Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/61472
Título: | Rational development of liposomal hydrogels: A strategy for topical vaginal antiretroviral drug delivery in the context of HIV prevention |
Autor(es): | Faria, Maria J. Machado, Raul Ribeiro, Artur Gonçalves, Hugo Real Oliveira, M. Elisabete C.D. Viseu, T. M. R. das Neves, José Lúcio, M. |
Palavras-chave: | drug release emtricitabine hydrogels liposomes liposomes microbicides nanomedicine tenofovir disoproxil fumarate topical PrEP |
Data: | 18-Set-2019 |
Editora: | Multidisciplinary Digital Publishing Institute |
Revista: | Pharmaceutics |
Citação: | 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. |
Resumo(s): | 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 (<i>J</i><sub>ss</sub> = 9.9 μg·cm<sup>−2</sup>·h<sup>−1</sup>). 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. |
Tipo: | Artigo |
URI: | https://hdl.handle.net/1822/61472 |
DOI: | 10.3390/pharmaceutics11090485 |
ISSN: | 1999-4923 |
Versão da editora: | https://www.mdpi.com/1999-4923/11/9/485 |
Arbitragem científica: | yes |
Acesso: | Acesso aberto |
Aparece nas coleções: | CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series CDF - FAMO - Artigos/Papers (with refereeing) DBio - Artigos/Papers |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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pharmaceutics-11-00485.pdf | 1,29 MB | Adobe PDF | Ver/Abrir |
Este trabalho está licenciado sob uma Licença Creative Commons