Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir

Women are still at high risk of contracting the human immunodeficiency virus (HIV) virus due to the lack of protection methods under their control, especially in sub-Saharan countries. Polyelectrolyte multilayer smart vaginal films based on chitosan derivatives (chitosan lactate, chitosan tartate, a...

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Detalles Bibliográficos
Autores: Cazorla Luna, Raúl, Martín Illana, Araceli, Notario Pérez, Fernando, Bedoya Del Olmo, Luis Miguel, Tamayo, Aitana, Ruiz Caro, Roberto, Rubio, Juan, Veiga Ochoa, María Dolores
Tipo de recurso: artículo
Fecha de publicación:2020
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/8526
Acceso en línea:https://hdl.handle.net/20.500.14352/8526
Access Level:acceso abierto
Palabra clave:Chitosan lactate
Chitosan tartrate
Chitosan citrate
Eudragit® S100
Layer-by-layer film
Mucoadhesive film
Tenofovir controlled release
pH responsive release
Vaginal preexposure prophylaxis
HIV sexual transmission
Enfermedades infecciosas
Biología molecular (Farmacia)
Farmacología (Farmacia)
3205.05 Enfermedades Infecciosas
3209 Farmacología
Descripción
Sumario:Women are still at high risk of contracting the human immunodeficiency virus (HIV) virus due to the lack of protection methods under their control, especially in sub-Saharan countries. Polyelectrolyte multilayer smart vaginal films based on chitosan derivatives (chitosan lactate, chitosan tartate, and chitosan citrate) and Eudragit® S100 were developed for the pH-sensitive release of Tenofovir. Films were characterized through texture analysis and scanning electron microscopy (SEM). Swelling and drug release studies were carried out in simulated vaginal fluid and a mixture of simulated vaginal and seminal fluids. Ex vivo mucoadhesion was evaluated in bovine vaginal mucosa. SEM micrographs revealed the formation of multilayer films. According to texture analysis, chitosan citrate was the most flexible compared to chitosan tartrate and lactate. The swelling studies showed a moderate water uptake (<300% in all cases), leading to the sustained release of Tenofovir in simulated vaginal fluid (up to 120 h), which was accelerated in the simulated fluid mixture (4–6 h). The films had high mucoadhesion in bovine vaginal mucosa. The multilayer films formed by a mixture of chitosan citrate and Eudragit® S100 proved to be the most promising, with zero toxicity, excellent mechanical properties, moderate swelling (<100%), high mucoadhesion capacity, and Tenofovir release of 120 h and 4 h in vaginal fluid and the simulated fluid mixture respectively.