Preparation and Characterization of a Curcumin Solid Dispersion with Enhanced Solubility and Hepato-protective Efficacy Against Non-Alcoholic Fatty Liver Disease

Background/Objectives: Curcumin has potential hepatoprotective effects in non-alcoholic fatty liver disease (NAFLD), but its poor aqueous solubility limits formulation development. This study aimed to prepare a curcumin solid dispersion (CSD) using polyvinylpyrrolidone K30 (PVP K30) and phosphatidylcholine to evaluate its physicochemical properties and hepatoprotective effects. Methods: CSD was prepared by solvent evaporation at a curcumin/phosphatidylcholine/PVP K30 weight ratio of 1:2:3. X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanning electron microscopy were used for characterization. Apparent solubility and in vitro dissolution were assessed in buffers at pH 1.2, 4.5, and 6.8. Raw curcumin and a corresponding physical mixture were used as comparators. Hepatoprotective effects were investigated in a high-fat diet/lipopolysaccharide-induced experimental NAFLD model using serum biochemical markers, hepatic inflammatory cytokines, and liver histology. The animal study compared oral CSD at curcumin-equivalent doses of 50 and 100 mg/kg/day with unformulated curcumin at 200 mg/kg/day. Results: The dispersion showed diffraction and thermal profiles consistent with amorphization of curcumin. Apparent solubility reached 184.2, 232.6, and 292.1 µg/mL at pH 1.2, 4.5, and 6.8, respectively. At pH 1.2, the reported 90 min cumulative dissolution increased from 8.8% for unformulated curcumin to 87.9% for CSD. CSD treatment was associated with lower serum ALT and ALP levels, reduced hepatic lipid accumulation, and decreased hepatic TNF-α, IL-6, and IL-1β levels. Conclusions: The PVP K30/phosphatidylcholine-based solid dispersion improved curcumin's apparent solubility and dissolution and showed hepatoprotective effects in an experimental NAFLD model. These findings support further evaluation of this formulation approach.

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Publication Details

Journal
Preprints.org
Published
2026-10-26
DOI
https://doi.org/10.20944/preprints202610.2537.v1
Primary Topic
Curcumin's Biomedical Applications
Type
preprint
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preprint

Preparation and Characterization of a Curcumin Solid Dispersion with Enhanced Solubility and Hepato-protective Efficacy Against Non-Alcoholic Fatty Liver Disease

Zhijun Guo, Wenhong Zhu, 臧庆华, Lian-lin Su et al.
Preprints.org
Curcumin's Biomedical Applications
preprint

Preparation and Characterization of a Curcumin Solid Dispersion with Enhanced Solubility and Hepato-protective Efficacy Against Non-Alcoholic Fatty Liver Disease

Zhijun Guo, Wenhong Zhu, 臧庆华, Lian-lin Su, Mingxuan Li, Changcan Shi, 毛春芹, Hong Jin, Tulin LU, Yu Li, Xiaodong Gong, Jiuba Zhang
preprint en

Abstract

Background/Objectives: Curcumin has potential hepatoprotective effects in non-alcoholic fatty liver disease (NAFLD), but its poor aqueous solubility limits formulation development. This study aimed to prepare a curcumin solid dispersion (CSD) using polyvinylpyrrolidone K30 (PVP K30) and phosphatidylcholine to evaluate its physicochemical properties and hepatoprotective effects. Methods: CSD was prepared by solvent evaporation at a curcumin/phosphatidylcholine/PVP K30 weight ratio of 1:2:3. X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanning electron microscopy were used for characterization. Apparent solubility and in vitro dissolution were assessed in buffers at pH 1.2, 4.5, and 6.8. Raw curcumin and a corresponding physical mixture were used as comparators. Hepatoprotective effects were investigated in a high-fat diet/lipopolysaccharide-induced experimental NAFLD model using serum biochemical markers, hepatic inflammatory cytokines, and liver histology. The animal study compared oral CSD at curcumin-equivalent doses of 50 and 100 mg/kg/day with unformulated curcumin at 200 mg/kg/day. Results: The dispersion showed diffraction and thermal profiles consistent with amorphization of curcumin. Apparent solubility reached 184.2, 232.6, and 292.1 µg/mL at pH 1.2, 4.5, and 6.8, respectively. At pH 1.2, the reported 90 min cumulative dissolution increased from 8.8% for unformulated curcumin to 87.9% for CSD. CSD treatment was associated with lower serum ALT and ALP levels, reduced hepatic lipid accumulation, and decreased hepatic TNF-α, IL-6, and IL-1β levels. Conclusions: The PVP K30/phosphatidylcholine-based solid dispersion improved curcumin's apparent solubility and dissolution and showed hepatoprotective effects in an experimental NAFLD model. These findings support further evaluation of this formulation approach.

Preprints.org
Curcumin's Biomedical Applications
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