Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/71034
Título: | Increased encapsulation efficiency of methotrexate in liposomes for rheumatoid arthritis therapy |
Autor(es): | Guimarães, Diana Isabel Pereira Noro, Jennifer Martins Loureiro, Ana Isabel Sá Lager, Franck Renault, Gilles Cavaco-Paulo, Artur Nogueira, Eugénia |
Palavras-chave: | liposomes methotrexate encapsulation pre-concentration ethanol injection method rheumatoid arthritis |
Data: | 18-Dez-2020 |
Editora: | MDPI |
Revista: | Biomedicines |
Citação: | Guimarães, Diana Isabel Pereira; Jennifer Noro; Loureiro, Ana; Lager, Franck; Renault, Gilles; Cavaco-Paulo, Artur; Nogueira, E., Increased encapsulation efficiency of methotrexate in liposomes for rheumatoid arthritis therapy. Biomedicines, 8(12), 630, 2020 |
Resumo(s): | Methotrexate (MTX) is a common drug used to treat rheumatoid arthritis. Due to the excessive side effects, encapsulation of MTX in liposomes is considered an effective delivery system, reducing drug toxicity, while maintaining its efficacy. The ethanol injection method is an interesting technique for liposome production, due to its simplicity, fast implementation, and reproducibility. However, this method occasionally requires the extrusion process, to obtain suitable size distribution, and achieve a low level of MTX encapsulation. Here, we develop a novel pre-concentration method, based on the principles of the ethanol injection, using an initial aqueous volume of 20% and 1:1 ratio of organic:aqueous phase (v/v). The liposomes obtained present small values of size and polydispersity index, without the extrusion process, and a higher MTX encapsulation (efficiency higher than 30%), suitable characteristics for in vivo application. The great potential of MTX to interact at the surface of the lipid bilayer was shown by nuclear magnetic resonance (NMR) studies, revealing mutual interactions between the drug and the main phospholipid via hydrogen bonding. In vivo experiments reveal that liposomes encapsulating MTX significantly increase the biological benefit in arthritic mice. This approach shows a significant advance in MTX therapeutic applications. |
Tipo: | Artigo |
URI: | https://hdl.handle.net/1822/71034 |
DOI: | 10.3390/biomedicines8120630 |
ISSN: | 2227-9059 |
Versão da editora: | https://www.mdpi.com/2227-9059/8/12/630 |
Arbitragem científica: | yes |
Acesso: | Acesso aberto |
Aparece nas coleções: | CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series |
Ficheiros deste registo:
Ficheiro | Descrição | Tamanho | Formato | |
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document_54071_1.pdf | 3,21 MB | Adobe PDF | Ver/Abrir |
Este trabalho está licenciado sob uma Licença Creative Commons