Martín-Illana Araceli, Notario-Pérez Fernando, Cazorla-Luna Raúl, Ruiz-Caro Roberto, Veiga María Dolores
Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain.
Pharmaceutics. 2019 May 13;11(5):232. doi: 10.3390/pharmaceutics11050232.
Sub-Saharan African women are still at risk from the human immunodeficiency virus (HIV), and sex with men is the main route of transmission. Vaginal formulations containing antiretroviral drugs are promising tools to give women the power to protect themselves. The aim of this work was to obtain freeze-dried bigels containing pectin, chitosan, or hypromellose for the vaginal controlled release of Tenofovir, which is accelerated in the presence of semen. Nine batches of bigels were formulated using different proportions of these polymers in the hydrogel (1, 2, and 3% /). The bigels obtained were freeze-dried and then underwent hardness and deformability, mucoadhesion, swelling, and drug release tests, the last two in simulated vaginal fluid (SVF) and SVF/simulated seminal fluid (SSF) mixture. The formulation containing 3% pectin (fd3P) has the highest values for hardness, resistance to deformation, and good mucoadhesivity. Its swelling is conditioned by the pH of the medium, which is responsive to the controlled release of Tenofovir in SVF, with the fastest release in the SVF/SSF mixture. fd3P would be an interesting smart microbicidal system to allow faster release of Tenofovir in the presence of semen, and thus increase women's ability to protect themselves from the sexual transmission of HIV.
撒哈拉以南非洲地区的女性仍面临感染人类免疫缺陷病毒（HIV）的风险，与男性发生性行为是主要传播途径。含有抗逆转录病毒药物的阴道制剂是赋予女性自我保护能力的有前景的工具。这项工作的目的是制备含有果胶、壳聚糖或羟丙甲纤维素的冻干双凝胶，用于替诺福韦的阴道控释，替诺福韦在精液存在时释放加速。使用水凝胶中这些聚合物的不同比例（1%、2%和3%）配制了九批双凝胶。将得到的双凝胶冻干，然后进行硬度和变形性、粘膜粘附性、溶胀性和药物释放测试，后两项测试在模拟阴道液（SVF）和SVF/模拟精液（SSF）混合物中进行。含有3%果胶的制剂（fd3P）在硬度、抗变形性和良好的粘膜粘附性方面具有最高值。其溶胀受介质pH值的影响，这对替诺福韦在SVF中的控释有响应，在SVF/SSF混合物中释放最快。fd3P将是一个有趣的智能杀菌系统，可在精液存在时使替诺福韦更快释放，从而增强女性预防HIV性传播的自我保护能力。
