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PubMed · 11964907

Vaginal microbicides.

Sheena McCormack
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Abstract

The focus of this review will be to highlight articles from 2000 and up to August 2001 that demonstrate the challenges in the evaluation of candidate microbicides, and the ways in which investigators have approached these challenges.

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Administration, IntravaginalAnti-HIV AgentsAnti-Infective AgentsClinical Trials as TopicDrug Delivery SystemsFemaleHIV InfectionsHumansPatient ComplianceSexually Transmitted DiseasesJournal ArticleReview

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Sheena McCormack. 2002. Vaginal microbicides.. https://doi.org/10.1097/00001432-200202000-00010

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PubMed2007

Effect of oral administration of dydrogestrone versus vaginal administration of natural micronized progesterone on the secretory transformation of endometrium and luteal endocrine profile in patients with premature ovarian failure: a proof of concept.

BACKGROUND: We aimed to explore the endometrial histology and endocrine profiles on day 21 of an artificial cycle in patients with premature ovarian failure (POF) treated with oral dydrogesterone (DG) or vaginal micronized progesterone. METHODS: The study was designed as a prospective pilot study at an academic reproductive medicine unit. Six POF patients were included in the study. After estrogen endometrial priming, patients were randomized to receive DG or progesterone in two subsequent cycles. The main outcome measure was the endometrial histology and the endocrine profiles on day 21 of the cycle. RESULTS: Development of endometrial glands corresponded to an early secretory phase in five out of six cases supplemented with DG (out-phase). In contrast, five out of six cases treated with micronized progesterone showed an endometrium corresponding to a mid-luteal phase (in-phase) (P = 0.021 versus DG). There was a significant difference in the mean progesterone value [8.6 versus 0.3 microg l(-1) (P = 0.013)], the mean LH value [12.9 versus 22.5 IU l(-1) (P = 0.049)] and the mean FSH value [13.0 versus 23.9 IU l(-1) (P = 0.047)] between the progesterone and DG group, respectively, on day 21 of the cycle. CONCLUSIONS: After estrogen endometrial priming in POF patients, exogenous vaginal micronized progesterone is more effective than oral DG in creating an 'in-phase' secretory endometrium and induces significantly higher progesterone and lower LH and FSH serum concentrations on day 21 of the cycle.

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PubMed2007

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Microbicides are drug delivery systems (DDSs) for the prevention of sexual transmission of HIV and other STDs. A topically applied vaginal microbicidal gel should provide uniform coating of vaginal tissue, retention of this gel layer prior to intercourse, and controlled release kinetics of antivirals to inactivate the viral load potentially introduced during sexual activity. Here, we describe the microbicide-oriented characterization of a DDS made with a dual pH sensitive and thermosensitive smart polymer gel composed of a random terpolymer of N-isopropyl acrylamide, butyl methacrylate, and acrylic acid. The system was engineered to coat vaginal tissue with a stable gel layer and to release entrapped model agents in a burst release profile in response to the presence of the infecting agent: semen. The gel rheology, layer erosion properties, model drug release kinetics, and cytocompatibility of the terpolymer system were studied. Negligible erosion of the gel in the presence of vaginal fluid simulant suggests prolonged retention. Burst release of molecular and macromolecular model compounds was observed when the system's pH changed from the vaginal pH to the pH of semen, and cytotoxicity studies showed that the terpolymer is equally cytocompatible as a commonly used polymeric vaginal carrier.

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