Chitosan and Kappa-Carrageenan Vaginal Acyclovir Formulations for Prevention of Genital Herpes. In Vitro and Ex Vivo Evaluation

Vaginal formulations for the prevention of sexually transmitted infections are currently gaining importance in drug development. Polysaccharides, such as chitosan and carrageenan, which have good binding capacity with mucosal tissues, are now included in vaginal delivery systems. Marine polymer-base...

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Detalles Bibliográficos
Autores: Sánchez Sánchez, María Pilar, Martín Illana, Araceli, Ruiz Caro, Roberto, Bermejo Benito, Paulina, Abad Martínez, María José, Carro, Rubén, Bedoya Del Olmo, Luis Miguel, Tamayo, Aitana, Rubio, Juan, Fernández Ferreiro, Anxo, Otero Espinar, Francisco, Veiga Ochoa, María Dolores
Tipo de recurso: artículo
Fecha de publicación:2015
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/23892
Acceso en línea:https://hdl.handle.net/20.500.14352/23892
Access Level:acceso abierto
Palabra clave:Chitosan
Kappa-carrageenan
Vaginal mucoadhesive formulations
Acyclovir controlled release
Swelling behaviour
Cytotoxicity
Genital herpes
Ex vivo bioadhesion
Biología celular (Farmacia)
Farmacología (Farmacia)
3209 Farmacología
Descripción
Sumario:Vaginal formulations for the prevention of sexually transmitted infections are currently gaining importance in drug development. Polysaccharides, such as chitosan and carrageenan, which have good binding capacity with mucosal tissues, are now included in vaginal delivery systems. Marine polymer-based vaginal mucoadhesive solid formulations have been developed for the controlled release of acyclovir, which may prevent the sexual transmission of the herpes simplex virus. Drug release studies were carried out in two media: simulated vaginal fluid and simulated vaginal fluid/simulated seminal fluid mixture. The bioadhesive capacity and permanence time of the bioadhesion, the prepared compacts, and compacted granules were determined ex vivo using bovine vaginal mucosa as substrate. Swelling processes were quantified to confirm the release data. Biocompatibility was evaluated through in vitro cellular toxicity assays, and the results showed that acyclovir and the rest of the materials had no cytotoxicity at the maximum concentration tested. The mixture of hydroxyl-propyl-methyl-cellulose with chitosan- or kappa-carrageenan-originated mucoadhesive systems that presented a complete and sustained release of acyclovir for a period of 8–9 days in both media. Swelling data revealed the formation of optimal mixed chitosan/hydroxyl-propyl-methyl-cellulose gels which could be appropriated for the prevention of sexual transmission of HSV.