Formulation of multicomponent inclusion complex of cyclodextrin-amino acid with Chrysin: Physicochemical characterization, cell viability and apoptosis assessment in human primary glioblastoma cell line

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Wael A. Mahdi , Mohammed Mufadhe Alanazi , Syed Sarim Imam , Sultan Alshehri , Afzal Hussain , Mohammad A. Altamimi , Sulaiman S. Alhudaithi
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引用次数: 1

Abstract

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.

Abstract Image

环糊精-氨基酸与黄菊花素多组分包合物的制备:人原发性胶质母细胞瘤细胞系理化特性、细胞活力及凋亡评估
据报道,赖氨酸(CR)是一种不溶于水的药物,具有不同的治疗效果。本研究采用微波辐照的方法制备了含有CR(药物)和载体羟丙基β-环糊精(HPβCD)和L-精氨酸(LA)的多组分包合物(CR-MC)。对制备的包合物(CR-MC)进行溶出度研究,并将结果与白杨素物理混合物(CR-PM)进行比较。此外,对样品进行了红外(IR)、核磁共振(NMR)、差示扫描量热计(DSC)、扫描电子显微镜(SEM)和分子对接评估。最后,还评估了细胞活力、活性氧和流式细胞仪研究,以检查所制备的包合物对人原发性胶质母细胞瘤细胞系(U87-MG细胞)的潜力。相溶解度结果显示稳定常数(773 mol L−1)以及0.027的络合效率。溶出度研究显示CR-MC的CR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研究结果显示转化为无定形形式。分子对接结果表明对接得分很高,这支持了复合物形成的发现。细胞活力、活性氧和流式细胞术研究结果显示,CR-MC对测试的人类原发性胶质母细胞瘤细胞系的活性增强。从结果中观察到,在络合后,chrysin的溶解度显著增加,并且在体外对癌症细胞系的活性也增强。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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