Physicochemical Characterization and Oral Bioavailability of Curcumin–Phospholipid Complex Nanosuspensions Prepared Based on Microfluidic System

<b>Background</b>: Curcumin has been proved to have promising prospects in the fields of anti-inflammation, antibacterial, anti-oxidation, and neuroprotection. However, its poor water solubility and stability in strong acid, as well as fast metabolism, lead to low bioavailability, making it difficult to develop further. This study aimed to improve the bioavailability of curcumin by using microfluidic preparation technology. <b>Methods</b>: Using a self-built microfluidic system, polyvinylpyrrolidone K30 and sodium dodecyl sulfate were used as stabilizers to further prepare curcumin-phospholipid complex nanoparticles (CPC-NPs) on the basis of curcumin-phospholipid complex (CPC). The CPC-NPs were characterized and evaluated by X-ray powder diffraction (XRD), differential scanning caborimetry (DSC), dynamic light scattering, and transmission electron microscopy (TEM). Blood samples were collected from rats after oral administration of curcumin, CPC, curcumin nanoparticles (CUR-NPs), and CPC-NPs, respectively. The pharmacokinetics were analyzed by enzymatic digestion and HPLC. <b>Results</b>: The optimized CPC-NPs had a particle size of 71.19 ± 1.37 nm, a PDI of 0.226 ± 0.047, and a zeta potential of -38.23 ± 0.89 mV, which showed a spherical structure under TEM and good stability within 5 days at 4 °C and 25 °C. It was successfully characterized by XRD combined with DSC, indicating the integrational state of curcumin-soy lecithin and conversion to an amorphous form. The results of the pharmacokinetic study showed that the C<sub>max</sub> of curcumin, CUR-NPs, CPC, and CPC-NPs were 133.60 ± 28.10, 270.23 ± 125.42, 1894.43 ± 672.65, and 2163.87 ± 777.36 ng/mL, respectively; the AUC<sub>0-t</sub> of curcumin, CUR-NPs, CPC, and CPC-NPs were 936.99 ± 201.83, 1155.46 ± 340.38, 5888.79 ± 1073.32, and 9494.28 ± 1863.64 ng/mL/h. <b>Conclusions</b>: CPC-NPs prepared by microfluidic technology had more controllable quality than that of traditional preparation and showed superior bioavailability compared with free drug, CPC, and CUR-NPs. Pharmacodynamic evaluation of anti-inflammatory, anti-oxidation, and neuroprotection needs to be confirmed in follow-up studies.

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Publication Details

Journal
Pharmaceutics
Published
2025-03-20
DOI
https://doi.org/10.3390/pharmaceutics17030395
Citations
8
Primary Topic
Curcumin's Biomedical Applications
Type
article
Field-Weighted Citation Impact
4.73

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article

Physicochemical Characterization and Oral Bioavailability of Curcumin–Phospholipid Complex Nanosuspensions Prepared Based on Microfluidic System

B. P. Zhang, Ruining Zhang, Minchen Liu, Jian Yang et al.
8 citations
Pharmaceutics
Curcumin's Biomedical Applications
4.73
article

Physicochemical Characterization and Oral Bioavailability of Curcumin–Phospholipid Complex Nanosuspensions Prepared Based on Microfluidic System

B. P. Zhang, Ruining Zhang, Minchen Liu, Jian Yang, Zhen‐Yu Chen, Jiquan Zhang, Wenjing Guo, Yaxin Chen
article en
8 citations

Abstract

<b>Background</b>: Curcumin has been proved to have promising prospects in the fields of anti-inflammation, antibacterial, anti-oxidation, and neuroprotection. However, its poor water solubility and stability in strong acid, as well as fast metabolism, lead to low bioavailability, making it difficult to develop further. This study aimed to improve the bioavailability of curcumin by using microfluidic preparation technology. <b>Methods</b>: Using a self-built microfluidic system, polyvinylpyrrolidone K30 and sodium dodecyl sulfate were used as stabilizers to further prepare curcumin-phospholipid complex nanoparticles (CPC-NPs) on the basis of curcumin-phospholipid complex (CPC). The CPC-NPs were characterized and evaluated by X-ray powder diffraction (XRD), differential scanning caborimetry (DSC), dynamic light scattering, and transmission electron microscopy (TEM). Blood samples were collected from rats after oral administration of curcumin, CPC, curcumin nanoparticles (CUR-NPs), and CPC-NPs, respectively. The pharmacokinetics were analyzed by enzymatic digestion and HPLC. <b>Results</b>: The optimized CPC-NPs had a particle size of 71.19 ± 1.37 nm, a PDI of 0.226 ± 0.047, and a zeta potential of -38.23 ± 0.89 mV, which showed a spherical structure under TEM and good stability within 5 days at 4 °C and 25 °C. It was successfully characterized by XRD combined with DSC, indicating the integrational state of curcumin-soy lecithin and conversion to an amorphous form. The results of the pharmacokinetic study showed that the C<sub>max</sub> of curcumin, CUR-NPs, CPC, and CPC-NPs were 133.60 ± 28.10, 270.23 ± 125.42, 1894.43 ± 672.65, and 2163.87 ± 777.36 ng/mL, respectively; the AUC<sub>0-t</sub> of curcumin, CUR-NPs, CPC, and CPC-NPs were 936.99 ± 201.83, 1155.46 ± 340.38, 5888.79 ± 1073.32, and 9494.28 ± 1863.64 ng/mL/h. <b>Conclusions</b>: CPC-NPs prepared by microfluidic technology had more controllable quality than that of traditional preparation and showed superior bioavailability compared with free drug, CPC, and CUR-NPs. Pharmacodynamic evaluation of anti-inflammatory, anti-oxidation, and neuroprotection needs to be confirmed in follow-up studies.

PharmaceuticsVol. 17(3)
Shanghai University of Traditional Chinese Medicine (CN)
Science and Technology Commission of Shanghai Municipality
Clean water and sanitation
Openalex Percentile: Top 4%
Curcumin's Biomedical Applications
4.73
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