An update on vaginal microbicides

Abstract

In response to an increasing prevalence of sexually transmitted diseases, especially AIDS, efforts to prevent further infections have been heightened. One of those approaches has been the development of topical microbicidal agents or microbicides. These are compounds designed to protect the body's mucosal surfaces from infection by sexually transmitted disease-causing pathogens. Numerous candidates are currently in preclinical stages; however, only a handful have been tested for safety, and even fewer are ready for clinical efficacy trials. In this update, we describe some of the specific features of microbicide research and development, including preclinical screening algorithms, candidate's ideal properties, examples of compounds presently in the pipeline, and future prospects.

Sophorolipids, Microbial Glycolipids with Anti-Human Immunodeficiency Virus and Sperm-Immobilizing Activities

“…Sophorolipids appear to act as membrane-perturbing agents. Other membrane-perturbing agents have been shown to display spermicidal and virucidal properties (18). The membrane partitioning of these compounds is critically involved in their microbicidal activity.…”

Porphyrin-based compounds exert antibacterial action against the sexually transmitted pathogens Neisseria gonorrhoeae and Haemophilus ducreyi

“…The continued world wide problem of STI and the lack of effective vaccines to block most bacterial, protozoal and viral STI [12] have prompted an interest in developing safe, effective topical microbicides [1,28]. In this respect, the most significant attention has been on compounds that block human immunodeficiency virus infection (HIV) and transmission [12].…”

“…The development and use of topical microbicides represents one such strategy. Topical microbicides are compounds designed to protect mucosal surfaces from infection by STI pathogens [1]. These agents could be employed by women to protect themselves from STI, providing them independence of the largely male partner's choice of condom usage.…”

Vaginal microbicides: A novel approach to preventing sexual transmission of HIV

“…Detailed recommendations for the conduct of preclinical studies have been written by the International Working Group on Microbicides and will be published in 2004. Figure 1 shows the screening algorithm used by the Global Microbicide Project (GMP) of CONRAD [60]. Briefly, a microbicidal agent needs to demonstrate potent activity against HIV and, preferably, other STPs, such as herpes virus and Chlamydia and Neisseria organisms, and prove that it is safe for topical use, displaying no mucosal irritation or inflammatory properties.…”