Title: Development and characterization of a solid dispersion film for the vaginal application of the anti-HIV microbicide UAMC01398
Authors: Grammen, Carolien ×
Van den Mooter, Guy
Appeltans, Bernard
Michiels, Johan
Crucitti, Tania
Ariën, Kevin K
Augustyns, Koen
Augustijns, Patrick
Brouwers, Joachim #
Issue Date: Nov-2014
Publisher: Elsevier/North Holland
Series Title: International Journal of Pharmaceutics vol:475 issue:1-2 pages:238-44
Abstract: The purpose of this work was to design and evaluate a vaginal film delivery system for UAMC01398, a novel non-nucleoside reverse transcriptase inhibitor currently under investigation for use as an anti-HIV microbicide. UAMC01398 (1mg) films consisting of hydroxypropylmethylcellulose (HPMC) and polyethylene glycol 400 (PEG400) in different ratios were prepared by solvent evaporation. Based on its flexibility, softness and translucent appearance, the 30% PEG400 and 70% HPMC containing film was selected for further assessment. The vaginal film formulation was fast-dissolving (<10 min in 1 mL of vaginal fluid simulant), stable up to at least one month and safe toward epithelial cells and lactobacilli. Furthermore, formulating UAMC01398 into the film dosage form did not influence its antiviral activity. Powder X-ray diffraction revealed the amorphous nature of the UAMC01398 film, resulting in enhanced compound permeation across the epithelial HEC-1A cell layer, presumably owing to the induction of supersaturation. The in vivo vaginal tissue uptake of UAMC01398 in rabbits, as measured by systemic concentrations, was increased compared to the previously established non-solubilizing gel (significant difference) and sulfobutyl ether-β-cyclodextrin (5%) containing gel. To conclude, we identified a film formulation suitable for the vaginal delivery of UAMC01398.
ISSN: 0378-5173
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Departement Industriƫle Wetenschappen en Technologie - UC Limburg
Drug Delivery and Disposition
× corresponding author
# (joint) last author

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