文献类型：期刊文献

英文题名：Slow-Release Drug-Drug Cocrystals of Oxaliplatin with Flavonoids: Delaying Hydrolysis and Reducing Toxicity

作者：Yin, He-Mei[1];Wu, Nan[1];Zhou, Bi-Jian[1];Hong, Ming-Huang[1];Zhu, Bin[1];Qi, Ming-Hui[1];Ren, Guo-Bin[1,2]

机构：[1]East China Univ Sci & Technol, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai Key Lab New Drug Design, Minist Educ,Lab Pharmaceut Crystal Engn & Technol, Shanghai 200237, Peoples R China

年份：2021

卷号：21

期号：1

起止页码：75

外文期刊名：CRYSTAL GROWTH & DESIGN

收录：;EI(收录号：20210209762885);WOS:【SCI-EXPANDED(收录号:WOS:000607623900011)】；

基金：This work was supported by National Natural Science Foundation of China (No. 21706064, No. 21776073) and Fundamental Research Funds for the Central Universities (No. 222201814049).

语种：英文

外文关键词：Single crystals - Cancer cells - Controlled drug delivery - Fourier transform infrared spectroscopy - Dissolution - Targeted drug delivery - Cells - Flavonoids - X ray diffraction - Hydrogen bonds - Thermoanalysis - Toxicity - Cytology

摘要：Oxaliplatin (OXA) is a third-generation, platinum-based anticancer agent that is reported to induce cell toxicity in normal cells, which severely limits its applications. Its instability in aqua solution plays an important role in the cytotoxic effects. In this study, two novel drugdrug cocrystals of OXA were synthesized using baicalein (BAI) and naringenin (NAR) as cocrystal formers, as well as characterized by single crystal X-ray diffraction, powder X-ray diffraction, Fourier transform-infrared spectroscopy, and thermal analysis. Further evaluation of the dissolution profiles of the two cocrystals presented that they both have a reduced release rate and delayed hydrolysis compared to OXA. Theoretical analyses of the correlation between the structure and dissolution indicate that heterosynthons OH center dot center dot center dot O and NH center dot center dot center dot O hydrogen bonds are essential for reducing the dissolution rate of the two cocrystals. In addition, cell toxicity was studied using the CCK-8 assay, with the result that OXANAR may possess higher safety and OXABAI may have more significant effects on inhibiting cancer cells when compared to OXA.