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

Marine Drugs

Mar໚-Pilar Sánchez-Sánchez³  Araceli Martín-Illana³  Roberto Ruiz-Caro³  Paulina Bermejo¹  Mar໚-José Abad¹  Rubén Carro¹  Luis-Miguel Bedoya¹  Aitana Tamayo⁴  Juan Rubio⁴  Anxo Fernández-Ferreiro²  Francisco Otero-Espinar²  Mar໚-Dolores Veiga³ 

[1] Departamento Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain; E-Mails:;Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad de Santiago de Compostela, Campus Vida s/n, 15782 Santiago de Compostela, Spain; E-Mails:;Departamento Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain; E-Mails:;Instituto de Cerámica y Vidrio, Consejo Superior de Investigaciones Científicas, 28049-Madrid, Spain, E-Mails:

关键词: chitosan;    kappa-carrageenan;    vaginal mucoadhesive formulations;    acyclovir controlled release;    swelling behaviour;    cytotoxicity;    genital herpes;    ex vivo bioadhesion;   

DOI  :  10.3390/md13095976

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.