Studies on Preparation and Evaluation of Soluble 1:1 Stoichiometric Curcumin Complex for Colorectal Cancer Treatment

Abstract

This study investigates the complex of curcumin (CMN), which has enhanced solubility and hence, higher cytotoxicity compared to free CMN. Insilco molecular modelling and phase solubility (PS) studies were performed with the drug and carriers for interaction. The complex was characterized by in vitro drug release, FT-IR, PXRD, TGA, DSC, SEM, DLS, and functionalized dyeing test. The result showed that the CMN-PEG6000 complex produced significant properties of solubility (≈ 190 folds) and dissolution (80.68 % at 30 min), with stability constants equivalent to 309 and 377 M-1 at 25 and 37 °C, respectively. It exhibited AL type of isotherm indicating 1:1 stoichiometry. The result from the in vitro cytotoxicity showed that 50 % inhibition (IC50) was achieved on the SW480 and Caco-2 cells at an amount of complex that was considerably lesser than free CMN. Apoptosis study showed that the cells underwent cell death mainly by apoptosis with a small number by necrosis.
 HIGHLIGHTS
 
 Enhanced curcumin solubility up to 190 fold higher than pure curcumin was investigated
 The phase solubility results of curcumin range from 5.7×10-4 M-1 and 7.8×10-4 M-1 at 25 and 37 °C, respectively
 First time of novel dyeing test was performed with complex of curcumin, signified its solubility
 This study provides useful approach for obtaining curcumin products with maximum aqueous solubility
 
 GRAPHICAL ABSTRACT

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

“…The broad endothermic peak at 244.68°C in the physical mixture of DoN and Kollidon corresponds to the melting of DoN. Broadening of peak and reduction in temperature indicate decrease in crystallinity [ 28 ]. Broadened endothermic peak at reduced temperature of 25°C confirms decrease in crystallinity of DoN.…”

Development of Atorvastatin Calcium Biloaded Capsules for Oral Administration of Hypercholesterolemia

“…The XRPD data were collected for the pure drugs, immediate and sustained release formulations in order to investigate any changes in physical form after development process ( Figure 6(b) ). The X-ray diffractogram of ATR shows sharp and intense peaks at diffraction angles (2 θ ) of 16.88, 18.97, 19.12, 21.49, 23.20, and 26.25°, suggesting a typical crystalline pattern, but ATN in nanoparticles shows few peaks at 16.96, 18.36, 19.08, 23.22, and 42.43° with low intensity [ 10 ]. This proves that the crystallinity of ATR decreases as most of the drug gets converted to an amorphous form.…”

“…The sealed flasks were agitated on a rotary shaker for 24 h at 37°C and equilibrated for 2 days. An aliquot was passed through a 0.1 μ m membrane filter (Millipore Corporation), and the filtrate was suitably diluted and analyzed on a UV spectrophotometer at 245 nm [ 10 ]. The mean results of triplicate measurements and the standard deviation were reported.…”

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

“…A TECHNAI 10 transmission electron microscope (TEM) is an efficient to produce better resolution, and operating at 200 kV was used to analyze the morphology and surface structure of the FU-NE [18] (Technai 10, Philips). A drop of NE was placed to the film grid and inspected after it dried to make the TEM observations.…”