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Efficacious Doxorubicin Delivery Using Glutathione-Responsive Hollow Non-phospholipid Vesicles Bearing Lipoyl Cholesterols

Kumar, K and Yadav, L and Kondaiah, P and Chaudhary, S (2019) Efficacious Doxorubicin Delivery Using Glutathione-Responsive Hollow Non-phospholipid Vesicles Bearing Lipoyl Cholesterols. In: ChemMedChem, 14 (18). pp. 1633-1640.

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Official URL: https://doi.org/10.1002/cmdc.201900335


In this study, we developed redox-sensitive vesicles using synthesised lipoyl cholesterol derivatives, a non-ionic surfactant and an optimum level of free cholesterol. Interestingly, concentration-dependent self-assembly was observed by scanning electron microscopy, wherein vesicles manifested as hollow spherical (at 0.15 mm) and triangular (0.50 mm). The redoxresponsive characteristics of the vesicles was probed in the presence of dithiothreitol; they underwent a clear increase in size as observed by dynamic light scattering measurements. These vesicles could easily encapsulate an anticancer drug, doxorubicin, and were observed to be stable in the presence of serum. They showed substantial release of the drug in response to biologically relevant stimulus, that is, glutathione. A toxicity assessment on HeLa and HepG2 cancer cells demonstrated activities of the drug-loaded vesicles comparable to that of free drug, whereas significantly enhanced toxicity and apoptotic induction were observed against drug-resistant HeLa cells, which was determined by studying the cellular internalisation of doxorubicin. © 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

Item Type: Journal Article
Publication: ChemMedChem
Publisher: John Wiley and Sons Ltd
Additional Information: The copyright for this article belongs to John Wiley and Sons Ltd
Keywords: cholesterol derivative; dithiothreitol; doxorubicin; glutathione; nonionic surfactant; thioctic acid; antineoplastic agent; cholesterol; doxorubicin; drug carrier; lipid, apoptosis; Article; conjugate; drug cytotoxicity; drug delivery system; drug release; drug-resistant cell line; encapsulation; female; fetal bovine serum; HeLa cell line; Hep-G2 cell line; human; human cell; internalization; photon correlation spectroscopy; priority journal; scanning electron microscopy; synthesis; cell proliferation; chemical structure; chemistry; dose response; drug effect; drug screening; particle size; porosity; structure activity relation; surface property; tumor cell culture, Antineoplastic Agents; Cell Proliferation; Cholesterol; Dose-Response Relationship, Drug; Doxorubicin; Drug Carriers; Drug Screening Assays, Antitumor; Glutathione; HeLa Cells; Hep G2 Cells; Humans; Lipids; Molecular Structure; Particle Size; Porosity; Structure-Activity Relationship; Surface Properties; Tumor Cells, Cultured
Department/Centre: Division of Biological Sciences > Molecular Reproduction, Development & Genetics
Date Deposited: 06 Jan 2023 04:40
Last Modified: 06 Jan 2023 04:40
URI: https://eprints.iisc.ac.in/id/eprint/78799

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