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Cytotoxic, Apoptotic and Genotoxic Effects of Lipid-Based and Polymeric Nano Micelles, an In Vitro Evaluation

1
Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Bezmialem Vakif University, Fatih, Istanbul 34093, Turkey
2
Department of Medical Biochemistry, Faculty of Medicine, Bezmialem Vakif University, Istanbul 34093, Turkey
3
Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, IL 60612, USA
4
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Bezmialem Vakif University, Fatih, Istanbul 34093, Turkey
*
Author to whom correspondence should be addressed.
Received: 4 December 2017 / Revised: 26 December 2017 / Accepted: 29 December 2017 / Published: 30 December 2017
(This article belongs to the Special Issue Nanoparticles Toxicity and Impacts on Biodiversity)
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Abstract

Self-assembly systems (SAS) mainly consist of micelles, and liposomes are the classes of Nano Drug Delivery Systems with superior properties compared to traditional therapeutics in targeting cancer tumors. All commercially available nano-formulations of chemotherapeutics currently consist of SAS. According to our knowledge, a specific toxicity comparison based on material differences has not yet been performed. The purpose of this study was to evaluate and compare the toxicity of two SAS consisting of Sterically Stabilized Micelles (SSM) made of a lipid-based amphiphilic distearoyl-sn-glycero-phosphatidylethanolamine-polyethylene glycol (PEG)-2000 and a polymeric micelle (PM) consisting of Y-shape amphiphilic block copolymer, synthesized using poly ε-caprolactone and PEG. The mechanism of cytotoxicity and genotoxicity of micelles on L-929 healthy mouse fibroblast cells was assessed using Sulforhodamine-B, WST-1, Acridine Orange/Ethidium Bromide and alkaline single-cell gel electrophoresis assays. Results showed that SSM in conc. of 40 mg/mL shows very low cytotoxicity at the end of 24, 48 and 72 h. The DNA damage caused by SSM was much lower than PM while the latter one showed significant toxicity by causing apoptosis with the ED50 value of 3 mg/mL. While the DNA damage caused by SSM was ignorable, some DNA chain breaks were detected on cells treated with PM. View Full-Text
Keywords: cytotoxicity; genotoxicity; lipid-based micelles; Nano Drug Delivery System; polymeric micelle; targeted cancer therapy cytotoxicity; genotoxicity; lipid-based micelles; Nano Drug Delivery System; polymeric micelle; targeted cancer therapy
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Bahadori, F.; Kocyigit, A.; Onyuksel, H.; Dag, A.; Topcu, G. Cytotoxic, Apoptotic and Genotoxic Effects of Lipid-Based and Polymeric Nano Micelles, an In Vitro Evaluation. Toxics 2018, 6, 7.

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