PloS one, 2015-06, Vol.10 (6), p.e0130555-e0130555
2015
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- Autor(en) / Beteiligte
- Titel
- Nanomicellar Formulation of Clotrimazole Improves Its Antitumor Action toward Human Breast Cancer Cells
- Ist Teil von
- PloS one, 2015-06, Vol.10 (6), p.e0130555-e0130555
- Ort / Verlag
- United States: Public Library of Science
- Erscheinungsjahr
- 2015
- Quelle
- EZB-FREE-00999 freely available EZB journals
- Beschreibungen/Notizen
- Although demonstrated as a selective anticancer drug, the clinical use of clotrimazole (CTZ) is limited due to its low solubility in hydrophilic fluids. Thus, we prepared a water-soluble nanomicellar formulation of CTZ (nCTZ) and tested on the human breast cancer cell line MCF-7 biology. CTZ was nanoencapsulated in tween 80 micelles, which generated nanomicelles of, approximately, 17 nm of diameter. MCF-7 cells were treated with nCTZ and unencapsulated DMSO-solubilized drug (sCTZ) was used for comparison. After treatment, the cells were evaluated in terms of metabolism, proliferation, survival and structure. We found that nCTZ was more efficient than sCTZ at inhibiting glycolytic and other cytosolic and mitochondrial enzymes. Moreover, this increased activity was also observed for lactate production, intracellular ATP content, ROS production and antioxidant potential. As a consequence, nCTZ-treated MCF-7 cells displayed alterations to the plasma membrane, mitochondria and the nucleus. Finally, nCTZ induced both apoptosis and necrosis in MCF-7 cells. MCF-7 cells are more sensible to nCTZ than to sCTZ. This was especially evident on regard to antioxidant potential, which is an important cell defense against drugs that affect cell metabolism. Moreover, this water-soluble formulation of CTZ strengths its potential use as an anticancer medicine.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1932-6203eISSN: 1932-6203DOI: 10.1371/journal.pone.0130555Titel-ID: cdi_plos_journals_1690399995
- Format
- –
- Schlagworte
- Adenosine Triphosphate - metabolism, Analysis, Antifungal agents, Antineoplastic Agents - chemistry, Antineoplastic Agents - pharmacology, Antioxidants, Antioxidants - chemistry, Antioxidants - pharmacology, Apoptosis, Apoptosis - drug effects, Breast cancer, Breast Neoplasms - drug therapy, Breast Neoplasms - metabolism, Cancer, Cell division, Cell growth, Cell Line, Tumor, Cell Membrane - drug effects, Cell proliferation, Cell Proliferation - drug effects, Cell survival, Chemistry, Pharmaceutical - methods, Chemotherapy, Clotrimazole, Clotrimazole - chemistry, Clotrimazole - pharmacology, Computational fluid dynamics, Drug metabolism, Drugs, Enzymes, Female, Glycolysis, Glycolysis - drug effects, Humans, Kinases, Lactates, Lactic acid, Lactic Acid - metabolism, MCF-7 Cells, Melanoma, Metabolism, Metabolites, Micelles, Microemulsions, Mitochondria, Mitochondria - drug effects, Mitochondria - metabolism, Mitochondrial DNA, Nanoparticles, Nanoparticles - administration & dosage, Nanoparticles - chemistry, Nuclei, Nuclei (cytology), Particle Size, Pharmaceuticals, Physiological aspects, Reactive Oxygen Species - metabolism, Solubility, Surface active agents, Surfactants, Water chemistry