Eudragit® L100/chitosan composite thin bilayer films for intravaginal pH-responsive release of Tenofovir

[EN] 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 formu...

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Detalles Bibliográficos
Autores: Martín-Illana, Araceli, Cazorla-Luna, Raúl, Notario-Pérez, Fernando, Rubio Alonso, Juan, Ruiz-Caro, Roberto, Tamayo Hernando, Aitana, Veiga, María Dolores
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/304450
Acceso en línea:http://hdl.handle.net/10261/304450
Access Level:acceso abierto
Palabra clave:Bilayer films
Chitosan-based films
Eudragit® L100-based films
Films’ mechanical properties
Mucoadhesive vaginal filmsTenofovir pH-responsive release
Vaginal microbicides
Descripción
Sumario:[EN] 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.