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New vaginal gel formulation promising for HIV-1 prevention
Kiser P. Antimicrob Agents Chemother. 2011.doi:10.1128/AAC.01368-10.
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A new vaginal microbicide gel and drug formulation may offer an inexpensive, stable and effective prevention measure for heterosexual transmission of HIV-1, according to new findings published in Antimicrobial Agents and Chemotherapy.
“The pyrimidine dione class of HIV-1 reverse transcriptase inhibitors is a promising category of compounds that can be used in gel formulations,” Patrick F. Kiser, MD, associate professor in the department of bioengineering at the University of Utah, told Infectious Disease News.
According to background information in the study, the pyrimidinediones class of compounds has previously shown to have antiviral activity in the nanomolar range. For this reason, Kiser and colleagues set out to assess nine analogs of the pyrimidinediones class with the use of virological, chemical and physical assays.
The researchers selected the pyrimidinediones molecule that demonstrated the best antiviral activity and good physical and chemical stability (IQP-0528, ImQuest BioSciences, Inc.) in reconstructed VEC-100 tissue and human polarized ectocervical tissue. Toxicity and microbicide formulations were also assessed for genital tissue irritation. “No significant loss in cell viability or significant inflammatory response was found during in vitro and ex vivo safety evaluations,” the researchers reported.
The formulation of the combination drug (0.25% IQP-0528 and 3% hydroxyethyl cellulose (HEC) vaginal gel) was highly active against HIV-1 in human tissue. Results from the in vitro HIV-1 inhibition assay indicated that the 3% HEC gel formulation had a 50% effective concentration of 0.14 mcg/mL for gel in culture media. The formulation also showed complete protection against HIV infection when polarized cervical explants were used.
Estimated cost of the gel would be 30 cents per dose, according to the researchers.
“Based on our in vitro and ex vivo evaluations, we conclude that our gels provide diffusion-controlled release of the active ingredient. In addition, this formulation is expected to provide complete protection against infection with no significant toxicity or irritation to vaginal tissue,” the researchers wrote. “These results are encouraging and warrant further evaluation IQP-0528 gel formulations in in vivo models, as well as the development of alternative formulations for the delivery of IQP-0528 as a microbicide.”
Disclosure: Dr. Kiser reports no relevant financial disclosures.
This reflects a heightened need to explore as many options as possible to allow women means of protecting themselves from HIV, particularly after the recent failure of oral antiretroviral pre-exposure prophylaxis in the FEM-PrEP trial.
– Paul A. Volberding, MD
Infectious Disease News Editorial Board member
Disclosure: Dr. Volberding reports no relevant financial disclosures.
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