Université Paris-Sud, Institut Galien Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, 5, rue J.B. Clément, 92296 Châtenay-Malabry cedex, France.
Int J Pharm. 2013 Oct 1;454(2):649-52. doi: 10.1016/j.ijpharm.2013.02.055. Epub 2013 Mar 7.
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.
miniCD4 M48U1 被制成热敏和黏膜黏附性的泊洛沙姆（®）水凝胶，作为抗 HIV-1 杀微生物剂。通过 Franz 扩散池在 24 小时内研究 F127/HPMC（20/1wt%）和 F127/F68/HPMC（22.5/2.5/1wt%）中 M48U1 的释放动力学，结果表明用作对照的 HEC 水凝胶（1.5wt%）释放了 93%的肽，而约 25%的 M48U1 仍留在泊洛沙姆（®）水凝胶中。M48U1 在泊洛沙姆（®）水凝胶中的配方可确保局部递送，因为在阴道恒河猴黏膜上使用 Ussing 室未检测到肽的扩散。最后，毒理学研究表明，与 HEC 和磷酸盐缓冲盐水相比，泊洛沙姆（®）水凝胶对 HeLa 细胞的活力没有显著差异。
