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Historical development of vaginal microbicides to prevent sexual transmission of HIV in women: from past failures to future hopes

Authors Notario-Pérez F, Ruiz-Caro R, Veiga-Ochoa MD

Received 25 January 2017

Accepted for publication 13 April 2017

Published 15 June 2017 Volume 2017:11 Pages 1767—1787

DOI https://doi.org/10.2147/DDDT.S133170

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Rasika Samarasinghe

Peer reviewer comments 2

Editor who approved publication: Professor Manfred Ogris

Fernando Notario-Pérez, Roberto Ruiz-Caro, María-Dolores Veiga-Ochoa

Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, Universidad Complutense de Madrid, Madrid, Spain

Abstract: 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.

Keywords: vaginal formulations, microbicides, prevention, sexual transmission, acquired immunodeficiency syndrome (AIDS), human immunodeficiency virus (HIV)

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