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Biomimetics 2018, 3(2), 13; https://doi.org/10.3390/biomimetics3020013

Oil-In-Water Microemulsions as Hosts for Benzothiophene-Based Cytotoxic Compounds: An Effective Combination

1
Institute of Biology, Medicinal Chemistry & Biotechnology, National Hellenic Research Foundation, 48 Vassileos Constantinou Avenue, 11635 Athens, Greece
2
Laboratory of Cell Proliferation and Ageing, Institute of Biosciences and Applications, National Centre of Scientific Research “Demokritos”, 11635 Athens, Greece
*
Author to whom correspondence should be addressed.
Received: 7 May 2018 / Revised: 7 June 2018 / Accepted: 12 June 2018 / Published: 16 June 2018
(This article belongs to the Special Issue Selected Papers from NanoBio&Med 2017)
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Abstract

Targeted delivery of chemotherapeutics in order to overcome side effects and enhance chemosensitivity remains a major issue in cancer research. In this context, biocompatible oil-in-water (O/W) microemulsions were developed as matrices for the encapsulation of DPS-2 a benzothiophene analogue, exhibiting high cytotoxicity in various cancer cell lines, among them the MW 164 skin melanoma and Caco-2 human epithelial colorectal adenocarcinoma cell lines. The microemulsion delivery system was structurally characterized by dynamic light scattering (DLS) and electron paramagnetic resonance (EPR) spectroscopy. The effective release of a lipophilic encapsulated compound was evaluated via confocal microscopy. The cytotoxic effect, in the presence and absence of DPS-2, was examined through the thiazolyl blue tetrazolium bromide (MTT) cell proliferation assay. When encapsulated, DPS-2 was as cytotoxic as when dissolved in dimethyl sulfoxide (DMSO). Hence, the oil cores of O/W microemulsions were proven effective biocompatible carriers of lipophilic bioactive molecules in biological assessment experiments. Further investigation through fluorescence-activated cell sorting (FACS) analysis, comet assay, and Western blotting, revealed that DPS-2, although non-genotoxic, induced S phase delay accompanied by cdc25A degradation and a nonapoptotic cell death in both cell lines, which implies that this benzothiophene analogue is a deoxyribonucleic acid (DNA) replication inhibitor. View Full-Text
Keywords: microemulsions; drug delivery; electron paramagnetic resonance; DNA replication fork; mechanisms of cell death; chemotherapy microemulsions; drug delivery; electron paramagnetic resonance; DNA replication fork; mechanisms of cell death; chemotherapy
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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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Theochari, I.; Papadimitriou, V.; Papahatjis, D.; Assimomytis, N.; Pappou, E.; Pratsinis, H.; Xenakis, A.; Pletsa, V. Oil-In-Water Microemulsions as Hosts for Benzothiophene-Based Cytotoxic Compounds: An Effective Combination. Biomimetics 2018, 3, 13.

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