Cocrystal of Lutein with Improved Stability and Bioavailability
文献类型:期刊论文
作者 | Zheng, Chenxuan2,3; Wang, Hao1; Xiao, Ziyao1; Sun, Zhixiong2,3; Bao, Junjie2; Dai, Wenjuan2; Zhang, Qi2; Mei, Xuefeng1,2,3![]() |
刊名 | ACS OMEGA
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出版日期 | 2024-07-01 |
页码 | 9 |
ISSN号 | 2470-1343 |
DOI | 10.1021/acsomega.4c03864 |
通讯作者 | Zhang, Qi(qizhang@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn) |
英文摘要 | 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 C-max and 2.2 times higher AUC at a single dose compared with marketed LT. |
WOS关键词 | SOLUBILITY |
资助项目 | Natural Science Foundation of Shanghai[22ZR147390] |
WOS研究方向 | Chemistry |
语种 | 英语 |
WOS记录号 | WOS:001261348100001 |
出版者 | AMER CHEMICAL SOC |
源URL | [http://119.78.100.183/handle/2S10ELR8/312146] ![]() |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Zhang, Qi; Mei, Xuefeng |
作者单位 | 1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China 3.Nanchang Univ, Jiangxi Med Coll, Sch Pharm, Nanchang 330006, Peoples R China |
推荐引用方式 GB/T 7714 | Zheng, Chenxuan,Wang, Hao,Xiao, Ziyao,et al. Cocrystal of Lutein with Improved Stability and Bioavailability[J]. ACS OMEGA,2024:9. |
APA | Zheng, Chenxuan.,Wang, Hao.,Xiao, Ziyao.,Sun, Zhixiong.,Bao, Junjie.,...&Mei, Xuefeng.(2024).Cocrystal of Lutein with Improved Stability and Bioavailability.ACS OMEGA,9. |
MLA | Zheng, Chenxuan,et al."Cocrystal of Lutein with Improved Stability and Bioavailability".ACS OMEGA (2024):9. |
入库方式: OAI收割
来源:上海药物研究所
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