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

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Cazorla Luna, Raúl and Martín Illana, Araceli and Notario Pérez, Fernando and Bedoya del Olmo, Luis Miguel and Tamayo, Aitana and Ruiz-Caro, Roberto and Rubio, Juan and Veiga Ochoa, María Dolores (2020) Vaginal Polyelectrolyte Layer-by-Layer Films Based on Chitosan Derivatives and Eudragit® S100 for pH Responsive Release of Tenofovir. Marine Drugs, 18 (1). p. 44. ISSN 1660-3397

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Official URL: https://doi.org/10.3390/md18010044




Abstract

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.


Item Type:Article
Uncontrolled 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
Subjects:Medical sciences > Medicine > Communicable diseases
Medical sciences > Pharmacy > Molecular biology
Medical sciences > Pharmacy > Pharmacology
ID Code:68532
Deposited On:04 Nov 2021 09:01
Last Modified:04 Nov 2021 09:04

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