
马纳维诺凝胶作为候选杀微生物剂的生物学活性和稳定性体外评价
Efficacy and stability of maraviroc gel as a microbicide candidate in vitro
为在体外评价马纳维诺凝胶的生物学活性和稳定性,用TZM-bl和Jurkat-T细胞系对马纳维诺与0.015%羟乙基纤维素(HEC)复合而成的凝胶制剂进行细胞毒性检测,评价其抑制人类免疫缺陷病毒(HIV)SVPB16和SVPC12亚型假病毒感染的活性,并与溶于磷酸盐缓冲液(PBS)的对照组作比较。将马纳维诺溶于1.5% HEC中,终浓度为6 mmol/L,分别置于4 ℃、室温、30 ℃和40 ℃,保持相对湿度75%,每隔1周检测其抗病毒活性。结果显示,当马纳维诺与HEC复合后,其细胞毒性并没有增加,而抗病毒活性轻微增强。马纳维诺凝胶置于4个温度,持续8周,即使是在高于人体温度的40 ℃,仍保持较好的抗病毒活性。综上所述,作为候选杀微生物剂,马纳维诺凝胶具有较好的生物学活性和稳定性。
To study the efficacy and stability of maraviroc gel in vitro, the cytotoxicity of maraviroc in phosphate buffered saline (PBS) or in 0.015% hydroxyethyl cellulose (HEC) were evaluated in TZM-bl and Jurkat-T cells. Meanwhile, two subtypes of human immunodeficiency virus (HIV) pseudovirus (SVPB16 and SVPC12) were used to evaluate the anti-HIV activity in vitro, the half maximal inhibitory concentration (IC50) or 90% maximal inhibitory concentration (IC90) of maraviroc gel were assessed. Furthermore, maraviroc was dissolved in 1.5% HEC with a final concentration of 6 mmol/L, and then maraviroc gel was stored at 4 ℃, room temperature, 30 ℃ and 40 ℃, respectively, in 75% relative humidity for 1 to 8 weeks. The anti-HIV activity was tested weekly. The data showed that maraviroc gel had nearly same cytotoxicity as maraviroc in PBS. HEC did not weaken the ant-HIV activity of maraviroc. Inversely, HEC might slightly enhance the anti-HIV efficacy of maraviroc. Maraviroc gel was stable for at least 8 weeks even at 40 ℃. It is concluded that maraviroc gel has good efficacy and stability as a microbicide candidate.
马纳维诺 / 羟乙基纤维素 / 人类免疫缺陷病毒 / 杀微生物剂
Maraviroc / Hydroxyethyl cellulose / Human immunodeficiency virus / Microbicide
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