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Microbicide testing

724

DEVELOPMENT OF A COMBINATION MICROBICIDE GEL FORMULATION CONTAINING IQP-0528 AND TENOFOVIR FOR THE PREVENTION OF HIV INFECTION.

In light of the increasing worldwide AIDS pandemic, there is a continuing need to develop new prevention strategies to inhibit the transmission of HIV-1. In the absence of a successful vaccine, topical microbicides represent the best strategies to reduce the epidemic. Following the success of HIV therapeutic cocktail strategies, combinations of microbicides including nucleotide reverse […]
766

ENGINEERING A DEGRADABLE POLYURETHANE INTRAVAGINAL RING FOR SUSTAINED DELIVERY OF DAPIVIRINE

We describe the engineering of a degradable intravaginal ring (IVR) for the delivery of the potent HIV-1 reverse transcriptase inhibitor dapivirine. The degradable polymer used in fabricating the device incorporated poly(caprolactone) ester blocks in a poly(tetramethylene ether) glycol ABA type polyurethane backbone. The polymer was designed to maintain its structure for 1 month during usage and […]
712

PRECLINICAL EVALUATION OF ANTI-HIV MICROBICIDE PRODUCTS: NEW MODELS AND BIOMARKERS.

A safe and effective microbicide product designed to prevent sexual transmission of HIV-1 rests on a solid foundation provided by the proper selection and preclinical characterization of both its active pharmaceutical ingredient (API) and formulation. The evaluation of API and formulation physicochemical properties, drug release, specific antiviral activity, cell and tissue toxicity, organ toxicity, pharmacokinetics, […]
710

VAGINAL MICROBICIDE GEL FOR DELIVERY OF IQP-0528, A PYRIMIDINEDIONE ANALOG WITH A DUAL MECHANISM OF ACTION AGAINST HIV-1.

Pyrimidinediones, a novel class of compounds, have previously been shown to possess antiviral activity at nanomolar concentrations. One member of this class of compounds, IQP-0528, was selected as the lead molecule for formulation development owing to its stability at physiologically relevant conditions, wide therapeutic window, and antiviral activity in the nanomolar range. Here, we report […]
665

PRECLINICAL EVALUATION OF UC781 MICROBICIDE VAGINAL DRUG DELIVERY.

UC781 is a potent nonnucleoside reverse transcriptase inhibitor being investigated as a potential microbicide to prevent transmission of HIV-1 both vaginally and rectally. This study was designed to investigate the in vitro drug release, in vitro permeability/safety, and in vivo pharmacokinetics in rabbits of a vaginal gel prepared with micronized or nonmicronized UC781 (UC781m and […]