Hui-Tian Li, Xiao-Min Wang, Jin-Xia An, En Lin, Wei Li, Hai-Xin Qin, Jian-Feng Zhen, Xia-Lin Dai, Zhenjie Zhang, Tong-Bu Lu and Jia-Mei Chen*,
{"title":"伊马替尼和姜黄素共晶混合物、共晶混合物和共晶混合物的比较研究:制备、表征和性能评价","authors":"Hui-Tian Li, Xiao-Min Wang, Jin-Xia An, En Lin, Wei Li, Hai-Xin Qin, Jian-Feng Zhen, Xia-Lin Dai, Zhenjie Zhang, Tong-Bu Lu and Jia-Mei Chen*, ","doi":"10.1021/acs.cgd.4c00926","DOIUrl":null,"url":null,"abstract":"<p >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.</p>","PeriodicalId":34,"journal":{"name":"Crystal Growth & Design","volume":"25 15","pages":"5689–5696"},"PeriodicalIF":3.4000,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Comparative Investigation on a Eutectic Mixture, Coamorphous Mixture, and Cocrystal of Imatinib and Curcumin: Preparation, Characterization, and Property Evaluation\",\"authors\":\"Hui-Tian Li, Xiao-Min Wang, Jin-Xia An, En Lin, Wei Li, Hai-Xin Qin, Jian-Feng Zhen, Xia-Lin Dai, Zhenjie Zhang, Tong-Bu Lu and Jia-Mei Chen*, \",\"doi\":\"10.1021/acs.cgd.4c00926\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >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. 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Comparative Investigation on a Eutectic Mixture, Coamorphous Mixture, and Cocrystal of Imatinib and Curcumin: Preparation, Characterization, and Property Evaluation
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.
期刊介绍:
The aim of Crystal Growth & Design is to stimulate crossfertilization of knowledge among scientists and engineers working in the fields of crystal growth, crystal engineering, and the industrial application of crystalline materials.
Crystal Growth & Design publishes theoretical and experimental studies of the physical, chemical, and biological phenomena and processes related to the design, growth, and application of crystalline materials. Synergistic approaches originating from different disciplines and technologies and integrating the fields of crystal growth, crystal engineering, intermolecular interactions, and industrial application are encouraged.