在硅片分析舒必利,纳米粒子的合成、表征和体外研究用于治疗精神分裂症。

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Kecel-Gunduz年代,Budama-Kilinc Y, Cakir-Koc R, Zorlu T, B Bicak Kokcu Y, Z,泽尔AE,阿克于兹

在硅片分析舒必利,纳米粒子的合成、表征和体外研究用于治疗精神分裂症。

咕咕叫第一版辅助药物洗脱支架。2020;16 (2):104 - 121。doi: 10.2174 / 1573409915666190627125643。

PubMed ID

31244443 (在PubMed

]

文摘

背景:舒必利,选择性多巴胺能阻断活动,是一种取代苯甲酰胺抗精神病药物治疗精神分裂症扮演着重要的角色,更有选择性和主要街区多巴胺D2和D3受体。摘要目的:本研究有两个主要目标,首先;分子建模研究(MD和对接,ADME)进行定义舒必利的分子概要和sulpiridereceptor交互,另一个与壳聚糖合成聚合物纳米粒子,在缓慢的优势/药物控制释放,改善药物的溶解性和稳定性,提高公用事业和降低毒性。方法:分子动力学仿真进行了确定构象变化和稳定性(水)的多巴胺D3受体的药物和绑定配置文件是由分子对接的计算。药物的药理特性被ADME分析显示。离子凝胶法被用来准备舒必利负载壳聚糖纳米粒子(CS NPs)。动态光散射(DLS),紫外可见吸收(UV)、扫描电镜(SEM)、傅里叶变换红外(ir)光谱技术进行了纳米粒子的特点。体外细胞细胞毒性实验研究与MTT测定小鼠成纤维细胞(L929),人类神经母细胞瘤(SH-SY5Y)和胶质母细胞瘤细胞(u - 87)。由方差分析统计评估。结果:残留(asp - 119,板式换热器- 417)D3受体提供了一个稳定的对接与药物,和重要的药理价值(血脑屏障,Caco-2渗透率和人类口服吸收)也确定。 The average particle size, PdI and zeta potential value of sulpiride- loaded chitosan NPs having a spherical morphology were calculated as 96.93 nm, 0.202 and +7.91 mV. The NPs with 92.8% encapsulation and 28% loading efficiency were found as a slow release profile with 38.49% at the end of the 10th day. Due to the formation of encapsulation, the prominent shifted wave numbers for C-O, S-O, S-N stretching, S-N-H bending of Sulpiride were also identified. Mitochondrial activity of U87, SHSY-5Y and L929 cell line were assayed and evaluated using the SPSS program. CONCLUSION: To provide more efficient use of Sulpiride having a low bioavailability of the gastrointestinal tract, the nanoparticle formulation with high solubility and bioavailability was designed and synthesized for the first time in this study for the treatment of schizophrenia. In addition to all pharmacological properties of drug, the dopamine blocking activity was also revealed. The toxic effect on different cell lines have also been interpreted.

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药物

舒必利