"Development and characterization of an amorphous curcumin-Eudragit(R)E100 solid dispersions with improved solubility, stability, and pharmacokinetic properties"

作者全名："Wang, Xin; Zhu, Yijian; Zhao, Xudong; Zhang, Shurong; Cao, Meiting; Wang, Xiaoyue; Li, Wei"

作者地址："[Wang, Xin; Zhu, Yijian; Zhao, Xudong; Zhang, Shurong; Cao, Meiting; Wang, Xiaoyue; Li, Wei] Chongqing Med Univ, Sch Pharm, Dept Med Chem, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China"

通信作者："Li, W (通讯作者)，Chongqing Med Univ, Sch Pharm, Dept Med Chem, 1 Yixueyuan Rd, Chongqing 400016, Peoples R China."

来源：PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY

ESI学科分类：PHARMACOLOGY & TOXICOLOGY

WOS号：WOS:000878955400001

JCR分区：Q2

影响因子：3.4

年份：2022

卷号：　

期号：　

开始页：　

结束页：　

文献类型：Article; Early Access

关键词：Curcumin; amorphous solid dispersions; bioavailability; hydrogen bonding; high resolution atomic force microscopy

摘要："The development of amorphous solid dispersions (ASD) is one way to overcome the bioavailability challenges of poorly water-soluble drug. Herein, Curcumin (CUR) was dispersed in the polymeric matrix of Eudragit(R)E100 by solvent evaporation, giving ASD, donated as CUR@Eudragit(R)E100. Solubility and stability of CUR were greatly enhanced. DSC and XRD analysis confirmed that the incorporated CUR was present in an amorphous state. The interaction between CUR and Eudragit(R)E100 was investigated through FTIR and molecular modelling studies which implied that -OH groups in CUR, and carboxyl and amino groups in Eudragit(R)E100 involved in the hydrogen bond formation. High resolution atomic force microscopy was employed to directly visualize the molecular morphology of Eudragit(R)E100 and CUR in CUR@Eudragit(R)E100 and the interaction between CUR and the polymer. pH influenced CUR release profile in which the sustained release pattern was revealed vs the physical mixtures. From the plasma concentration vs time profile graph, oral bioavailability of Cur@Eudragit(R)E100 was approximately 5-fold higher than that of native CUR. These results confirmed the potential of designing ASD to enhance the solubility and bioavailability of CUR, simultaneously deliver CUR through this alternative administration route."

基金机构："Municipal Science and Technology Committee of Chongqing [CSTC2014jcy-jA0019]; Chongqing Municipality Education Commission [KJ1400212]; School of Pharmacy, Chongqing Medical University"

基金资助正文："The authors acknowledge the financial support from the Municipal Science and Technology Committee of Chongqing [CSTC2014jcy-jA0019], Chongqing Municipality Education Commission [KJ1400212], and School of Pharmacy, Chongqing Medical University."