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叶酸偶联壳聚糖载原花青素纳米粒的合成、表征及体外消化。

Synthesis, characterization and in vitro digestion of folate conjugated chitosan-loaded proanthocyanidins nanoparticles.

机构信息

School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China; Department of Pharmacy, Ningbo First Hospital, Ningbo Hospital of Zhejiang University, Ningbo 315010, China.

School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China.

出版信息

Food Res Int. 2023 Jan;163:112141. doi: 10.1016/j.foodres.2022.112141. Epub 2022 Nov 19.

Abstract

Proanthocyanidins have significant biological activity and pharmacological effects and are widely used in food, medicine, and cosmetics. Chitosan nanoparticles loaded with proanthocyanidins have been proven to improve their biological activity. Given some deficiencies of chitosan (CS), the modification of chitosan by folic acid (FA) can obtain new variants with different functions. For this objective, the folic acid conjugated chitosan was designed, and in vitro properties of proanthocyanidins loaded nanoparticles were studied systemically. Firstly, folic acid-chitosan conjugate (FA-CS) was synthesized and characterized. Folate-coupled chitosan-loaded proanthocyanidin nanoparticles (PC-CS/FA-NPs) were prepared by ionic gelation technique using FA-CS as a carrier. The successful nanoparticle synthesis was characterized by dynamic light scattering (DLS) techniques and Fourier transform infrared (FT-IR) spectroscopy. The synthesized nanoparticles exhibited a spherical shape and smooth and uniform distribution features with a size range of less than 300 nm, as observed by a scanning electron microscope (SEM). Meanwhile, PC-CS/FA-NPs had good thermal and gastrointestinal digestive stability and had a protective effect on AAPH-induced erythrocyte oxidative hemolysis. In conclusion, folic acid decorated chitosan nanoparticles improved the stability and bioavailability of proanthocyanidins in gastrointestinal digestion.

摘要

原花青素具有显著的生物活性和药理作用,广泛应用于食品、医药和化妆品领域。负载原花青素的壳聚糖纳米粒已被证明能提高其生物活性。鉴于壳聚糖(CS)的一些缺陷,通过叶酸(FA)对壳聚糖进行修饰可以获得具有不同功能的新变体。为此,设计了叶酸接枝壳聚糖,并系统研究了负载原花青素纳米粒的体外性质。首先,合成并表征了叶酸-壳聚糖偶联物(FA-CS)。采用离子凝胶技术,以 FA-CS 为载体,制备了叶酸偶联壳聚糖-负载原花青素纳米粒(PC-CS/FA-NPs)。成功的纳米颗粒合成通过动态光散射(DLS)技术和傅里叶变换红外(FT-IR)光谱进行了表征。扫描电子显微镜(SEM)观察到,合成的纳米颗粒呈球形,分布均匀,粒径小于 300nm。同时,PC-CS/FA-NPs 具有良好的热稳定性和胃肠道消化稳定性,对 AAPH 诱导的红细胞氧化溶血具有保护作用。总之,叶酸修饰的壳聚糖纳米粒提高了原花青素在胃肠道消化过程中的稳定性和生物利用度。

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