A review of the recent outcomes regarding technologies to prevent vaginal transmission of HIV, mainly by using antiretroviral (ARV) drugs formulated as microbicides. An introduction about the HIV transmission mechanisms by the vaginal route is included, together with the recent challenges faced for development of successful microbicide products. The outcomes of clinical evaluations are mentioned, and the different formulation strategies studied to-date, with the requirements, advantages, disadvantages and limitations of each dosage-form type, are presented. Finally, the recent attempts to apply various types of nanotechnologies in order to develop advanced microbicide-products and overcome existing limitations, are discussed.