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Doxorubicin conjugated carbon dots as a drug delivery system for human breast cancer therapy.

ABSTRACT: OBJECTIVES:Carbon dots (CDs) are one of the most promising carbon-based materials in bioimaging and drug/gene delivery applications. In this study, we have attempted to study the drug carrying capacity of highly fluorescent CDs for delivery of doxorubicin (DOX) and investigate the therapeutic activity of the CDs-DOX drug delivery system. MATERIALS AND METHODS:Carbon dots were synthesized by means of a hydrothermal approach with mixing citric acid and ethylenediamine. The properties of CDs were characterized in respects of spectral property, zeta potential, particle morphology and chemical composition. The drug loading efficiency (DLE) and release profile of CDs-DOX were determined by a fluorescence spectrophotometer. We investigated the cellular toxicity and pharmaceutical activity of CDs and CDs-DOX in L929 cells and MCF-7 cells by the CCK-8 assay. We also studied the cellular uptake of CDs-DOX with the methods of confocal microscopy and flow cytometry. In addition, the effect of CDs-DOX on cell apoptosis was assessed by flow cytometry. RESULTS:The obtained CDs possessed good biocompatibility and showed a potential capacity of promoting proliferation. DOX was successfully conjugated to CDs through electrostatic interaction, and the results of the DLE and loading content (DLC) suggested a relatively high drug loading capacity of CDs. Compared with free DOX, the CDs-DOX complex had a higher cellular uptake and better anti-tumour efficacy on MCF-7 cells. CONCLUSIONS:The results of this study indicated that the CDs-DOX drug delivery system had a potential value in cancer chemotherapeutic application.

SUBMITTER: Kong T

PROVIDER: S-EPMC6528846 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature

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Doxorubicin conjugated carbon dots as a drug delivery system for human breast cancer therapy.

Kong Tingting T Hao Liying L Wei Yuanyuan Y Cai Xiaoxiao X Zhu Bofeng B

Cell proliferation 20180724 5

<h4>Objectives</h4>Carbon dots (CDs) are one of the most promising carbon-based materials in bioimaging and drug/gene delivery applications. In this study, we have attempted to study the drug carrying capacity of highly fluorescent CDs for delivery of doxorubicin (DOX) and investigate the therapeutic activity of the CDs-DOX drug delivery system.<h4>Materials and methods</h4>Carbon dots were synthesized by means of a hydrothermal approach with mixing citric acid and ethylenediamine. The propertie ...[more]

PMID: 30039515

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Project description:Doxorubicin (Dox) is an anthracycline chemotherapeutic agent used to treat breast, leukemia, and lymphoma malignancies. However, cardiotoxicity and inherent acquired resistance are major drawbacks, limiting its clinical application. We have previously shown that cyclic peptide [WR]9 containing alternate tryptophan (W) and arginine (R) residues acts as an efficient molecular transporter. An amphiphilic cyclic peptide containing a lysine (K) residue and alternative W and R was conjugated through a free side chain amino group with Dox via a glutarate linker to afford [(WR)8WKβA]-Dox conjugate. Antiproliferative assays were performed in different cancer cell lines using the conjugate and the corresponding physical mixture of the peptide and Dox to evaluate the effectiveness of synthesized conjugate compared to the parent drug alone. [(WR)8WKβA]-Dox conjugate showed higher antiproliferative activity at 10 µM and 5 µM than Dox alone at 5 μM. The conjugate inhibited the cell viability of ovarian adenocarcinoma (SK-OV-3) by 59% and the triple-negative breast cancer cells MDA-MB-231 and MCF-7 by 71% and 77%, respectively, at a concentration of 5 μM after 72 h of incubation. In contrast, Dox inhibited the proliferation of SK-OV-3, MDA-MB-231, and MCF-7 by 35%, 63%, and 57%, respectively. Furthermore, [(WR)8WKβA]-Dox conjugate (5 µM) inhibited the cell viability of Dox-resistant cells (MES-SA/MX2) by 92%, while the viability of cells incubated with free Dox was only 15% at 5 μM. Confocal microscopy images confirmed the ability of both Dox conjugate and the physical mixture of the peptide with the drug to deliver Dox through an endocytosis-independent pathway, as the uptake was not inhibited in the presence of endocytosis inhibitors. The stability of Dox conjugate was observed at different time intervals using analytical HPLC when the conjugate was incubated with 25% human serum. Half-life (t1/2) for [(WR)8WKβA]-Dox conjugate was (∼6 h), and more than 80% of the conjugate was degraded at 12 h. The release of free Dox was assessed intracellularly using the CCRF-CEM cell line. The experiment demonstrated that approximately 100% of free Dox was released from the conjugate intracellularly within 72 h. These data confirm the ability of the cyclic cell-penetrating peptide containing tryptophan and arginine residues as an efficient tool for delivery of Dox and for overcoming resistance to it.

Dataset Information

Doxorubicin conjugated carbon dots as a drug delivery system for human breast cancer therapy.

Publications

Doxorubicin conjugated carbon dots as a drug delivery system for human breast cancer therapy.

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