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TitlePTS micelles for the delivery of hydrophobic methotrexate
Author(s)Cerqueira, Patrícia
Noro, Jennifer Martins
Moura, Sofia
Guimarães, Diana
Silva, Carla
Cavaco-Paulo, Artur
Loureiro, Ana Isabel Sá
KeywordsPTS micelles
Methotrexate di-ethylated
Auxiliary solvent method
Sonication method
Cancer therapy
Issue date2019
JournalInternational Journal of Pharmaceutics
CitationCerqueira, 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
Abstract(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.
Publisher version
AccessOpen access
Appears in Collections:CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series

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