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肠道靶向纳米凝胶具有广谱自主清除活性氧性能,可增强白藜芦醇的生物活性。

Intestinal Targeted Nanogel with Broad-Spectrum Autonomous ROS Scavenging Performance for Enhancing the Bioactivity of Resveratrol.

机构信息

School of Food Science and Engineering, School of Biological and Pharmaceutical Sciences, Shaanxi University of Science & Technology, Xi'an, 710021, People's Republic of China.

Xi'an Key Laboratory of Antiviral and Antimicrobial-Resistant Bacteria Therapeutics Research, Xi'an, 710021, People's Republic of China.

出版信息

Int J Nanomedicine. 2024 Jun 14;19:5995-6014. doi: 10.2147/IJN.S464849. eCollection 2024.

Abstract

INTRODUCTION

To improve the bioavailability of resveratrol (-Res), it is commonly co-delivered with antioxidant bioactives using a complex synthetic intestinal targeted carrier, however, which makes practical application challenging.

METHODS

A nanogel (Ngel), as broad-spectrum autonomous ROS scavenger, was prepared using selenized thiolated sodium alginate (TSA-Se) and crosslinked with calcium lactate (CL) for loading Res to obtain Ngel@Res, which maintained spherical morphology in the upper digestive tract but broke down in the lower digestive tract, resulting in -Res release.

RESULTS

Under protection of Ngel, Res showed enhanced stability and broad-spectrum ROS scavenging activity. The synergistic mucoadhesion of Ngel prolonged the retention time of Res in the intestine. Ngel and Ngel@Res increased the lifespan of to 26.00 ± 2.17 and 26.00 ± 4.27 days by enhancing the activity of antioxidases, upregulating the expression of and , while downregulating the expression of and .

CONCLUSION

This readily available, intestinal targeted selenized alginate-based nanogel effectively improves the bioactivity of Res.

摘要

简介

为了提高白藜芦醇(-Res)的生物利用度,通常将其与抗氧化生物活性物质一起使用复杂的合成肠道靶向载体来共递送,然而这使得实际应用具有挑战性。

方法

一种纳米凝胶(Ngel),作为广谱自主活性氧(ROS)清除剂,使用硒化巯基化的海藻酸钠(TSA-Se)和乳酸钙(CL)交联制备,用于负载 Res 以获得 Ngel@Res,其在上消化道中保持球形形态,但在下消化道中分解,导致 -Res 释放。

结果

在 Ngel 的保护下,Res 表现出增强的稳定性和广谱 ROS 清除活性。Ngel 的协同黏膜黏附作用延长了 Res 在肠道中的保留时间。Ngel 和 Ngel@Res 通过增强抗氧化酶的活性、上调 和 的表达,同时下调 和 的表达,将 的寿命延长至 26.00±2.17 和 26.00±4.27 天。

结论

这种易于获得的、肠道靶向的基于硒化海藻酸盐的纳米凝胶可有效提高 Res 的生物活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/164f/11185258/d21d92212361/IJN-19-5995-g0001.jpg

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