title: Note on the formulation of thermosensitive and mucoadhesive vaginal hydrogels containing the miniCD4 M48U1 as anti-HIV-1 microbicide.
abstract: 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.
authors.affiliation: Université Paris-Sud, Institut Galien Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, 5, rue J.B. Clément, 92296 Châtenay-Malabry cedex, France. kawthar.bouchemal@u-psud.fr
authors.forename: Kawthar
authors.initials: K
authors.lastname: Bouchemal
authors.forename: Justyna
authors.initials: J
authors.lastname: Frelichowska
authors.forename: Loïc
authors.initials: L
authors.lastname: Martin
authors.forename: Vanessa
authors.initials: V
authors.lastname: Lievin-Le Moal
authors.forename: Roger
authors.initials: R
authors.lastname: Le Grand
authors.forename: Nathalie
authors.initials: N
authors.lastname: Dereuddre-Bosquet
authors.forename: Madeleine
authors.initials: M
authors.lastname: Djabourov
authors.forename: Armelle
authors.initials: A
authors.lastname: Aka-Any-Grah
authors.forename: Armand
authors.initials: A
authors.lastname: Koffi
authors.forename: Gilles
authors.initials: G
authors.lastname: Ponchel
mesh_terms: D000268:Adhesiveness; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000737:chemistry*; D015704:CD4 Antigens / Q000378:metabolism; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D005260:Female; D006367:HeLa Cells; D006358:Hot Temperature; D006801:Humans; D020100:Hydrogels; D065347:Hypromellose Derivatives; D066298:In Vitro Techniques; D008252:Macaca fascicularis; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009092:Mucous Membrane / Q000378:metabolism*; D010455:Peptides / Q000008:administration & dosage / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry; D014621:Vagina / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D015704:CD4 Antigens; D020100:Hydrogels; D010455:Peptides; D020442:Poloxamer; D065347:Hypromellose Derivatives; D008747:Methylcellulose
keywords: Anti-HIV-1 microbicides; M48U1; Pluronic(®); Release profiles; Toxicological evaluation