Pradines Bénédicte, Bories Christian, Vauthier Christine, Ponchel Gilles, Loiseau Philippe M, Bouchemal Kawthar
Institut Galien Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, Univ Paris-Sud, Châtenay-Malabry, France.
Pharm Res. 2015 Apr;32(4):1229-36. doi: 10.1007/s11095-014-1528-7. Epub 2014 Oct 16.
The present work reports a non-conventional therapeutic strategy based on the use of vaginally-applied formulations for the treatment of trichomoniasis due to Trichomonas vaginalis without adding a drug.
The formulations were based on a thermosensitive pluronic® F127 hydrogel containing mucoadhesive poly(isobutylcyanoacrylate) nanoparticles coated with a mixture of chitosan and thiolated chitosan (75/25 wt%). The nanoparticles were obtained by anionic emulsion polymerization of isobutylcyanoacrylate. The anti-T. vaginalis activity of the formulations was evaluated in vitro.
Chitosan-coated nanoparticles showed a strong anti-T. vaginalis activity at 100 μg/mL independently on the proportion of thiolated chitosan. No anti-T. vaginalis activity was reported neither with chitosan-uncoated poly(isobutylcyanoacrylate) nanoparticles nor with chitosan used as a solution. These results suggest that the anti-T. vaginalis activity was related to poly(isobutylcyanoacrylate) nanoparticles but only when they are coated with chitosan. Histological analysis of ex vivo pig vaginal mucosa in contact with pluronic® F127 hydrogel containing poly(isobutylcyanoacrylate) nanoparticles coated with the mixture chitosan/thiolated chitosan (75/25 wt%) did not reveal any toxicity.
This study demonstrated that poly(isobutylcyanoacrylate) nanoparticles coated with chitosan were active against T. vaginalis without adding a drug. Besides their anti-T. vaginalis activity, the formulations are non-toxic towards pig vaginal mucosa.
本研究报告了一种非传统的治疗策略，该策略基于使用经阴道给药的制剂来治疗由阴道毛滴虫引起的滴虫病，且不添加药物。
这些制剂基于一种热敏性的普朗尼克® F127水凝胶，其中含有用壳聚糖和硫醇化壳聚糖混合物（75/25重量%）包覆的粘膜粘附性聚（异丁基氰基丙烯酸酯）纳米颗粒。纳米颗粒通过异丁基氰基丙烯酸酯的阴离子乳液聚合获得。对这些制剂的抗阴道毛滴虫活性进行了体外评估。
壳聚糖包覆的纳米颗粒在100 μg/mL时显示出强大的抗阴道毛滴虫活性，与硫醇化壳聚糖的比例无关。未包覆壳聚糖的聚（异丁基氰基丙烯酸酯）纳米颗粒以及用作溶液的壳聚糖均未报告有抗阴道毛滴虫活性。这些结果表明，抗阴道毛滴虫活性与聚（异丁基氰基丙烯酸酯）纳米颗粒有关，但仅当它们用壳聚糖包覆时才具有活性。对与含有用壳聚糖/硫醇化壳聚糖混合物（75/25重量%）包覆的聚（异丁基氰基丙烯酸酯）纳米颗粒的普朗尼克® F127水凝胶接触的离体猪阴道粘膜进行组织学分析，未发现任何毒性。
本研究表明，用壳聚糖包覆的聚（异丁基氰基丙烯酸酯）纳米颗粒在不添加药物的情况下对阴道毛滴虫具有活性。除了其抗阴道毛滴虫活性外，这些制剂对猪阴道粘膜无毒。
