Mayson H Alkhatib ,
Norah S Alkhayyal
Department of Biochemistry, College of Science, King Abdulaziz University, PO Box 42801, Jeddah 21551, Saudi Arabia;
For correspondence:- Mayson Alkhatib
Email: mhalkhatib@kau.edu.sa Tel:+966599240526
Received: 1 February 2013
Accepted: 8 January 2014
Published: 20 February 2014
Citation:
Alkhatib MH, Alkhayyal NS.
Cytotoxicity of Gemcitabine-Loaded-Microemulsions in Breast and Colon Cancer Cells. Trop J Pharm Res 2014; 13(2):217-224
doi:
10.4314/tjpr.v13i2.8
© 2014 The authors.
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Abstract
Purpose: To evaluate the antitumor activity of gemcitabine (GEM), incorporated in microemulsions with varying surfactant-to-oil (S/O) ratio, against MCF-7 breast cancer cells and HCT 116 colon cancer cells.
Methods: The microemulsion formulations consisted of Tween 80, Span 20, isopropyl myristate (IPM) and aqueous ethanol (40 %). Anticancer assessment involved determination of hemolysis activity, screening for cytotoxicity using sulphorhodamine B assay and determination of the mechanism of cell death using light microscope and ApopNexin FITC apoptosis detection kit.
Results: Hemolysis activity of all the microemulsion formulations, either blank or drug-loaded, was significantly less than that of GEM solution. On average, MCF-7 cell viability significantly (p < 0.05) decreased from 38.53 ± 6.04 to 30.1 ± 4.66 % when the administered microemulsion concentration in modified eagle medium (MEM), increased from 0.03 to 0.3 % v/v but significantly (p < 0.05) increased by 1.4-fold when exposed to GEM solution at equivalent concentrations. In contrast, the cytotoxicity of the microemulsion formulation against HCT116 cells was similar to that of 0.03 % v/v GEM solution but greater than that of GEM solution by 1.5-fold when their concentration in MEM increased to 0.3 %v/v. Microscopic studies show that the microemulsions stimulated apoptosis in MCF-7 and HCT116 cell within 48 h and at low concentration (0.03 %v/v).
Conclusion: Microemulsion formulations improved the efficacy of GEM and induced apoptosis in MCF-7 and HCT116 cells.
Keywords: Apoptosis, MCF-7 breast cancer cells, HCT116 colon cancer cells, Hemolysis, Sulphorhodamine B assay, Microemulsion