Notario-Pérez Fernando, Ruiz-Caro Roberto, Veiga-Ochoa María-Dolores
Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, Universidad Complutense de Madrid, Madrid, Spain.
Drug Des Devel Ther. 2017 Jun 15;11:1767-1787. doi: 10.2147/DDDT.S133170. eCollection 2017.
Infection with human immunodeficiency virus (HIV) remains a global public health concern and is particularly serious in low- and middle-income countries. Widespread sexual violence and poverty, among other factors, increase the risk of infection in women, while currently available prevention methods are outside the control of most. This has driven the study of vaginal microbicides to prevent sexual transmission of HIV from men to women in recent decades. The first microbicides evaluated were formulated as gels for daily use and contained different substances such as surfactants, acidifiers and monoclonal antibodies, which failed to demonstrate efficacy in clinical trials. A gel containing the reverse transcriptase inhibitor tenofovir showed protective efficacy in women. However, the lack of adherence by patients led to the search for dosage forms capable of releasing the active principle for longer periods, and hence to the emergence of the vaginal ring loaded with dapivirine, which requires a monthly application and is able to reduce the sexual transmission of HIV. The future of vaginal microbicides will feature the use of alternative dosage forms, nanosystems for drug release and probiotics, which have emerged as potential microbicides but are still in the early stages of development. Protecting women with vaginal microbicide formulations would, therefore, be a valuable tool for avoiding sexual transmission of HIV.
感染人类免疫缺陷病毒（HIV）仍然是一个全球公共卫生问题，在低收入和中等收入国家尤为严重。广泛存在的性暴力和贫困等因素增加了女性感染的风险，而目前可用的预防方法大多不在大多数人的控制范围内。这推动了近几十年来阴道杀微生物剂的研究，以预防HIV从男性向女性的性传播。最初评估的杀微生物剂被制成每日使用的凝胶剂，含有不同的物质，如表面活性剂、酸化剂和单克隆抗体，但在临床试验中未能证明其有效性。一种含有逆转录酶抑制剂替诺福韦的凝胶剂在女性中显示出保护效果。然而，患者缺乏依从性导致人们寻找能够更长时间释放活性成分的剂型，因此出现了负载达匹韦林的阴道环，它需要每月使用一次，能够减少HIV的性传播。阴道杀微生物剂的未来将采用替代剂型、用于药物释放的纳米系统和益生菌，这些已成为潜在的杀微生物剂，但仍处于开发的早期阶段。因此，用阴道杀微生物剂制剂保护女性将是避免HIV性传播的一个有价值的工具。
