Design of a sustained-release nanosystem for ultra-efficient absorption of anthocyanins and regulating lung damage through the “lung-gut” axis

Abstract

Introduction

Anthocyanins have various health benefits but are limited by fast elimination and low bioavailability. Many studies have shown that nano delivery systems are effective in improving the intestinal absorption and bioavailability of anthocyanins. However, in the process of selecting anthocyanin nanomaterials, a dilemma is faced: numerous functional nanomaterials lack edible properties, it is difficult to meet the edible and functional requirements of nanomaterials simultaneously. Therefore, it is necessary and inevitable to select nano-anthocyanin carriers that are edible and have certain functional and morphological characteristics.

Objectives

We aim to provide an efficient, sustained-release and easy to industrialize nanosystem method to solve the problem of low bioavailability of anthocyanins.

Methods

A succinylated casein-phospholipid-anthocyanin nanosystem (CLS) was designed via computational chemistry-guided one-step self-assembly. Morphological, in vitro/in vivo digestion, pharmacokinetic were conducted. Furthermore, the effects of CLS on intestinal microecology were verified by using enteritis model animals, and the lung-targeting effect of CLS on lung health was verified by using lung injury model animals.

Results

CLS exhibited 24-hour intestinal sustained release and lung-targeted enrichment. Pharmacokinetic studies showed 25.7-fold higher lung AUC_(0-t) and 13.1-fold higher blood AUC_(0-t) compared to free anthocyanins. CLS significantly alleviated lung injury and colitis in model rats via the gut-lung axis.

Conclusion

This study significantly improved the bioavailability of anthocyanins and demonstrated the oral lung-targeting function of anthocyanins for the first time, paving the way for utilizing anthocyanins as dietary supplements and precision nutrition.