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Article

Synthesis of Two Methotrexate Prodrugs for Optimizing Drug Loading into Liposomes

1
Laboratory of Nanotechnology for Precision Medicine, Fondazione Istituto Italiano di Tecnologia, Via Morego 30, 16163 Genoa, Italy
2
Department of Informatics, Bioengineering, Robotics and System Engineering, University of Genoa, Via Opera Pia 13, 16145 Genoa, Italy
*
Authors to whom correspondence should be addressed.
These authors contribute equally to this paper.
Academic Editor: Sophia G. Antimisiaris
Pharmaceutics 2021, 13(3), 332; https://doi.org/10.3390/pharmaceutics13030332
Received: 7 February 2021 / Revised: 24 February 2021 / Accepted: 1 March 2021 / Published: 4 March 2021
(This article belongs to the Section Nanomedicine and Nanotechnology)
Methotrexate (MTX), a compound originally used as an anticancer drug, has also found applications in a broad variety of autoimmune disorders thanks to its anti-inflammation and immunomodulatory functions. The broad application of MTX is anyway limited by its poor solubility in biological fluids, its poor bioavailability and its toxicity. In addition, encapsulating its original form in nanoformulation is very arduous due to its considerable hydrophobicity. In this work, two strategies to efficiently encapsulate MTX into liposomal particles are proposed to overcome the limitations mentioned above and to improve MTX bioavailability. MTX solubility was increased by conjugating the molecule to two different compounds: DSPE and PEG. These two compounds commonly enrich liposome formulations, and their encapsulation efficiency is very high. By using these two prodrugs (DSPE-MTX and PEG-MTX), we were able to generate liposomes comprising one or both of them and characterized their physiochemical features and their toxicity in primary macrophages. These formulations represent an initial step to the development of targeted liposomes or particles, which can be tailored for the specific application MTX is used for (cancer, autoimmune disease or others). View Full-Text
Keywords: nanomedicine; drug delivery; methotrexate; prodrug; fitting and release profile; liposomes nanomedicine; drug delivery; methotrexate; prodrug; fitting and release profile; liposomes
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MDPI and ACS Style

Di Francesco, V.; Di Francesco, M.; Decuzzi, P.; Palomba, R.; Ferreira, M. Synthesis of Two Methotrexate Prodrugs for Optimizing Drug Loading into Liposomes. Pharmaceutics 2021, 13, 332. https://doi.org/10.3390/pharmaceutics13030332

AMA Style

Di Francesco V, Di Francesco M, Decuzzi P, Palomba R, Ferreira M. Synthesis of Two Methotrexate Prodrugs for Optimizing Drug Loading into Liposomes. Pharmaceutics. 2021; 13(3):332. https://doi.org/10.3390/pharmaceutics13030332

Chicago/Turabian Style

Di Francesco, Valentina, Martina Di Francesco, Paolo Decuzzi, Roberto Palomba, and Miguel Ferreira. 2021. "Synthesis of Two Methotrexate Prodrugs for Optimizing Drug Loading into Liposomes" Pharmaceutics 13, no. 3: 332. https://doi.org/10.3390/pharmaceutics13030332

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