β-环糊精-氨基酸-黄芩素的多成分包结物的制备:在人类原发性胶质母细胞瘤细胞株中进行物理化学表征、细胞存活性和凋亡评估。
Formulation of multicomponent inclusion complex of cyclodextrin-amino acid with Chrysin: Physicochemical characterization, cell viability and apoptosis assessment in human primary glioblastoma cell line.
发表日期:2023 Dec 15
作者:
Wael A Mahdi, Mohammed Mufadhe Alanazi, Syed Sarim Imam, Sultan Alshehri, Afzal Hussain, Mohammad A Altamimi, Sulaiman S Alhudaithi
来源:
International Journal of Pharmaceutics-X
摘要:
菊粉(CR)是一种水不溶性药物,已被报道具有不同的治疗效果。本研究采用微波辐射方法制备了一种多组分包合物(CR-MC),其中包含CR(药物)、载体羟丙基β环糊精(HP β CD)和L-精氨酸(LA)。对制备的包合物(CR-MC)进行了溶解度研究,并将结果与菊粉物理混合物(CR-PM)进行了比较。此外,还对样品进行了红外(IR)、核磁共振(NMR)、差示扫描量热仪(DSC)、扫描电子显微镜(SEM)和分子对接分析。最后,通过细胞活力、活性氧和流式细胞仪分析,评估了制备的包合物对人类原发性脑胶质母细胞瘤细胞系(U87-MG细胞)的潜力。相溶性研究结果显示稳定常数(773 mol L-1)和络合效率为0.027。溶解度研究显示CR-MC的释放显著增加(99.03±0.39%)>CR-PM(70.58±1.16%)>纯CR(35.29±1.55%)。NMR和IR光谱数据显示CR与载体之间没有相互作用。SEM和DSC研究结果显示了形态转变为无定形的形式。分子对接结果显示高的对接得分,支持了形成复合物的发现。细胞活力、活性氧和流式细胞仪研究结果表明,CR-MC对测试的人类原发性脑胶质母细胞瘤细胞系的活性增强。从结果中可以观察到,菊粉的溶解度在复合化后显著增加,并且其体外活性对抗癌细胞系也得到增强。© 2023 作者。
Chrysin (CR) is a water-insoluble drug reported for different therapeutic effects. The microwave irradiation method was used in this study to create a multicomponent inclusion complex (CR-MC) containing CR (drug) and carrier hydroxyl propyl beta cyclodextrin (HP β CD) and L-arginine (LA). The prepared inclusion complex (CR-MC) was evaluated for dissolution study and results were compared with chrysin physical mixture (CR-PM). Further, the samples were assessed for infra-red (IR), nuclear magnetic resonance (NMR), differential scanning calorimeter (DSC), scanning electron microscope (SEM) and molecular docking. Finally, the cell viability, reactive oxygen species and flow cytometer studies were also assessed to check the potential of the prepared inclusion complex on the human primary glioblastoma cell line (U87-MG cell). The phase solubility findings revealed a stability constant (773 mol L-1) as well as a complexation efficiency of 0.027. The dissolution study displayed a significant increase in CR release from CR-MC (99.03 ± 0.39%) > CR-PM (70.58 ± 1.16%) > pure CR (35.29 ± 1.55%). NMR and IR spectral data revealed no interaction between CR and carriers. SEM and DSC study results revealed the conversion into amorphous form. The molecular docking results illustrated a high docking score, which supports the findings of complex formation. The cell viability, reactive oxygen species, and flow cytometry studies results showed enhanced activity from CR-MC against the tested human primary glioblastoma cell line. From the results it has been observed that chrysin solubility significantly increased after complexation and there in vitro activity also enhanced against cancer cell line.© 2023 The Authors.