RT Journal Article
T1 Chitosan and Kappa-Carrageenan Vaginal Acyclovir Formulations for Prevention of Genital Herpes. In Vitro and Ex Vivo Evaluation
A1 Sánchez Sánchez, María Pilar
A1 Martín Illana, Araceli
A1 Ruiz Caro, Roberto
A1 Bermejo, Paulina
A1 Abad, María José
A1 Carro, Rubén
A1 Bedoya, Luis Miguel
A1 Tamayo, Aitana
A1 Rubio, Juan
A1 Fernández Ferreiro, Anxo
A1 Otero Espinar, Francisco Javier
A1 Veiga, María Dolores
K1 Chitosan
K1 Kappa-carrageenan
K1 Vaginal mucoadhesive formulations
K1 Acyclovir controlled release
K1 Swelling behaviour
K1 Cytotoxicity
K1 Genital herpes
K1 Ex vivo bioadhesion
AB 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
PB MDPI
YR 2015
FD 2015
LK http://hdl.handle.net/10347/23609
UL http://hdl.handle.net/10347/23609
LA eng
NO Sánchez-Sánchez, M.-P.; Martín-Illana, A.; Ruiz-Caro, R.; Bermejo, P.; Abad, M.-J.; Carro, R.; Bedoya, L.-M.; Tamayo, A.; Rubio, J.; Fernández-Ferreiro, A.; Otero-Espinar, F.; Veiga, M.-D. Chitosan and Kappa-Carrageenan Vaginal Acyclovir Formulations for Prevention of Genital Herpes. In Vitro and Ex Vivo Evaluation. Mar. Drugs 2015, 13, 5976-5992
NO This work was supported by the Spanish Ministry of Economy and Competitiveness (MAT2012-34552)
DS Minerva
RD 28 abr 2026