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Open AccessArticle

Rational Development of Liposomal Hydrogels: A Strategy for Topical Vaginal Antiretroviral Drug Delivery in the Context of HIV Prevention

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CF-UM-UP—Centro de Física das Universidades do Minho e Porto, Departamento de Física da Universidade do Minho, 4710-057 Braga, Portugal
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CBMA—Centro de Biologia Molecular e Ambiental, Departamento de Biologia, Universidade do Minho, 4710-057 Braga, Portugal
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IB-S—Institute of Science and Innovation for Bio-Sustainability, Universidade do Minho, 4710-057 Braga, Portugal
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CEB—Centro de Engenharia Biológica, Universidade do Minho, 4710-057 Braga, Portugal
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Paralab, SA, 4420-392 Valbom, Portugal
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i3S—Instituto de Investigação e Inovação em Saúde, Universidade do Porto, 4200-135 Porto, Portugal
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INEB—Instituto de Engenharia Biomédica, Universidade do Porto, 4200-135 Porto, Portugal
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CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, 4585-116 Gandra, Portugal
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Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(9), 485; https://doi.org/10.3390/pharmaceutics11090485
Received: 22 August 2019 / Revised: 11 September 2019 / Accepted: 14 September 2019 / Published: 18 September 2019
(This article belongs to the Special Issue Vaginal Drug Delivery for Local and Systemic Applications)
HIV/AIDS stands as a global burden, and vaginal microbicides constitute a promising strategy for topical pre-exposure prophylaxis. Preceding the development of a microbicide containing tenofovir disoproxil fumarate (TDF) and emtricitabine (FTC), in silico and in vitro studies were performed to evaluate the physicochemical characteristics of both drugs, and to study their biophysical impact in lipid model systems. Results from these pre-formulation studies defined hydrogels as adequate vehicles to incorporate TDF-loaded liposomes and FTC. After studying interactions with mucin, zwitterionic liposomes with a mean diameter of 134 ± 13 nm, an encapsulation TDF efficiency of approximately 84%, and a transition temperature of 41 °C were selected. The chosen liposomal formulation was non-cytotoxic to HEC-1-A and CaSki cells, and was able to favor TDF permeation across polysulfone membranes (Jss = 9.9 μg·cm−2·h−1). After the incorporation of TDF-loaded liposomes and FTC in carbomer hydrogels, the drug release profile was sustained over time, reaching around 60% for both drugs within 3–6 h, and best fitting the Weibull model. Moreover, liposomal hydrogels featured pseudoplastic profiles that were deemed suitable for topical application. Overall, the proposed liposomal hydrogels may constitute a promising formulation for the vaginal co-delivery of TDF/FTC. View Full-Text
Keywords: drug release; emtricitabine; hydrogels; liposomes; microbicides; nanomedicine; tenofovir disoproxil fumarate; topical PrEP drug release; emtricitabine; hydrogels; liposomes; microbicides; nanomedicine; tenofovir disoproxil fumarate; topical PrEP
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MDPI and ACS Style

Faria, M.J.; Machado, R.; Ribeiro, A.; Gonçalves, H.; Real Oliveira, M.E.C.D.; Viseu, T.; das Neves, J.; Lúcio, M. Rational Development of Liposomal Hydrogels: A Strategy for Topical Vaginal Antiretroviral Drug Delivery in the Context of HIV Prevention. Pharmaceutics 2019, 11, 485.

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