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Capsanthin-Loaded Micelles: Preparation, Characterization and in vitro Evaluation of Cytotoxicity Using MDA-MB-231 Breast Cancer Cell Line

Velmurugan Shanmugham*orcid tiny and Ravi Subbanorcid tiny

Department of Chemistry, Karpagam Academy of Higher Education, Salem-Kochi Highway, Eachanari, 641 021 Coimbatore, India

Article history:

Received: 4 July 2021

Accepted: 11 April 2022

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Key words:

capsanthin; breast cancer; triple negative breast cancer cell line; micelles; water solubility; bioavailability


Research background. Breast cancer is one of the most common cancers and remains a major cause of morbidity and mortality among women worldwide. In developed nations, breast cancer as a multifactorial disease is a major health concern, and its incidence is constantly rising in low and middle-income countries. Numerous studies have demonstrated that phytochemicals such as carotenoids inhibit breast cancer growth and induce apoptosis. We recently enhanced the aqueous solubility of capsanthin by encapsulating in diosgenin polyethylene glycol succinate, a novel non-ionic surfactant. Thus, this study aims to evaluate the cytotoxicity of aqueous soluble capsanthin-loaded micelles in MDA-MB-231 cells in vitro through MTT assay.

Experimental approach. In the current study, capsanthin, a hydrophobic carotenoid, is extracted from the fruits of Capsicum annuum. Capsanthin-loaded diosgenin polyethylene glycol succinate-1000 (Cap-DPGS-1000) micelles were prepared from capsanthin extract (CAP) and diosgenin polyethylene glycol succinate 1000 (DPGS-1000) using the solid dispersion method. The capsanthin extract and Cap-DPGS-1000 were characterized by UV–visible spectroscopy, high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), particle size distribution, polydispersity, and scanning electron microscopy (SEM). The cytotoxicity of CAP and Cap-DPGS-1000 on a human triple-negative breast cancer cell line (MDA-MB-231) was performed to check the cell viability, proliferation, and cytotoxicity effects. 

Results and conclusions. The aqueous solubility of encapsulated Cap-DPGS-1000 is greatly enhanced and leads to an increased scope for localized drug delivery, a better delivery option for treating residual cancer tumors. The encapsulated capsanthin showed a sustained release in simulated intestinal fluid (pH=6.8). Our research proposes a sustained drug delivery system that ensures effective and controlled release to the affected site. The characterization data revealed no change in structure and functional groups in the encapsulated capsanthin. The IC50 value of the Cap-DPGS-1000 micelles against MDA-MB-231 breast cancer cells was (3.10±1.09) μg/mL, which is much lower than capsanthin extract (81.06±1.51) μg/mL. Capsanthin extract and capsanthin-loaded Cap-DPGS-1000 are promising drug candidates to induce apoptosis and increase reactive oxygen species (ROS) in cancer cells. 

Novelty and scientific contribution. The result shows the cytotoxic effect of capsanthin and capsanthin-loaded micelles on MDA-MB-231 cell line for the first time. Capsanthin from Capsicum annuum showed remarkable cytotoxic effect on the triple negative MDA-MB-231 cell line. 

*Corresponding author:

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