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

被引：17

作者：

Bouchemal, Kawthar ^{[1
]}

Frelichowska, Justyna ^{[1
]}

Martin, Loic ^{[2
]}

Lievin-Le Moal, Vanessa ^{[3
]}

Le Grand, Roger ^{[4
]}

Dereuddre-Bosquet, Nathalie ^{[4
]}

Djabourov, Madeleine ^{[5
]}

Aka-Any-Grah, Armelle ^{[1
,6
]}

Koffi, Armand ^{[6
]}

Ponchel, Gilles ^{[1
]}

机构：

[1] Univ Paris 11, Fac Pharm, CNRS, UMR 8612,Inst Galien Paris Sud, F-92296 Chatenay Malabry, France

[2] CEA, IBiTecS, Serv Ingn Mol Prot SIMOPRO, F-91191 Gif Sur Yvette, France

[3] Univ Paris 11, Fac Pharm, Grp Chimiotherapie Antiparasitaire, UMR CNRS Biomol Concept Isolement Synth 8076, F-92296 Chatenay Malabry, France

[4] CEA, IMETI, Div Immunovirol, Fontenay Aux Roses, France

[5] ESPCI Paris Tech, Lab Phys Therm, F-75231 Paris 05, France

[6] UFR Sci Pharmaceut & Biol Abidjan, Lab Pharmacol & Pharmacocinet, Telex 26138, Cote Ivoire

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2013年 / 454卷 / 02期

关键词：

Pluronic (R); Anti-HIV-1; microbicides; M48U1; Toxicological evaluation; Release profiles; ENVELOPE;

D O I：

10.1016/j.ijpharm.2013.02.055

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The miniCD4 M48U1 was formulated into thermosensitive and mucoadhesive pluronic (R) 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 24 h 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 (R) hydrogels. The formulation of M48U1 in pluronic (R) 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 (R) hydrogels in comparison with HEC and phosphate buffer saline. (C) 2013 Elsevier B. V. All rights reserved.

引用

页码：649 / 652

页数：4

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