Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.
Departamento de Farmacología, Farmacognosia y Botánica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.
Eur J Pharm Sci. 2019 Jan 15;127:38-51. doi: 10.1016/j.ejps.2018.10.013. Epub 2018 Oct 19.
Nowadays, million women live with the human immunodeficiency virus (HIV) worldwide and many of them are dying per year, particularly in Sub-Saharan Africa. The development of systems that can be accessed by this population group to prevent the sexual transmission of the virus is therefore necessary. The aim of this work was the formulation of freeze-dried bioadhesive vaginal bigels releasing Tenofovir in a controlled manner. Systems containing three different proportions of guar gum hydrogel and sesame oil were prepared, adding Span®60 or Span®60 and Tween®60 as surfactants. Drug and excipients were evaluated by cytotoxicity assays, showing no toxicity at the concentrations tested neither for the drug nor any of the excipients. Fresh formulations were characterised through texture analyses and confocal laser microcopy. The system with the lowest guar gum hydrogel/sesame oil proportion and containing Span®60 and Tween®60 (batch ST1) had the highest consistency and adhesion capacity according to texture analyses. Furthermore, a genuine bigel microstructure was observed. After freeze-drying, swelling, bioadhesion and drug release tests were performed on the resulting systems. ST1 showed the longest bioadhesion time and the most controlled release, as well as a low swelling grade, becoming an interesting option for preventing HIV sexual transmission in women.
如今，全世界有数百万女性携带人类免疫缺陷病毒（HIV），其中许多人每年都会死亡，尤其是在撒哈拉以南非洲地区。因此，有必要开发能够被该人群群体访问的系统，以防止病毒的性传播。这项工作的目的是开发能够以受控方式释放替诺福韦的冻干生物黏附阴道双凝胶。制备了含有三种不同比例瓜尔胶水凝胶和芝麻油的系统，并添加了 Span®60 或 Span®60 和 Tween®60 作为表面活性剂。通过细胞毒性测定评估药物和赋形剂，在测试的浓度下，无论是药物还是任何赋形剂都没有显示出毒性。通过质地分析和共聚焦激光显微镜对新鲜制剂进行了表征。根据质地分析，具有最低瓜尔胶水凝胶/芝麻油比例并含有 Span®60 和 Tween®60 的系统（批次 ST1）具有最高的稠度和粘附能力。此外，还观察到了真正的大凝胶微观结构。对所得系统进行了冻干、溶胀、生物黏附性和药物释放测试。ST1 表现出最长的生物黏附时间和最受控的释放，以及低的溶胀等级，成为预防女性 HIV 性传播的一个有趣选择。
