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.

中文翻译：

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设计缓释纳米系统，用于超高效吸收花青素并通过“肺-肠”轴调节肺损伤

  介绍

花青素具有多种健康益处，但受到快速消除和低生物利用度的限制。许多研究表明，纳米递送系统可有效改善花青素的肠道吸收和生物利用度。然而，在选择花青素纳米材料的过程中，面临着一个困境：许多功能性纳米材料缺乏可食用性，难以同时满足纳米材料的可食用性和功能性要求。因此，选择可食用且具有一定功能和形态特性的纳米花青素载体是必要和必然的。

  目标

我们的目标是提供一种高效、缓释且易于工业化的纳米系统方法，以解决花青素生物利用度低的问题。

  方法

通过计算化学引导的一步自组装设计了琥珀酰化酪蛋白-磷脂-花青素纳米系统 （CLS）。进行形态学、 体外/体内消化、药代动力学。此外，使用肠炎模型动物验证了 CLS 对肠道微生态的影响，使用肺损伤模型动物验证了 CLS 对肺健康的肺靶向作用。

  结果

CLS 表现出 24 h 肠道缓释和肺靶向富集。药代动力学研究表明，与游离花青素相比，肺 AUC _（0-t） 高 25.7 倍，血液 AUC _（0-t） 高 13.1 倍。CLS 通过肠-肺轴显著减轻模型大鼠的肺损伤和结肠炎。

  结论

本研究显著提高了花青素的生物利用度，并首次证明了花青素的口服肺靶向功能，为花青素作为膳食补充剂和精准营养铺平了道路。