Improvements of Solubility and Bioavailability of Lutein Through Grafting with Hydrophilic Polyacrylic Acid

Peng Liu; Xiaoxue Xu; Xiaoyu Bai; Xingtong Gao; Kai Liu; Yiming Xu; Aixiang Li; Xinhua Song

doi:10.1016/j.xphs.2023.05.010

Improvements of Solubility and Bioavailability of Lutein Through Grafting with Hydrophilic Polyacrylic Acid

J Pharm Sci. 2023 Nov;112(11):2811-2819. doi: 10.1016/j.xphs.2023.05.010. Epub 2023 May 19.

Authors

Peng Liu¹, Xiaoxue Xu², Xiaoyu Bai¹, Xingtong Gao¹, Kai Liu¹, Yiming Xu², Aixiang Li³, Xinhua Song⁴

Affiliations

¹ School of Material Science and Engineering, Shandong University of Technology, Zibo, 255049, People's Republic of China.
² College of Life Sciences, Shandong University of Technology, Zibo, 255049, People's Republic of China.
³ School of Material Science and Engineering, Shandong University of Technology, Zibo, 255049, People's Republic of China. Electronic address: axl@sdut.edu.cn.
⁴ College of Life Sciences, Shandong University of Technology, Zibo, 255049, People's Republic of China; Shandong Tianyin Biotechnology Co., Ltd., Zibo, 255000, People's Republic of China.

PMID: 37211314
DOI: 10.1016/j.xphs.2023.05.010

Abstract

In this study, polyacrylic acid grafted lutein (PAA-g-lutein) was prepared by hydrophilic modification of lutein with polyacrylic acid (PAA) through Steglish esterification method. The unreacted lutein was loaded in micelles formed by self-assembly of graft copolymers in water to form composite nanoparticles. The bioaccessibility and bioavailability of lutein nanoparticles were studied by in vitro and in vivo digestion experiments. Compared with free lutein, the saturated solubility and bioaccessibility of lutein nanoparticles were increased by 78 times and 3.6 times, respectively. The pharmacokinetics results in the mice model showed that the maximum concentration (C_max) and area under concentration-time curve (AUC) of plasma of mice were increased by 3.05 and 6.07 times with lutein nanoparticles compared with free lutein. Meanwhile, the prepared lutein nanoparticles also promoted the accumulation of lutein in the liver, mesenteric adipose, and eyeballs. These results indicate that graft copolymerization of lutein with water-soluble polymers to form nanoparticles is an effective method to promote the bioavailability of lutein in vivo. Moreover, this method is simple and applicable, and can also be used for the modification of other bioactive molecules.

Keywords: Bioavailability; Composite nanoparticle; Graft copolymer; Lutein; Pharmacokinetics.