（52.6±2.7）%,（60.5±1.9）% and HBe Ag in vitro by （8.3±0.8）% ,（40.5±3.2）% ,（47.4±1.2）% ,（50.4±0.6）% were 10.0,20.0,40.0,80.0mg·L^-1. CONCLUSION Acyclovir liposomes are prepared by reverse phase evaporation, whose ability to inhibit hepatitis B virus HBs Ag and HBe Ag in vitro is better than acyclovir.