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

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Sánchez Sánchez, María Pilar and Martín Illana, Araceli and Ruiz Caro, Roberto and Bermejo Benito, Paulina and Abad Martínez, María José and Carro, Rubén and Bedoya del Olmo, Luis Miguel and Tamayo, Aitana and Rubio, Juan and Fernández Ferreiro, Anxo and Otero Espinar, Francisco and Veiga Ochoa, María Dolores (2015) Chitosan and Kappa-Carrageenan Vaginal Acyclovir Formulations for Prevention of Genital Herpes. In Vitro and Ex Vivo Evaluation. Marine Drugs, 13 (9). pp. 5976-5992. ISSN 1660-3397

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Official URL: https://doi.org/10.3390/md13095976




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.


Item Type:Article
Uncontrolled Keywords:chitosan; kappa-carrageenan; vaginal mucoadhesive formulations; acyclovir controlled release; swelling behaviour; cytotoxicity; genital herpes; ex vivo bioadhesion
Subjects:Medical sciences > Pharmacy > Cytology
Medical sciences > Pharmacy > Pharmacology
ID Code:68529
Deposited On:04 Nov 2021 08:47
Last Modified:04 Nov 2021 09:02

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