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
-
Transition Metal-Based Prodrugs for Anticancer Drug Delivery
Current Medicinal Chemistry Cellular Relationships of Testicular Germ Cell Tumors Determined by Partial Canonical Correlation Analysis of Gene Expression Signatures
Current Bioinformatics In Vivo Optical Imaging in Gene & Cell Therapy
Current Gene Therapy Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer
Current Radiopharmaceuticals The Molecular Mechanisms of TRAIL Resistance in Cancer Cells: Help in Designing New Drugs
Current Pharmaceutical Design Recent Patents on Thiazole Derivatives Endowed with Antitumor Activity
Recent Patents on Anti-Cancer Drug Discovery Using Pharmacologic Data to Plan Clinical Treatments for Patients with Peritoneal Surface Malignancy
Current Drug Discovery Technologies The Endocannabinoid System in the Cancer Therapy: An Overview
Current Medicinal Chemistry Emerging Concepts in the Analysis of Mitochondrial Genome Instability
Current Genomics An Overview of Targeting Legumain for Inhibiting Cancers
Current Pharmaceutical Design Preclinical and Clinical Studies of Novel Breast Cancer Drugs Targeting Molecules Involved in Protein Kinase C Signaling, the Putative Metastasis-Suppressor Gene Cap43 and the Y-box Binding Protein-1
Current Medicinal Chemistry Adhesion Molecules as Targets for the Treatment of Neoplastic Diseases
Current Pharmaceutical Design Theranostic Radiopharmaceuticals Targeting Cancer-Associated Fibroblasts
Current Radiopharmaceuticals Clinical Trials of Cancer Therapies Targeting Prostate-Specific Membrane Antigen
Reviews on Recent Clinical Trials MtDNA As a Cancer Marker: A Finally Closed Chapter?
Current Genomics Adenovirus-Based Cancer Gene Therapy
Current Gene Therapy The Significance of Meat in the Diet
Current Nutrition & Food Science Cdc42 Signaling Pathway Inhibition as a Therapeutic Target in Ras- Related Cancers
Current Medicinal Chemistry Nanoliposome is a Promising Carrier of Protein and Peptide Biomolecule for the Treatment of Cancer
Anti-Cancer Agents in Medicinal Chemistry Analysis of Oxaliplatin Resistance in Colorectal Cancer Cells by Combined Proteomics and Phosphoproteomic
Current Proteomics