Sánchez Sánchez, María PilarMartín Illana, AraceliRuiz Caro, RobertoBermejo, PaulinaAbad, María JoséCarro, RubénBedoya, Luis MiguelTamayo, AitanaRubio, JuanFernández Ferreiro, AnxoOtero Espinar, Francisco JavierVeiga, María Dolores2020-11-092020-11-092015Sánchez-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, 5976-5992http://hdl.handle.net/10347/23609Vaginal 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 HSVeng© 2015 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/)Atribución 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/ChitosanKappa-carrageenanVaginal mucoadhesive formulationsAcyclovir controlled releaseSwelling behaviourCytotoxicityGenital herpesEx vivo bioadhesionjournal article10.3390/md130959761660-3397open access