当前位置: X-MOL 学术BMC Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy.
BMC Chemistry ( IF 4.6 ) Pub Date : 2020-02-14 , DOI: 10.1186/s13065-020-0664-x
Niyaz Ahmad 1, 2 , Rizwan Ahmad 3 , Sadiq Al Qatifi 1 , Mahdi Alessa 1 , Hassan Al Hajji 1 , Md Sarafroz 2
Affiliation  

To formulate a nanoformulation (PLGA-NPs) and to improve brain bioavailability for thymoquinone (THQ) through intranasal (i.n.) drug delivery, using a newly UHPLC-PDA developed the method and validated. Five different THQ-PLGA-NPs (THQ-N1 to THQ-N5) were prepared by emulsion solvent evaporation method. A new UHPLC method developed and validated for biodistribution studies in the rat's brain, lungs and plasma. Optimized-THQ-N1-NPs showed a particle size of 97.36 ± 2.01 nm with a low PDI value of 0.263 ± 0.004, ZP of - 17.98 ± 1.09, EE of 82.49 ± 2.38% and DL of 5.09 ± 0.13%. THQ-N1-NPs showed sustained release pattern via in vitro release profile. A bioanalytical method was developed by UHPLC-PDA and validated for the evaluation of pharmacokinetics parameters, biodistribution studies, brain drug-targeting potential (89.89 ± 9.38%), and brain-targeting efficiency (8075.00 ± 113.05%) studies through intranasal administration which showed an improved THQ-brain- bioavailability, compared to i.v. Moreover, THQ-PLGA-NPs improved the seizure threshold treatment i.e. epilepsy increasing current electroshock (ICES) rodent models induced seizures in rats. A significant role of THQ-PLGA-NPs with high brain targeting efficiency of the nanoformulations was established. The reported data supports the treatment of epilepsy.

中文翻译:

基于UHPLC的生物分析方法,用于定量治疗癫痫的胸腺素负载的PLGA纳米颗粒。

为了配制纳米制剂(PLGA-NPs)并通过鼻内(内)药物递送提高胸腺醌(THQ)的大脑生物利用度,使用了最新的UHPLC-PDA开发的方法并进行了验证。通过乳液溶剂蒸发法制备了五种不同的THQ-PLGA-NP(THQ-N1至THQ-N5)。开发并验证了一种新的UHPLC方法,用于大鼠脑,肺和血浆中的生物分布研究。优化的THQ-N1-NPs的粒径为97.36±2.01 nm,PDI值为0.263±0.004,ZP为-17.98±1.09,EE为82.49±2.38%,DL为5.09±0.13%。THQ-N1-NPs通过体外释放曲线显示出持续释放模式。UHPLC-PDA开发了一种生物分析方法,并经过验证可用于评估药代动力学参数,生物分布研究,脑部药物靶向潜力(89.89±9.38%),鼻内给药的研究和脑靶向效率研究(8075.00±113.05%),与iv相比具有更高的THQ-大脑生物利用度。此外,THQ-PLGA-NPs改善了癫痫发作阈值治疗,即癫痫增加电流电击(ICES)啮齿动物模型诱发大鼠癫痫发作。建立了THQ-PLGA-NP对纳米制剂具有高脑靶向作用的重要作用。报告的数据支持癫痫的治疗。建立了THQ-PLGA-NP对纳米制剂具有高脑靶向作用的重要作用。报告的数据支持癫痫的治疗。建立了THQ-PLGA-NP对纳米制剂具有高脑靶向作用的重要作用。报告的数据支持癫痫的治疗。
更新日期:2020-04-22
down
wechat
bug