Enhanced Doxorubicin Delivery in Folate-Overexpressed Breast Cancer Cells Using Mesoporous Carbon Nanospheres

Kandasamy Vinothini; Sathish Sundar Dhilip Kumar; Heidi Abrahamse; Mariappan Rajan

doi:10.1021/acsomega.1c04820

Enhanced Doxorubicin Delivery in Folate-Overexpressed Breast Cancer Cells Using Mesoporous Carbon Nanospheres

ACS Omega. 2021 Dec 10;6(50):34532-34545. doi: 10.1021/acsomega.1c04820. eCollection 2021 Dec 21.

Authors

Kandasamy Vinothini¹, Sathish Sundar Dhilip Kumar², Heidi Abrahamse², Mariappan Rajan¹

Affiliations

¹ Biomaterials in Medicinal Chemistry Laboratory, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625021 Tamil Nadu, India.
² Laser Research Centre, Faculty of Health Sciences, University of Johannesburg, Johannesburg 2028, South Africa.

Abstract

Nanoparticle-based drug delivery reveals the safety and effectiveness and avoids premature drug release from the nanocarrier. These nanoparticles improve the bioavailability and stability of the drug against chemical and enzymatic degradation and facilitate targeted drug delivery. Herein, targeted folic acid-conjugated oxidized mesoporous carbon nanospheres (Ox-MPCNPs) were successfully fabricated and developed as antitumoral doxorubicin delivery for targeted breast cancer therapy. Fourier transform infrared spectroscopy studies confirmed that the doxorubicin was successfully bound on the Ox-MPCNP through hydrogen bonding and π-π interactions. X-ray diffraction studies showed that the synthesized doxorubicin-loaded Ox-MPCNP is semi-crystalline. The surface morphology of the synthesized doxorubicin-loaded Ox-MPCNP (DOX/Ox-MPCNP-Cys-PAsp-FA) was studied by scanning electron microscopy and high-resolution transmission electron microscopy, which demonstrates a sphere-shaped morphology. The cytotoxic effects of DOX/Ox-MPCNP-Cys-PAsp-FA were studied in MCF-7 breast cancer cells using the CytoTox96 assay kit. The study confirmed the cytotoxic effects of the synthesized nanospheres in vitro. Moreover, DOX/Ox-MPCNP-Cys-PAsp-FA-treated cells displayed efficient cell apoptosis and cell death in flow cytometry analysis. The mitochondrial fragmentation and nucleus damages were further confirmed by fluorescence microscopy. Thus, the approach used to construct the DOX/Ox-MPCNP-Cys-PAsp-FA carrier provides excellent opportunities for the targeted treatment of breast cancer.