4.6 Article

The enhancement of N-acetylcysteine on intestinal absorption and oral bioavailability of hydrophobic curcumin

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ELSEVIER
DOI: 10.1016/j.ejps.2020.105506

Keywords

Curcumin; Bovine serum albumin nanoparticle; N-acetylcysteine; Gastrointestinal tract; Oral bioavailability

Funding

  1. Open Project of State Key Laboratory of Natural Medicines [3144060210]
  2. College Students Innovation Project for the R&D of Novel Drugs [J1310032]

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To solve the low oral bioavailability of curcumin (CUR) due to the limits imposed by gastrointestinal (GI) barrier, we constructed a nano delivery system to evaluate the effect of N-acetyl-L-cysteine (NAC) on intestinal absorption and oral bioavailability of CUR. CUR was first encapsulated in bovine serum albumin nanoparticles (CUR-BSA-NPs), and then was further modified by NAC (CUR-NBSA-NPs). In situ single-pass intestinal perfusion assay demonstrated that CUR-NBSA-NPs displayed excellent permeation and absorption rates in GI tract. Additionally, the distribution study in GI tract revealed that more NBSA-NPs were absorbed by intestinal segments compared to the BSA nanoparticles. Plasma concentration-time curves in rats showed that AUC(0-t), C-max and MRT0-t values of CUR after oral administration of CUR-NBSA-NPs were increased to 3.25-, 4.42-, and 1.43-fold compared with that of CUR suspension. In conclusion, NAC promotes oral absorption of CUR, thereby improving its oral bioavailability.

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