Utilize este identificador para referenciar este registo:
https://hdl.handle.net/1822/60532
Título: | PTS micelles for the delivery of hydrophobic methotrexate |
Autor(es): | Cerqueira, Patrícia Noro, Jennifer Martins Moura, Sofia Guimarães, Diana Silva, Carla Cavaco-Paulo, Artur Loureiro, Ana Isabel Sá |
Palavras-chave: | PTS micelles Methotrexate di-ethylated Prodrug Auxiliary solvent method Sonication method Cancer therapy |
Data: | 2019 |
Editora: | Elsevier |
Revista: | International Journal of Pharmaceutics |
Citação: | Cerqueira, P.; Jennifer Noro; Moura, A.; Guimarães, Diana Isabel Pereira; Silva, Carla; Cavaco-Paulo, Artur; Loureiro, Ana, PTS micelles for the delivery of hydrophobic methotrexate. International Journal of Pharmaceutics, 566, 282-290, 2019 |
Resumo(s): | Polyoxyethanyl--tocopheryl sebacate (PTS) is an amphiphilic compound with self-emulsifying properties known to form micelles. In this work, we report the production of PTS micelles for the encapsulation and delivery of a hydrophobic derivative of methotrexate, MTX di-ethylated (MTX-OEt). We optimized the micelles production by testing two different techniques: auxiliary solvent and sonication. Small and homogeneous micelles ( 40 nm) were obtained through the auxiliary solvent method performed at 30 °C and using 15 mg/mL of PTS. The produced micelles with the most promising physicochemical properties did not induce cytotoxicity when tested in normal human cells (BJ5ta cells), being considered for the encapsulation of MTX-OEt. This prodrug was achieved by Fisher esterification using ethanol, being isolated in good yield (= 68 %). MTX-OEt was efficiently encapsulated onto the produced micelles which preserved their physicochemical properties. The PTS micelles loaded with MTX-OEt, free MTX-OEt and free unmodified MTX revealed similar biological effect against cancer cells (Caco-2 cells). These results demonstrated that the biological activity of MTX is not altered after modification. The developed PTS micelles revealed a promising intracellular delivery performance with potentiality for cancer therapy. |
Tipo: | Artigo |
URI: | https://hdl.handle.net/1822/60532 |
DOI: | 10.1016/j.ijpharm.2019.05.049 |
ISSN: | 03785173 |
Versão da editora: | http://www.elsevier.com/locate/issn/03785173 |
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_51726_1.pdf | 2,06 MB | Adobe PDF | Ver/Abrir |