Formulation and Characterization of gallic acid and quercetin chitosan nanoparticles for sustained release in treating Colorectal Cancer

Cancer was ranked as the second leading cause of death, and colon cancer is recognized as third most common cancer worldwide with high morbidity and mortality. Chemotherapeutic drugs act on normal and cancerous cells similarly; therefore, they have various adverse side effects. The present study was undertaken synergistic effect of anticancer phytochemicals gallic acid isolated from amla fruit and quercetin isolated from peels of pomegranate fruit incorporated into chitosan have been used as nanoplatform for the targeted delivery to colorectal cancer.

The study was evaluated using cytotoxic assay such as MTT assay and in-vivo studies were performed on DMH induced colorectal cancer in Wistar rats. Identification of the biomolecules was performed by using different chromatographic and spectroscopic techniques, as 1H-NMR, GC-MS, LC-MS, and HPTLC. Characterization of chitosan (CS) nanoparticles carried out by using X-ray diffraction (XRD) Differential scanning calorimetry (DSC), Scanning Electron Microscope (SEM), entrapment efficiency and In vitro drug release confirmed successful encapsulation of biomolecules into nanoparticles. A significant change in aberrant crypt foci (ACF) in CS nanoparticles compared to polyherbal extract were observed, with a decrease in the colonic glutathione, catalase and superoxide dismutase levels and values differed significantly (P < 0.005).

Graphical abstract

The present study was undertaken synergistic effect of anticancer phytochemicals gallic acid isolated from amla fruit and quercetin isolated from peels of pomegranate fruit incorporated into chitosan have been used as nanoplatform for the targeted delivery to colorectal cancer. The study was evaluated using cytotoxic assay and in-vivo studies were performed on DMH induced colorectal cancer in Wistar rats. Identification of the biomolecules was performed by using different chromatographic and spectroscopic techniques. Characterization of chitosan (CS) nanoparticles carried out by using XRD, DSC, SEM entrapment efficiency and In-vitro drug release confirmed successful encapsulation of biomolecules into nanoparticles. A significant change in aberrant crypt foci in CS nanoparticles compared to polyherbal extract was observed, with a decrease in the colonic glutathione, catalase and superoxide dismutase levels.

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Article information: Poounima Patil, Suresh Killedar. Formulation and Characterization of gallic acid and quercetin chitosan nanoparticles for sustained release in treating Colorectal Cancer, Journal of Drug Delivery Science and Technology, 2021. https://doi.org/10.1016/j.jddst.2021.102523.

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