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Bile Acid-based Microcapsule-Like Cocrystals of Phytosterols with Enhanced Solubility, Bioavailability, and Bioactivity

文献类型：期刊论文

作者Tang, Lei4,5; Feng, Yinan3; Bian, Yifei2; Sun, Zhixiong3; Ding, Qiaoce5; Chen, Dongying2,4,5; Wang, Jian-Rong5; Mei, Xuefeng1,4,5
刊名MOLECULAR PHARMACEUTICS
出版日期2025-09-09
页码13
关键词pharmaceutical cocrystal phytosterols solubility bioavailability lipid-lowering
ISSN号1543-8384
DOI10.1021/acs.molpharmaceut.5c00851
通讯作者Wang, Jian-Rong(jrwang@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn)
英文摘要Phytosterols are a class of natural steroids found in various plants. Commercially available phytosterols (PS) are primarily extracted from the deodorized distillate of soybean oil and consist predominantly of beta-sitosterol with smaller amounts of stigmasterol and campesterol. Numerous studies have consistently demonstrated the significant lipid-lowering activity of PS. However, the application of PS is limited due to their low oral bioavailability. To enhance the water solubility and in turn the absorption of PS at the molecular level, microcapsule-like cocrystals were designed using bile acids via hydrogen bonding. As expected, four microcapsule-like cocrystals were successfully prepared: beta-sitosterol with cholic acid (CA) and chenodeoxycholic acid (CDCA), and PS with CA and CDCA. The cocrystal of PS with CA (PS-CA) was selected for further investigation, and the results demonstrated that PS-CA exhibited significantly enhanced solubility in vitro and markedly improved oral bioavailability in vivo. Specifically, the AUC1-24 h of PS-CA was 6 times that of PS, while the C max was 4 times. Moreover, as a result of the improved bioavailability of PS, PS-CA showed superior lipid-lowering activity.
WOS关键词IN-VITRO BIOACCESSIBILITY ; BETA-SITOSTEROL ; BLOOD CHOLESTEROL ; MECHANISM ; STEROL ; ESTERS
资助项目Chinese Academy of Sciences[XDB1060000] ; Strategic Priority Research Program of the Chinese Academy of Sciences
WOS研究方向Research & Experimental Medicine ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001567302000001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/321420]  
专题中国科学院上海药物研究所
通讯作者Wang, Jian-Rong; Mei, Xuefeng
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Chem Biol, Shanghai 201203, Peoples R China
2.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China
3.Nanchang Univ, Jiangxi Med Coll, Sch Pharm, Nanchang 330006, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
5.Chinese Acad Sci, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Tang, Lei,Feng, Yinan,Bian, Yifei,et al. Bile Acid-based Microcapsule-Like Cocrystals of Phytosterols with Enhanced Solubility, Bioavailability, and Bioactivity[J]. MOLECULAR PHARMACEUTICS,2025:13.
APA Tang, Lei.,Feng, Yinan.,Bian, Yifei.,Sun, Zhixiong.,Ding, Qiaoce.,...&Mei, Xuefeng.(2025).Bile Acid-based Microcapsule-Like Cocrystals of Phytosterols with Enhanced Solubility, Bioavailability, and Bioactivity.MOLECULAR PHARMACEUTICS,13.
MLA Tang, Lei,et al."Bile Acid-based Microcapsule-Like Cocrystals of Phytosterols with Enhanced Solubility, Bioavailability, and Bioactivity".MOLECULAR PHARMACEUTICS (2025):13.

入库方式： OAI收割

来源：上海药物研究所

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