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Keywords = pre-concentration ethanol injection method

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15 pages, 3210 KB  
Article
Increased Encapsulation Efficiency of Methotrexate in Liposomes for Rheumatoid Arthritis Therapy
by Diana Guimarães, Jennifer Noro, Ana Loureiro, Franck Lager, Gilles Renault, Artur Cavaco-Paulo and Eugénia Nogueira
Biomedicines 2020, 8(12), 630; https://doi.org/10.3390/biomedicines8120630 - 18 Dec 2020
Cited by 49 | Viewed by 7987
Abstract
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 [...] Read more.
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. Full article
(This article belongs to the Section Immunology and Immunotherapy)
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