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Reduction-Triggered Doxorubicin Delivery by Self-Assembled Nanospheres of Lipoylated Caffeine

Kumar, K and Kumar Shyamlal, BR and Verma, R and Kondaiah, P and Chaudhary, S (2020) Reduction-Triggered Doxorubicin Delivery by Self-Assembled Nanospheres of Lipoylated Caffeine. In: ChemMedChem, 15 (9). pp. 733-737.

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Official URL: https://doi.org/10.1002/cmdc.202000070


This study reports a new amphiphilic bioconjugate (CAFF-LA) derived from the lipoylation of a hydroxyethyl derivative of caffeine. In water, CAFF-LA self-assembles into nanospheres with an average size of 155 nm, as evidenced from dynamic light scattering and electron microscopy studies. The nanospheres are stable in serum and could be disintegrated upon exposure to the reducing environment of dithiothreitol (DTT; 10 mM) and glutathione (GSH; 10 mM). These nanospheres easily encapsulate the chemotherapy medication, doxorubicin (DOX), and demonstrate an efficacious transport into doxorubicin-resistant cervical cancer (HeLa) cells, wherein a marked induction in apoptosis and significantly lower IC50 have been observed when compared to that of free drug. The in vitro assessment of cell viability and hemocompatibility present these nanospheres as potentially safe and efficient intracellular reduction stimulus-responsive drug-delivery vehicles.

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: ABC transporter subfamily B; amphophile; caffeine; dithiothreitol; doxorubicin; glutathione; nanosphere; antineoplastic antibiotic; caffeine; doxorubicin; drug carrier; nanosphere, apoptosis; Article; blood compatibility; cancer resistance; cell viability; comparative study; cytotoxicity; dispersity; doxorubicin-resistant cell line; drug delivery system; electron microscopy; female; gene overexpression; HeLa cell line; hemolysis; human; human cell; hydrodynamics; IC50; in vitro study; internalization; lipoylation; MDA-MB-231 cell line; nanoencapsulation; nanopharmaceutics; particle size; photon correlation spectroscopy; priority journal; reduction (chemistry); cell proliferation; cell survival; chemical structure; chemistry; drug delivery system; drug effect; drug screening; lipoylation; oxidation reduction reaction; surface property, Antibiotics, Antineoplastic; Apoptosis; Caffeine; Cell Proliferation; Cell Survival; Doxorubicin; Drug Carriers; Drug Delivery Systems; Drug Screening Assays, Antitumor; HeLa Cells; Humans; Lipoylation; Molecular Structure; Nanospheres; Oxidation-Reduction; Particle Size; Surface Properties
Department/Centre: Division of Biological Sciences > Molecular Reproduction, Development & Genetics
Date Deposited: 06 Feb 2023 09:14
Last Modified: 06 Feb 2023 09:14
URI: https://eprints.iisc.ac.in/id/eprint/79905

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