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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Mitochondria as a Therapeutic Target in Metabolic Disorders
Mitochondria are the primary site of adenosine triphosphate (ATP) production in mammalian cells. Moreover, these organelles are an important source of reactive oxygen and nitrogen species in virtually any nucleated cell type. The modulation of a myriad of cellular signaling pathways depends on the mitochondrial physiology. Mitochondrial dysfunction is observed ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Membrane Transporters as Determinants of the Pharmacology of Platinum Anticancer Drugs
Current Cancer Drug Targets Pharmacokinetics of 3’-O-Retinoyl-5-fluoro-2’-deoxyuridine (RFUdR), a Dual Acting Mutually Masking Prodrug, and Its Metabolites in Tumor Bearing Mice
Current Drug Delivery Complications of Anti-Vascular Endothelial Growth Factor Drugs
Current Drug Therapy Developments in Synthesis of the Anti-inflammatory Drug, Celecoxib: A Review
Recent Patents on Inflammation & Allergy Drug Discovery In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH<sub>2</sub>Ph)]Br
Anti-Cancer Agents in Medicinal Chemistry Search for New and Novel Chemotherapeutics for the Treatment of Human Malignancies
Mini-Reviews in Medicinal Chemistry Nampt/Visfatin/PBEF: A Functionally Multi-faceted Protein with a Pivotal Role in Malignant Tumors
Current Pharmaceutical Design CD20-based Immunotherapy of B-cell Derived Hematologic Malignancies
Current Cancer Drug Targets Lipid-Based Vectors for Therapeutic mRNA-Based Anti-Cancer Vaccines
Current Pharmaceutical Design Advances in Clinical Study of Curcumin
Current Pharmaceutical Design Synergistic Two-Way Interactions of Dietary Polyphenols and Dietary Components on the Gut Microbial Composition: Is There a Positive, Negative, or Neutralizing Effect in the Prevention and Management of Metabolic Diseases?
Current Protein & Peptide Science Cetuximab: Its Use in Combination with Radiation Therapy and Chemotherapy in the Multimodality Treatment of Head and Neck Cancer
Recent Patents on Anti-Cancer Drug Discovery Editorial [Hot Topic: The Impact of Microbiota and Cytokines on Inflammatory Bowel Disease (Executive Editors: Osamu Kanauchi and Keiichi Mitsuyama)]
Current Pharmaceutical Design Tumor Growth-Promoting Properties of Macrophage Migration Inhibitory Factor
Current Pharmaceutical Design Synthesis and Characterization of a New Benzoindole Derivative with Apoptotic Activity Against Colon Cancer Cells
Current Pharmaceutical Design Entropy Model for Multiplex Drug-Target Interaction Endpoints of Drug Immunotoxicity
Current Topics in Medicinal Chemistry Cancer Pharmacogenetics: The Move from Pharmacokinetics to Pharmacodynamics
Current Pharmacogenomics Marine Derived Anticancer Drugs Targeting Microtubule
Recent Patents on Anti-Cancer Drug Discovery Omics Derived Networks in Bacteria
Current Bioinformatics Aurora-B Kinase Inhibitors for Cancer Chemotherapy
Mini-Reviews in Medicinal Chemistry