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Mar. Drugs 2015, 13(9), 5976-5992; doi:10.3390/md13095976

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

1
Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain
2
Departamento Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain
3
Instituto de Cerámica y Vidrio, Consejo Superior de Investigaciones Científicas, 28049-Madrid, Spain,
4
Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Vida s/n, 15782 Santiago de Compostela, Spain
*
Author to whom correspondence should be addressed.
Academic Editor: Hitoshi Sashiwa
Received: 2 August 2015 / Revised: 11 September 2015 / Accepted: 15 September 2015 / Published: 18 September 2015
(This article belongs to the Special Issue Advances in Marine Chitin and Chitosan II, 2017)
View Full-Text   |   Download PDF [574 KB, uploaded 18 September 2015]   |  

Abstract

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. View Full-Text
Keywords: chitosan; kappa-carrageenan; vaginal mucoadhesive formulations; acyclovir controlled release; swelling behaviour; cytotoxicity; genital herpes; ex vivo bioadhesion chitosan; kappa-carrageenan; vaginal mucoadhesive formulations; acyclovir controlled release; swelling behaviour; cytotoxicity; genital herpes; ex vivo bioadhesion
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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.

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