<p>Xanthorrhizol and curcumin are bioactive compounds derived from plants, including <i>Curcuma xanthorrhiza</i>, a member of the ginger family. However, their limited solubility leads to low oral bioavailability and poses significant constraints for industrial applications. Therefore, we developed nanostructured lipid carriers (NLCs) loaded with standardized ethanolic <i>Curcuma xanthorrhiza</i> extract (CXE). The CXE-NLCs were optimized by varying the initial concentration of CXE, resulting in homogeneous particles with a size of 130.0 ± 1.0&#xa0;nm and a high encapsulation efficiency of approximately 83%. CXE-NLCs exhibited enhanced biostability under simulated gastrointestinal conditions, and in vitro release studies demonstrated the sustained release of CXE. Additionally, CXE-NLCs demonstrated significantly improved permeability across the Caco-2/HT-29 cell monolayer (P<sub>app</sub> = 4.2 × 10<sup>− 5</sup> cm/s), which is favorable for the oral delivery of bioactive compounds. In vivo studies confirmed that CXE-NLCs inhibited carrageenan-induced inflammation in the paw, prostaglandins E<sub>1</sub> and E<sub>2</sub>, as well as the eicosanoid and MAPK pathways in a dose-dependent manner. This study highlights the enhanced oral delivery and bioactivity of synthesized CXE-NLCs containing both xanthorrhizol and curcumin in the treatment of acute inflammation. This indicates a useful application and suggests their potential as a nano delivery system for nutraceuticals and pharmaceuticals.</p>

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Plant derived extract loaded nanostructured lipid carriers with enhanced oral delivery for the treatment of acute inflammation

  • Eun Yong Lee,
  • JeongUn Choi,
  • Young Min Kim,
  • Kyungjik Yang,
  • A-yeong Jang,
  • Hae Kyung Shin,
  • Hae Rim Kim,
  • Keonwook Nam,
  • Jae Kwan Hwang,
  • Jiyong Park,
  • Woo Jung Park,
  • Young Hoon Roh

摘要

Xanthorrhizol and curcumin are bioactive compounds derived from plants, including Curcuma xanthorrhiza, a member of the ginger family. However, their limited solubility leads to low oral bioavailability and poses significant constraints for industrial applications. Therefore, we developed nanostructured lipid carriers (NLCs) loaded with standardized ethanolic Curcuma xanthorrhiza extract (CXE). The CXE-NLCs were optimized by varying the initial concentration of CXE, resulting in homogeneous particles with a size of 130.0 ± 1.0 nm and a high encapsulation efficiency of approximately 83%. CXE-NLCs exhibited enhanced biostability under simulated gastrointestinal conditions, and in vitro release studies demonstrated the sustained release of CXE. Additionally, CXE-NLCs demonstrated significantly improved permeability across the Caco-2/HT-29 cell monolayer (Papp = 4.2 × 10− 5 cm/s), which is favorable for the oral delivery of bioactive compounds. In vivo studies confirmed that CXE-NLCs inhibited carrageenan-induced inflammation in the paw, prostaglandins E1 and E2, as well as the eicosanoid and MAPK pathways in a dose-dependent manner. This study highlights the enhanced oral delivery and bioactivity of synthesized CXE-NLCs containing both xanthorrhizol and curcumin in the treatment of acute inflammation. This indicates a useful application and suggests their potential as a nano delivery system for nutraceuticals and pharmaceuticals.