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具有改善稳定性和生物利用度的叶黄素共晶体。

Cocrystal of Lutein with Improved Stability and Bioavailability.

作者信息

Zheng Chenxuan, Wang Hao, Xiao Ziyao, Sun Zhixiong, Bao Junjie, Dai Wenjuan, Zhang Qi, Mei Xuefeng

机构信息

School of Pharmacy, Jiangxi Medical College, Nanchang University, Nanchang 330006, People's Republic of China2.

Pharmaceutical Analytical&Solid-State Chemistry ResearchCenter, Shanghai Institute of Materia Medica, ChineseAcademy of Sciences, Shanghai 201203, People's Republic of China.

出版信息

ACS Omega. 2024 Jul 1;9(34):36389-36397. doi: 10.1021/acsomega.4c03864. eCollection 2024 Aug 27.

DOI:10.1021/acsomega.4c03864
PMID:39220502
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11359614/
Abstract

Lutein (LT) is a natural carotenoid and is widely used for its vision protection and antioxidant activity. However, the long-chain polyene structure makes lutein sensitive to light and oxygen and poses many difficulties in the production, processing, and storage. In addition, the special chemical structure of LT leads to low solubility and bioavailability. In this study, we propose an efficient solution to address these issues. A cocrystal of LT with adipic acid (LT-APC) was obtained for the first time. The cocrystals were fully characterized. After cocrystallization, the melting point of marketed LT was increased. The chemical stability of LT was significantly improved, and the influence of impurities on stability was limited. Dissolution experiments were performed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) and the cocrystal generated a much higher apparent solubility. To deepen insight into the mechanisms underlying the cocrystal's improved solubility, wettability tests were performed by contact angle determination and film flotation methods. The cocrystal presented better wettability than the marketed LT. Finally, pharmacokinetic studies of marketed LT and its cocrystal were conducted in rats. The results showed that the cocrystal exhibited 3.4 times higher and 2.2 times higher AUC at a single dose compared with marketed LT.

摘要

叶黄素（LT）是一种天然类胡萝卜素，因其具有保护视力和抗氧化活性而被广泛应用。然而，长链多烯结构使叶黄素对光和氧敏感，这给其生产、加工和储存带来了诸多困难。此外，LT的特殊化学结构导致其溶解度和生物利用度较低。在本研究中，我们提出了一种有效解决这些问题的方案。首次获得了LT与己二酸的共晶体（LT-APC）。对该共晶体进行了全面表征。共结晶后，市售LT的熔点升高。LT的化学稳定性显著提高，杂质对稳定性的影响有限。在模拟胃液（SGF）和模拟肠液（SIF）中进行了溶解实验，结果表明该共晶体具有更高的表观溶解度。为了深入了解共晶体溶解度提高的潜在机制，通过接触角测定和膜浮选法进行了润湿性测试。该共晶体表现出比市售LT更好的润湿性。最后，在大鼠体内对市售LT及其共晶体进行了药代动力学研究。结果表明，与市售LT相比，该共晶体在单剂量给药时的AUC高出3.4倍，Cmax高出2.2倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/4261d43a6813/ao4c03864_0010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/b79116f905b0/ao4c03864_0011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/a93395dbf18c/ao4c03864_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/658da2c7a54c/ao4c03864_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/ac155ef97cb4/ao4c03864_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/428b3f38c2cb/ao4c03864_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/fa7ad135adff/ao4c03864_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/cf054cf94a33/ao4c03864_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/f9513d16ceb6/ao4c03864_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/3e1371bff9d6/ao4c03864_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/5f9ddf48251e/ao4c03864_0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/4261d43a6813/ao4c03864_0010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/b79116f905b0/ao4c03864_0011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/a93395dbf18c/ao4c03864_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/658da2c7a54c/ao4c03864_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/ac155ef97cb4/ao4c03864_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/428b3f38c2cb/ao4c03864_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/fa7ad135adff/ao4c03864_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/cf054cf94a33/ao4c03864_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/f9513d16ceb6/ao4c03864_0007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/3e1371bff9d6/ao4c03864_0008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/5f9ddf48251e/ao4c03864_0009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10da/11359614/4261d43a6813/ao4c03864_0010.jpg

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本文引用的文献

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Enzymatic acylation improves the stability and bioactivity of lutein: Protective effects of acylated lutein derivatives on L-O2 cells upon HO-induced oxidative stress.酶促酰化提高了叶黄素的稳定性和生物活性：酰化叶黄素衍生物对HO诱导的氧化应激下L-O2细胞的保护作用。
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Lutein and Zeaxanthin and Their Roles in Age-Related Macular Degeneration-Neurodegenerative Disease.叶黄素和玉米黄质及其在年龄相关性黄斑变性-神经退行性疾病中的作用。
Nutrients. 2022 Feb 16;14(4):827. doi: 10.3390/nu14040827.
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Characterisation of spray dried microencapsules with amorphous lutein nanoparticles: Enhancement of processability, dissolution rate, and storage stability.
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Lutein attenuates angiotensin II- induced cardiac remodeling by inhibiting AP-1/IL-11 signaling.叶黄素通过抑制AP-1/IL-11信号通路减轻血管紧张素II诱导的心脏重塑。
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Lutein supplementation and retinopathy of prematurity: a meta-analysis.叶黄素补充剂与早产儿视网膜病变：一项荟萃分析。
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Molecular evidence that oral supplementation with lycopene or lutein protects human skin against ultraviolet radiation: results from a double-blinded, placebo-controlled, crossover study.分子证据表明，口服补充番茄红素或叶黄素可保护人体皮肤免受紫外线辐射：来自一项双盲、安慰剂对照、交叉研究的结果。
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