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载姜黄素壳聚糖/卵磷脂纳米粒的制备及其抗氧化活性和体内生物利用度的提高。

Preparation of curcumin-loaded chitosan/lecithin nanoparticles with increased anti-oxidant activity and in vivo bioavailability.

机构信息

Medical College, Guangxi University, Nanning 530004, China.

Key Laboratory of Research and Development on Clinical Molecular Diagnosis for High-Incidence Diseases of Baise, Affiliated Hospital of Youjiang Medical University for Nationalities, Baise 533000, China.

出版信息

Int J Biol Macromol. 2024 Nov;281(Pt 4):136659. doi: 10.1016/j.ijbiomac.2024.136659. Epub 2024 Oct 16.

Abstract

As a natural polyphenol, curcumin (Cur) has exhibited a range of bioactive properties, including anti-inflammatory, anti-oxidant, and anti-infection properties. However, the chemical instability and low water solubility of Cur hinder its wide application. Herein, Cur-loaded chitosan/lecithin nanoparticles (CCL NPs) were prepared by the electrostatic self-assembly method. The prepared CCL NPs showed a small particle size (122.86 ± 1.53 nm) with homogeneous distribution (PDI = 0.17 ± 0.01). The high EE (79.34 ± 2.93 %) and LC (9.33 ± 0.34 %) indicated that most of Cur was encapsulated in CCL NPs. Meanwhile, the Cur was released from CCL NPs in a quick and sustained way after being exposed to simulated gastrointestinal fluids. The CCL NPs displayed superior anti-oxidant activity than that of free Cur. Moreover, the in vivo pharmacokinetic studies showed that the CCL NPs could lead to a ~ 2.64-fold increase in oral bioavailability compared with that of free Cur. All these findings indicated that the formation of CCL NPs would be a promising platform to deliver Cur in the food industry.

摘要

姜黄素(Cur)作为一种天然多酚,具有多种生物活性,包括抗炎、抗氧化和抗感染特性。然而,Cur 的化学不稳定性和低水溶性限制了其广泛应用。本文采用静电自组装法制备了载姜黄素壳聚糖/卵磷脂纳米粒(CCL NPs)。所制备的 CCL NPs 粒径较小(122.86±1.53nm),分布均匀(PDI=0.17±0.01)。高包封率(EE=79.34±2.93%)和载药量(LC=9.33±0.34%)表明大部分 Cur 被包封在 CCL NPs 中。同时,CCL NPs 在模拟胃肠道液中迅速且持续地释放 Cur。CCL NPs 的抗氧化活性优于游离 Cur。此外,体内药代动力学研究表明,与游离 Cur 相比,CCL NPs 可使口服生物利用度提高约 2.64 倍。这些结果表明,CCL NPs 的形成将成为食品工业中递送 Cur 的有前途的平台。

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