Malli Sophia, Bories Christian, Pradines Bénédicte, Loiseau Philippe M, Ponchel Gilles, Bouchemal Kawthar
Institut Galien Paris Sud, UMR CNRS 8612, Univ. Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie, 5, rue J-B. Clément, 92296 Châtenay-Malabry, France; BioCIS « Biomolécules: Conception, Isolement, Synthèse » - « Chimiothérapie Antiparasitaire », UMR CNRS 8076, Univ. Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie, 5, rue J.B. Clément, 92296 Châtenay-Malabry cedex, France.
BioCIS « Biomolécules: Conception, Isolement, Synthèse » - « Chimiothérapie Antiparasitaire », UMR CNRS 8076, Univ. Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie, 5, rue J.B. Clément, 92296 Châtenay-Malabry cedex, France.
Eur J Pharm Biopharm. 2017 Mar;112:143-147. doi: 10.1016/j.ejpb.2016.11.024. Epub 2016 Nov 24.
The objective of this work is to design topically-applied thermosensitive and mucoadhesive hydrogel containing metronidazole (MTZ) for the treatment of Trichomonas vaginalis infections. Hydrogel composed of pluronic® F127 (20wt%), chitosan (1wt%) and metronidazole MTZ (0.7wt%) mixture showed its ability to decrease by a factor 4 MTZ flux and apparent permeability absorption through vaginal mucosa. The impact of hydrogel on transmucosal penetration of MTZ was evaluated ex vivo on excised porcine vaginal mucosa mounted on Franz diffusion cell. The anti-T. vaginalis activity of MTZ formulated into F127/chitosan hydrogel was preserved since the viability curve evaluated in vitro was similar to MTZ solution.
这项工作的目的是设计一种局部应用的含甲硝唑（MTZ）的热敏性和粘膜粘附性水凝胶，用于治疗阴道毛滴虫感染。由普朗尼克® F127（20wt%）、壳聚糖（1wt%）和甲硝唑MTZ（0.7wt%）混合物组成的水凝胶显示出其能够使MTZ通量降低4倍，并降低通过阴道粘膜的表观渗透吸收。在安装在Franz扩散池上的离体猪阴道粘膜上，对水凝胶对MTZ经粘膜渗透作用进行了体外评估。由于体外评估的活力曲线与MTZ溶液相似，因此制成F127/壳聚糖水凝胶的MTZ的抗阴道毛滴虫活性得以保留。
