Eudragit® L100/chitosan composite thin bilayer films for intravaginal pH-responsive release of Tenofovir



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Martín Illana, Araceli and Cazorla Luna, R. and Notario Pérez, Fernando and Rubio, J. and Ruiz Caro, Roberto and Tamayo, A. and Veiga Ochoa, María Dolores (2022) Eudragit® L100/chitosan composite thin bilayer films for intravaginal pH-responsive release of Tenofovir. International journal of pharmaceutics, 616 . p. 121554. ISSN 0378-5173

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The high rate of HIV new infections and AIDS-related deaths each year make prevention tools still necessary today. Different dosage forms – including films – for vaginal administration of antiretroviral drugs have been developed for this purpose. Six batches of Tenofovir-loaded films were formulated based on Eudragit® L100 (EL100) and chitosan, containing triethyl citrate and glycerol. In all the cases films structured in two layers – the upper layer mainly attributed to EL100 and the lower layer to chitosan – were revealed by SEM. A higher content in EL100 and plasticizers improves the mechanical properties and control over drug release in the vaginal medium without affecting mucoadhesion. The EL100-based layer acts as a structuring agent that controls Tenofovir release for days in the vaginal medium while it occurs in a few hours in the presence of seminal fluid. Bilayer films with the highest tested content of EL100 and plasticizers would be the most suitable as vaginal microbicides as they are easier to administer due to their excellent mechanical properties and they offer more comfortable posology and enhanced protection against HIV during intercourse due to their pH-responsive release of Tenofovir.

Item Type:Article
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CRUE-CSIC (Acuerdos Transformativos 2022)

Uncontrolled Keywords:Bilayer films, Chitosan-based films, Eudragit® L100-based films, Films’ mechanical properties, Mucoadhesive vaginal films, Tenofovir pH-responsive release, Vaginal microbicides
Subjects:Medical sciences > Pharmacy > Pharmaceutical technology
ID Code:72523
Deposited On:26 May 2022 12:18
Last Modified:18 Oct 2022 09:00

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