Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir
Vaginal microbicides have the potential to give women at high risk of contracting HIV the option of self-protection by preventing the sexual transmission of the virus. In this paper, mucoadhesive vaginal tablets based on chitosan, alone and in combination with pectin and locust bean gum, were develo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-01-01
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| Series: | Pharmaceutics |
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| Online Access: | http://www.mdpi.com/1999-4923/11/1/20 |
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| author | Raúl Cazorla-Luna Fernando Notario-Pérez Araceli Martín-Illana Roberto Ruiz-Caro Aitana Tamayo Juan Rubio María Dolores Veiga |
| author_facet | Raúl Cazorla-Luna Fernando Notario-Pérez Araceli Martín-Illana Roberto Ruiz-Caro Aitana Tamayo Juan Rubio María Dolores Veiga |
| author_sort | Raúl Cazorla-Luna |
| collection | DOAJ |
| description | Vaginal microbicides have the potential to give women at high risk of contracting HIV the option of self-protection by preventing the sexual transmission of the virus. In this paper, mucoadhesive vaginal tablets based on chitosan, alone and in combination with pectin and locust bean gum, were developed for the sustained release of tenofovir (an antiretroviral drug). The formulations were placed in simulant vaginal fluid (SVF) to swell, and Hg porosity and SEM microscopy were used for the microstructural characterization of the swelling witnesses. The results show that the association of pectin and chitosan generated polyelectrolyte complexes and produced a robust system able to maintain its structure during the swelling process, when small pores are formed. Drug release and bovine vaginal mucoadhesion studies were performed in SVF showing that tenofovir-controlled dissolution profiles and adhesion to the mucosa were conditioned by the swelling processes of the polymer/s in each formulation. Tablets based on chitosan/pectin have the most homogeneous tenofovir dissolution profiles and last up to 96 h, remaining attached to the vaginal mucosa for the same period. These formulations can therefore be considered a good option for the self-protection of women from the sexual transmission of HIV. |
| first_indexed | 2024-04-11T22:03:08Z |
| format | Article |
| id | doaj.art-57e0f52e35f1483f830d34e71c0de5f2 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T22:03:08Z |
| publishDate | 2019-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-57e0f52e35f1483f830d34e71c0de5f22022-12-22T04:00:51ZengMDPI AGPharmaceutics1999-49232019-01-011112010.3390/pharmaceutics11010020pharmaceutics11010020Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug TenofovirRaúl Cazorla-Luna0Fernando Notario-Pérez1Araceli Martín-Illana2Roberto Ruiz-Caro3Aitana Tamayo4Juan Rubio5María Dolores Veiga6Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, SpainDepartamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, SpainDepartamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, SpainDepartamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, SpainInstituto de Cerámica y Vidrio, Consejo Superior de Investigaciones Científicas, 28049 Madrid, SpainInstituto de Cerámica y Vidrio, Consejo Superior de Investigaciones Científicas, 28049 Madrid, SpainDepartamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, SpainVaginal microbicides have the potential to give women at high risk of contracting HIV the option of self-protection by preventing the sexual transmission of the virus. In this paper, mucoadhesive vaginal tablets based on chitosan, alone and in combination with pectin and locust bean gum, were developed for the sustained release of tenofovir (an antiretroviral drug). The formulations were placed in simulant vaginal fluid (SVF) to swell, and Hg porosity and SEM microscopy were used for the microstructural characterization of the swelling witnesses. The results show that the association of pectin and chitosan generated polyelectrolyte complexes and produced a robust system able to maintain its structure during the swelling process, when small pores are formed. Drug release and bovine vaginal mucoadhesion studies were performed in SVF showing that tenofovir-controlled dissolution profiles and adhesion to the mucosa were conditioned by the swelling processes of the polymer/s in each formulation. Tablets based on chitosan/pectin have the most homogeneous tenofovir dissolution profiles and last up to 96 h, remaining attached to the vaginal mucosa for the same period. These formulations can therefore be considered a good option for the self-protection of women from the sexual transmission of HIV.http://www.mdpi.com/1999-4923/11/1/20vaginal preexposure prophylaxis of HIVtenofovir controlled releasemucoadhesive vaginal tabletsnatural polymers combinationchitosanpectinlocust bean gum |
| spellingShingle | Raúl Cazorla-Luna Fernando Notario-Pérez Araceli Martín-Illana Roberto Ruiz-Caro Aitana Tamayo Juan Rubio María Dolores Veiga Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir Pharmaceutics vaginal preexposure prophylaxis of HIV tenofovir controlled release mucoadhesive vaginal tablets natural polymers combination chitosan pectin locust bean gum |
| title | Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir |
| title_full | Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir |
| title_fullStr | Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir |
| title_full_unstemmed | Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir |
| title_short | Chitosan-Based Mucoadhesive Vaginal Tablets for Controlled Release of the Anti-HIV Drug Tenofovir |
| title_sort | chitosan based mucoadhesive vaginal tablets for controlled release of the anti hiv drug tenofovir |
| topic | vaginal preexposure prophylaxis of HIV tenofovir controlled release mucoadhesive vaginal tablets natural polymers combination chitosan pectin locust bean gum |
| url | http://www.mdpi.com/1999-4923/11/1/20 |
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