Roles of effective stabilizers in improving oral bioavailability of naringenin nanocrystals:Maintenance of supersaturation generated upon dissolution by inhibition of drug dimerization

作     者：Guangshuai Zhang Haishan Guan Jianfeng Li Mo Li Xiaofan Sui Baocheng Tian Huiming Dong Bingyang Liu Zhonggui He Ning Li Mingming Zhao Qiang Fu Guangshuai Zhang;Haishan Guan;Jianfeng Li;Mo Li;Xiaofan Sui;Baocheng Tian;Huiming Dong;Bingyang Liu;Zhonggui He;Ning Li;Mingming Zhao;Qiang Fu

作者机构：Wuya College of InnovationShenyang Pharmaceutical UniversityShenyang 110016China Department of PharmacyShengjing Hospital of China Medical UniversityShenyang 110004China School of PharmacyShenyang Pharmaceutical UniversityShenyang 110016China Liaoning Institute for Drug ControlShenyang 110016China School of PharmacyBinzhou Medical UniversityYantai 264003China Liaoning Inspection Examination and Certification CentreShenyang 110016China 

出 版 物：《Asian Journal of Pharmaceutical Sciences》 (亚洲药物制剂科学（英文）)

年 卷 期：2022年第17卷第5期

页      面：741-750页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 07[理学] 070205[理学-凝聚态物理] 10[医学] 100602[医学-中西医结合临床] 0702[理学-物理学] 

基　　金：by the National Natural Science Foundation of China(No.82173765) the Science Foundation for Outstanding Youth of Liaoning Province(2021-YQ-08) Ningxia Key Research and Invention Program(No.2021BEG02039) Basic Research Projects of Liaoning Provincial Department of Education(2020LFW01) the Career Development Program for Young Teachers in Shenyang Pharmaceutical University(ZQN2019003) the Outstanding Youth Lifting Program in Shenyang Pharmaceutical University(YQ202115) the Natural Science Foundation of Liaoning Province(2020-MS-074) Open Fund of Key Laboratory of Biotechnology and Bioresources Utilization(Dalian Minzu University),Ministry of Education(KF2022005),China. 

主　　题：Nanocrystals Stabilizers Bioavailability Supersaturation maintenance Dimer 

摘      要：Nanocrystals(NCs),a colloidal dispersion system formulated with stabilizers,have attracted widespread interest due to their ability to effectively improve the oral bioavailability of poorly water-soluble drugs.The stabilizer plays a key role because it can affect the physical stability and even the oral bioavailability of NCs.However,how stabilizers affect the bioavailability of NCs remains unknown.In this study,F68,F127,HPMC,and PVP were each used as a stabilizer to formulate naringenin NCs.The NCs formulated with PVP exhibited excellent release behaviors,cellular uptake,permeability,oral bioavailability,and anti-inflammatory effects.The underlying mechanism is that PVP effectively inhibits the formation of naringenin dimer,which in turn improves the physical stability of the supersaturated solution generated when NC is dissolved.This finding provides insights into the effects of stabilizers on the in vivo performances of NCs and supplies valuable knowledge for the development of poorly water-soluble drugs.