共晶
姜黄素
表征(材料科学)
共晶体系
化学
伊马替尼
组合化学
纳米技术
材料科学
有机化学
结晶学
医学
癌症研究
生物化学
分子
微观结构
氢键
髓系白血病
作者
H. Li,Xiaomin Wang,Jinxia An,En Lin,Wei Li,Hailiang Qin,Jian-Feng Zhen,Xia-Lin Dai,Zhenjie Zhang,Tong‐Bu Lu,Jia‐Mei Chen
标识
DOI:10.1021/acs.cgd.4c00926
摘要
Multidrug solid systems (eutectic, coamorphous, and cocrystalline) offer potential to simultaneously improve both drugs’ properties. Yet, systematic comparisons of these forms for a given drug combination remain scarce. Imatinib (IM) and curcumin (CUR) demonstrate synergistic anticancer activity, and both are classified as BCS II drugs, characterized by poor solubility and bioavailability. Herein, a eutectic mixture (IM-CUR EM), coamorphous mixture (IM-CUR CM), and cocrystal (IM-CUR CC) involving IM and CUR were successfully prepared and fully characterized. Combined DSC and PXRD analyses revealed that IM-CUR CC exhibited an intermediate melting point and distinct diffraction peaks compared to individual components, whereas IM-CUR EM showed a lower melting endotherm with unchanged diffraction patterns. The amorphization of IM-CUR CA was verified by the absence of crystalline reflections (halo pattern) in the PXRD analysis and the presence of a single glass transition event in both DSC and modulated DSC thermograms. Crystal structure and FTIR analyses revealed strong intermolecular hydrogen bonding between the piperazine N of IM and phenolic O–H of CUR in both cocrystalline and coamorphous phases. Stability, dissolution and compaction performances, and anticancer activity were systematically evaluated. Notably, IM-CUR EM exhibited superior dissolution performance, while IM-CUR CA and IM-CUR CC showed an improved anticancer effect. All three solid forms exhibited excellent stability. The comparative study offers valuable guidance for the development of synergistic formulations of IM and CUR.
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