A Hydroxypropyl Methylcellulose-Based Solid Dispersion of Curcumin with Enhanced Bioavailability and Its Hepatoprotective Activity

Abstract

Curcumin is a polyphenol compound derived from the rhizomes of Curcuma longa that exhibits antioxidant, anti-inflammatory, anticancer, and antimicrobial properties. However, its low solubility in aqueous solutions, low absorption following oral administration, and rapid degradation limit its use as a functional food material. In this study, a hydroxypropyl methylcellulose-based solid dispersion of curcumin (DW-CUR 20) was prepared and its bioavailability was evaluated. In addition, its therapeutic efficacy as a hepatoprotective agent was investigated using the model of tert-butyl hydroperoxide (t-BHP)-induced hepatocyte damage. The rat plasma pharmacokinetic study showed that the oral curcumin bioavailability of DW-CUR 20 significantly increased compared to that of non-formulated curcumin. DW-CUR 20 showed a concentration-dependent hepatocyte protective effect on t-BHP-induced HepG2 cells. DW-CUR 20 inhibited the release of lactate dehydrogenase and decreased apoptosis-related proteins such as Poly (ADP-ribose) polymerase, cleaved caspase-7 and cleaved caspase-8 on t-BHP-treated HepG2 cells. These findings suggest that DW-CUR 20 could be a promising formulation for enhancing the therapeutic efficiency of curcumin and for improving the safety.

Therapeutic Applications of Solid Dispersions for Drugs and New Molecules: In Vitro and In Vivo Activities

“…SDs of CM prepared using HPMC as the polymer have been reported by Shin et al [ 48 ], who studied their possible hepatoprotective action in HepG2 cells treated with tert-butyl hydroperoxide (t-BHP) as a hepatotoxic agent. The survival rate of cells, which in the presence of t-BHP was about 40%, significantly increased after treatment with DSs-CM at concentrations of 10, 20 and 40 µg/mL compared to the treatment with CM alone at equivalent concentrations (2, 4 and 8 µg/mL, respectively).…”

“…Instead, Shin et al [ 48 ] tested in vivo the hepatoprotective activity of CM-containing SDs with HPMC against tert-butyl hydroperoxide (t-BHP)-treated mice by administering 80 mg/kg of CM (positive control) or an equivalent dose of SD (400 mg/kg). Levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST), which indicate liver damage in response to t-BHP, were reduced by SD, while CM alone had no statistically significant effect.…”

Evaluation of the Solid Dispersion System Engineered from Mesoporous Silica and Polymers for the Poorly Water Soluble Drug Indomethacin: In Vitro and In Vivo

“…The FESEM images are shown in Figure 3, exhibiting clearly the dispersion state of pure IMC and SDs. The shape of pure drug particles is observed in Figure 3A, and the pure IMC was regarded as a "crystalline form" because of its natural crystalline state with a particle size varying from 20 to 100 µm [22]. The SEM image of pure IMC showed a slightly smooth surface and plate-shaped particles ( Figure 3A), whereas that of F3 ( Figure 3B), F6 ( Figure 3C), and F9 ( Figure 3D) showed spherical-shaped, smooth-surfaced SDs.…”

“…Different measurements can obtain various values of PAMPA permeability coefficients, just like the so-called percentage of flux (%F) or transported solute (%T) which measures the part of the test compound in the acceptor compartment. The PAMPA is able to rapidly determine the tendency of compounds to penetrate membranes by passive diffusion and is therefore suitable for screening solid dispersion and relative drugs [22].…”

Polysaccharide-Based Formulations for Healing of Skin-Related Wound Infections: Lessons from Animal Models and Clinical Trials

“…Cellulose in association with collagen was used for the fabrication of nanocrystals composite scaffolds containing curcumin-loaded gelatin microspheres (Cur/GMs/Coll-CNCs) [34]. This approach was employed due to the low stability and high hydrophobicity of curcumin, a compound highlighted for high therapeutic potential as antimicrobial, healing, and anti-inflammatory agent [84][85][86][87]. The authors showed that curcumin was released in a controlled and sustained way from the scaffolds.…”