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Open AccessArticle

Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir

1
Department of Pharmaceutics and Food Technology, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
2
Department of Pharmacology, Pharmacognosy and Botany, Faculty of Pharmacy, Complutense University of Madrid, 28040 Madrid, Spain
3
Institute of Ceramics and Glass, Spanish National Research Council, 28049 Madrid, Spain
*
Author to whom correspondence should be addressed.
Mar. Drugs 2020, 18(1), 44; https://doi.org/10.3390/md18010044
Received: 11 December 2019 / Revised: 3 January 2020 / Accepted: 6 January 2020 / Published: 9 January 2020
(This article belongs to the Special Issue Marine Chitin 2019)
Women are still at high risk of contracting the human immunodeficiency virus (HIV) virus due to the lack of protection methods under their control, especially in sub-Saharan countries. Polyelectrolyte multilayer smart vaginal films based on chitosan derivatives (chitosan lactate, chitosan tartate, and chitosan citrate) and Eudragit® S100 were developed for the pH-sensitive release of Tenofovir. Films were characterized through texture analysis and scanning electron microscopy (SEM). Swelling and drug release studies were carried out in simulated vaginal fluid and a mixture of simulated vaginal and seminal fluids. Ex vivo mucoadhesion was evaluated in bovine vaginal mucosa. SEM micrographs revealed the formation of multilayer films. According to texture analysis, chitosan citrate was the most flexible compared to chitosan tartrate and lactate. The swelling studies showed a moderate water uptake (<300% in all cases), leading to the sustained release of Tenofovir in simulated vaginal fluid (up to 120 h), which was accelerated in the simulated fluid mixture (4–6 h). The films had high mucoadhesion in bovine vaginal mucosa. The multilayer films formed by a mixture of chitosan citrate and Eudragit® S100 proved to be the most promising, with zero toxicity, excellent mechanical properties, moderate swelling (<100%), high mucoadhesion capacity, and Tenofovir release of 120 h and 4 h in vaginal fluid and the simulated fluid mixture respectively. View Full-Text
Keywords: chitosan lactate; chitosan tartrate; chitosan citrate; Eudragit® S100; layer-by-layer film; mucoadhesive film; Tenofovir controlled release; pH responsive release; vaginal preexposure prophylaxis; HIV sexual transmission chitosan lactate; chitosan tartrate; chitosan citrate; Eudragit® S100; layer-by-layer film; mucoadhesive film; Tenofovir controlled release; pH responsive release; vaginal preexposure prophylaxis; HIV sexual transmission
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MDPI and ACS Style

Cazorla-Luna, R.; Martín-Illana, A.; Notario-Pérez, F.; Bedoya, L.M.; Tamayo, A.; Ruiz-Caro, R.; Rubio, J.; Veiga, M.-D. Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir. Mar. Drugs 2020, 18, 44.

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