Efficacy of HIV antiviral polyanionic carbosilane dendrimer G2-S16 in the presence of semen

• Published in: International journal of nanomedicine Vol. 11; no. default; pp. 2443 - 2450
• Main Authors: Ceña-Diez, Rafael, García-Broncano, Pilar, de la Mata, Francisco Javier, Gómez, Rafael, Muñoz-Fernández, M Ángeles
• Format: Journal Article
• Language: English
• Published: New Zealand Dove Medical Press Limited 01-01-2016; Taylor & Francis Ltd; Dove Medical Press
• Subjects: Acquired immune deficiency syndrome; Administration, Topical; AIDS; Alkanesulfonates - pharmacology; Anti-HIV Agents - administration & dosage; Anti-HIV Agents - pharmacology; Antiretroviral agents; Antiretroviral drugs; antiretrovirals; CD4 Antigens - metabolism; Cells, Cultured; Clinical trials; dendrimer; Dendrimers; Dendrimers - pharmacology; G2-S16; Health aspects; HIV; HIV Envelope Protein gp120 - metabolism; HIV infections; HIV Infections - prevention & control; HIV-1; HIV-1 - pathogenicity; Human immunodeficiency virus; Human immunodeficiency virus 1; Humans; Infection; Infections; Leukocytes, Mononuclear - drug effects; Leukocytes, Mononuclear - virology; Lysine; Male; microbicide; Organosilicon Compounds - pharmacology; Original Research; Prevention; Receptors, CCR5 - metabolism; Semen - drug effects; Semen - virology; SEVI; Statistical analysis; Surface active agents; Viral infections; Virus replication; Virus Replication - drug effects; United States > US; Spain; HIV-1; G2-S16; SEVI; microbicide; antiretrovirals; dendrimer
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S104292

The development of a safe and effective microbicide to prevent the sexual transmission of human immunodeficiency virus (HIV)-1 is urgently needed. Unfortunately, the majority of microbicides, such as poly(L-lysine)-dendrimers, anionic polymers, or antiretrovirals, have proved inactive or even increased the risk of HIV infection in clinical trials, most probably due to the fact that these compounds failed to prevent semen-exposed HIV infection. We showed that G2-S16 dendrimer exerts anti-HIV-1 activity at an early stage of viral replication, blocking the gp120/CD4/CCR5 interaction and providing a barrier to infection for long periods, confirming its multifactorial and nonspecific ability. Previously, we demonstrated that topical administration of G2-S16 prevents HIV transmission in humanized BLT mice without irritation or vaginal lesions. Here, we demonstrated that G2-S16 is active against mock- and semen-exposed HIV-1 and could be a promising microbicide against HIV infection.