增塑剂
黏膜黏附
壳聚糖
立即释放
杀菌剂
双层
甘油
性传播疾病用杀菌剂
控制释放
替诺福韦
化学
剂型
药理学
药品
材料科学
人类免疫缺陷病毒(HIV)
色谱法
化学工程
医学
毒品携带者
有机化学
病毒学
膜
生物化学
卫生服务
工程类
环境卫生
人口
作者
Araceli Martín-Illana,Raúl Cazorla-Luna,Fernando Notario-Pérez,J. L. Rubio,Roberto Ruíz-Caro,Aitana Tamayo,M.M. Veiga
标识
DOI:10.1016/j.ijpharm.2022.121554
摘要
The high rate of HIV new infections and AIDS-related deaths each year make prevention tools still necessary today. Different dosage forms - including films - for vaginal administration of antiretroviral drugs have been developed for this purpose. Six batches of Tenofovir-loaded films were formulated based on Eudragit® L100 (EL100) and chitosan, containing triethyl citrate and glycerol. In all the cases films structured in two layers - the upper layer mainly attributed to EL100 and the lower layer to chitosan - were revealed by SEM. A higher content in EL100 and plasticizers improves the mechanical properties and control over drug release in the vaginal medium without affecting mucoadhesion. The EL100-based layer acts as a structuring agent that controls Tenofovir release for days in the vaginal medium while it occurs in a few hours in the presence of seminal fluid. Bilayer films with the highest tested content of EL100 and plasticizers would be the most suitable as vaginal microbicides as they are easier to administer due to their excellent mechanical properties and they offer more comfortable posology and enhanced protection against HIV during intercourse due to their pH-responsive release of Tenofovir.
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