Preparation of Soluble Complex of Curcumin for the Potential Antagonistic Effects on Human Colorectal Adenocarcinoma Cells

Abstract

This study was designed to investigate the effects of curcumin (CMN) soluble complex (SC) prepared by melt casting (HM) and hot-melt extrusion (HME) technology. Phase solubility (PS) study, in silico molecular modeling, aqueous solubility, drug release, and physicochemical investigation including a novel dyeing test was performed to obtain an optimized complex by a central composite design (CCD). The results show that the HME-SC produces better improvements towards solubility (0.852 ± 0.02), dissolution (91.87 ± 0.21 % at 30 min), with an ideal stability constant (309 and 377 M−1 at 25 and 37 °C, respectively) and exhibits AL type of isotherm indicating 1:1 stoichiometry. Intermolecular hydrogen bonding involves the formation of SC, which does not undergo any chemical modification, followed by the complete conversion of the amorphous form which was identified by XRD. The in vitro cytotoxicity showed that IC50 was achieved in the SW480 (72 µM.mL−1) and Caco-2 (40 µM.mL−1) cells while that of pure CMN ranged from 146 to 116 µM/mL−1. Apoptosis studies showed that cell death is primarily due to apoptosis, with a low rate of necrosis. In vivo toxicity, confirmed by the zebrafish model, exhibited the safety of the HME-SC. In conclusion, the HME-SC potentially enhances the solubility and cytotoxicity to the treatment of colorectal cancer (CRC).

Ameliorated Stomach Specific Floating Microspheres for Emerging Health Pathologies Using Polymeric Konjac Glucomannan-Based Domperidone

“…The dissolution studies on pure DoN, PM, and SD (equivalent to 10 mg of DoN) was supported out by USP paddle apparatus (type II) by 500 mL dissolution medium (distilled water and 0.1 N HCL). Rotation speed was 100 rpm and temperature ( T ) was maintained 37 ± 1°C [ 13 ]. 5 mL sample was removed at regular intervals (30, 60, 90, 120, 150, 180, and 210 min), and aliquot was withdrawn and replaced with equal volume of fresh dissolution medium, filtered, and analyzed, using double-beam UV spectrophotometer at 284 nm.…”

Curcumin Plant for Colorectal Cancer Prediction and Prevention Using In Silico Molecular Analysis; HOT-MELT Extrusion

“…From 20 to 300°C, the sample was heated at a rate of 10°C·min −1 . With the pure drug and complexes, the enthalpy changes were computed [ 21 ].…”

An Ideal Approach for Enhancing 5-Fluorouracil Anticancer Efficacy by Nanoemulsion for Cytotoxicity against a Human Hepatoma Cell Line (HepG2 Cells)

“…The FU-NEs have the ability to deliver the medicine in a regulated manner, as demonstrated in this study. As a result of the improved solubility of FU, continuous/uninterrupted drug release over a lengthy period of time may be obtained [27].…”