Abstract
Microemulsions combine the advantages of emulsions with those of nanocarriers, overcoming the stability problems of the former and providing facile scalable systems with compartments adequate for high drug loadings. Recently, microemulsions are gaining attention in the formulation of anticancer drugs not only for topical treatment, but also for systemic delivery as well as for the development of theranostic systems. The aim of this paper is two-fold. First, an updated review about general features, preparation, characterization and pharmaceutical applications, with a special focus on colorectal cancer, is provided. Second, a case study of formulation of methotrexate in microemulsions is presented. Various essential oils (menthol, trans-anethole, α-tocopherol) and surfactants (TPGS-1000, Maxemul 6112, Noigen RN-20) were investigated for the preparation of o/w microemulsions for the delivery of methotrexate, and the ability of methotrexate-loaded microemulsions to inhibit cancer cell growth was then evaluated. Disregarding the surfactants used, menthol and trans-anethole led to cytotoxic microemulsions, whereas α-tocopherol based-formulations induced cell proliferation. These findings highlight the role that the oily component may play in the efficacy and safety of the microemulsions.
Keywords: Antitumor therapy, colorectal cancer, essential oils, methotrexate formulation, microemulsion, phase diagrams.
Mini-Reviews in Medicinal Chemistry
Title:Microemulsions for Colorectal Cancer Treatments. General Considerations and Formulation of Methotrexate
Volume: 16 Issue: 6
Author(s): Sergio E. Flores, M. Isabel Rial-Hermida, Jorge C. Ramirez, Alejandro Pazos, Angel Concheiro, Carmen Alvarez-Lorenzo and René D. Peralta
Affiliation:
Keywords: Antitumor therapy, colorectal cancer, essential oils, methotrexate formulation, microemulsion, phase diagrams.
Abstract: Microemulsions combine the advantages of emulsions with those of nanocarriers, overcoming the stability problems of the former and providing facile scalable systems with compartments adequate for high drug loadings. Recently, microemulsions are gaining attention in the formulation of anticancer drugs not only for topical treatment, but also for systemic delivery as well as for the development of theranostic systems. The aim of this paper is two-fold. First, an updated review about general features, preparation, characterization and pharmaceutical applications, with a special focus on colorectal cancer, is provided. Second, a case study of formulation of methotrexate in microemulsions is presented. Various essential oils (menthol, trans-anethole, α-tocopherol) and surfactants (TPGS-1000, Maxemul 6112, Noigen RN-20) were investigated for the preparation of o/w microemulsions for the delivery of methotrexate, and the ability of methotrexate-loaded microemulsions to inhibit cancer cell growth was then evaluated. Disregarding the surfactants used, menthol and trans-anethole led to cytotoxic microemulsions, whereas α-tocopherol based-formulations induced cell proliferation. These findings highlight the role that the oily component may play in the efficacy and safety of the microemulsions.
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Cite this article as:
Flores E. Sergio, Rial-Hermida Isabel M., Ramirez C. Jorge, Pazos Alejandro, Concheiro Angel, Alvarez-Lorenzo Carmen and Peralta D. René, Microemulsions for Colorectal Cancer Treatments. General Considerations and Formulation of Methotrexate, Mini-Reviews in Medicinal Chemistry 2016; 16 (6) . https://dx.doi.org/10.2174/1389557515666150909142920
DOI https://dx.doi.org/10.2174/1389557515666150909142920 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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