Oil-In-Water Microemulsions as Hosts for Benzothiophene-Based Cytotoxic Compounds: An Effective Combination
AbstractTargeted 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
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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.
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(2):13.Chicago/Turabian Style
Theochari, Ioanna; Papadimitriou, Vassiliki; Papahatjis, Demetris; Assimomytis, Nikos; Pappou, Efthimia; Pratsinis, Harris; Xenakis, Aristotelis; Pletsa, Vasiliki. 2018. "Oil-In-Water Microemulsions as Hosts for Benzothiophene-Based Cytotoxic Compounds: An Effective Combination." Biomimetics 3, no. 2: 13.
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