International Journal of Pharmaceutics 2013-10-01

Note on the formulation of thermosensitive and mucoadhesive vaginal hydrogels containing the miniCD4 M48U1 as anti-HIV-1 microbicide.

Kawthar Bouchemal, Justyna Frelichowska, Loïc Martin, Vanessa Lievin-Le Moal, Roger Le Grand, Nathalie Dereuddre-Bosquet, Madeleine Djabourov, Armelle Aka-Any-Grah, Armand Koffi, Gilles Ponchel

文献索引：Int. J. Pharm. 454(2) , 649-52, (2013)

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摘要

The miniCD4 M48U1 was formulated into thermosensitive and mucoadhesive pluronic(®) hydrogels as anti-HIV-1 microbicide. The release kinetics of M48U1 from F127/HPMC (20/1 wt%) and F127/F68/HPMC (22.5/2.5/1 wt%) studied during 24h by using Franz diffusion cells showed that HEC hydrogel (1.5 wt%) used as control released 93% of the peptide, while about 25% of M48U1 remained in pluronic(®) hydrogels. The formulation of M48U1 in pluronic(®) hydrogels ensures a local delivery because no diffusion of the peptide was detected through vaginal Cynomolgus macaque mucosa using Ussing chamber. Finally, toxicological studies showed no significant difference in the HeLa cell viability of the pluronic(®) hydrogels in comparison with HEC and phosphate buffer saline.Copyright © 2013 Elsevier B.V. All rights reserved.