A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy
A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy
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DOI：
10.1186/s13065-020-0664-x
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发表时间：
2020-02-14
期刊：
影响因子：
4.6
通讯作者：
Sarafroz, Md
中科院分区：
文献类型：
--
作者：
Ahmad, Niyaz;Ahmad, Rizwan;Sarafroz, Md
为了配制纳米制剂（PLGA-NP）并通过鼻内（i. n.）药物输送，使用新的UHPLC-PDA开发的方法和验证。通过乳液溶剂蒸发法制备五种不同的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-NP显示出97.36 +/-2.01nm的粒度，具有0.263 +/-0.004的低PDI值、-17.98 +/-1.09的ZP、82.49 +/-2.38%的EE和5.09 +/-0.13%的DL。THQ-N1-NP通过体外释放曲线显示出持续释放模式。通过UHPLC-PDA开发并验证了生物分析方法，用于评价药代动力学参数，生物分布研究，脑靶向潜力（89.89 +/- 9.38%），脑靶向效率（8075.00 +/- 113.05%）研究，与静脉给药相比，鼻内给药显示出改善的THQ-脑生物利用度。此外，THQ-PLGA-NP改善癫痫发作阈值治疗，即癫痫增加电流电休克（ICES）啮齿动物模型诱导大鼠癫痫发作。确立了具有纳米制剂的高脑靶向效率的THQ-PLGA-NP的显著作用。报告的数据支持癫痫的治疗。
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.