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一种基于超高效液相色谱法的生物分析方法，用于定量测定用于癫痫治疗的载百里醌聚乳酸-羟基乙酸共聚物纳米颗粒。

A bioanalytical UHPLC based method used for the quantification of Thymoquinone-loaded-PLGA-nanoparticles in the treatment of epilepsy.

作者信息

Ahmad Niyaz, Ahmad Rizwan, Al Qatifi Sadiq, Alessa Mahdi, Al Hajji Hassan, Sarafroz Md

机构信息

1Department of Pharmaceutics, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia.

2Department of Pharmaceutical Chemistry, College of Clinical Pharmacy, Imam Abdulrahman Bin Faisal University, Dammam, Kingdom of Saudi Arabia.

出版信息

BMC Chem. 2020 Feb 14;14(1):10. doi: 10.1186/s13065-020-0664-x. eCollection 2020 Dec.

DOI:10.1186/s13065-020-0664-x
PMID:32083254
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7023730/
Abstract

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.

摘要

为了制备一种纳米制剂（PLGA-NPs）并通过鼻内给药提高百里醌（THQ）的脑生物利用度，采用新开发的UHPLC-PDA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-NPs（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。优化后的THQ-N1-NPs粒径为97.36±2.01nm，PDI值低至0.263±0.004，ZP为-17.98±1.09，包封率为82.49±2.38%，载药量为5.09±0.13%。THQ-N1-NPs通过体外释放曲线显示出缓释模式。通过UHPLC-PDA开发了一种生物分析方法，并进行了验证，用于评估药代动力学参数、生物分布研究、脑靶向潜力（89.89±9.38%）和脑靶向效率（8075.00±113.05%）研究，通过鼻内给药显示与静脉注射相比，THQ的脑生物利用度有所提高。此外，THQ-PLGA-NPs改善了癫痫阈值治疗，即改善了癫痫大鼠模型中电流电击（ICES）诱导的癫痫发作。确定了具有高脑靶向效率的纳米制剂THQ-PLGA-NPs的重要作用。报告的数据支持癫痫的治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/de6021621f60/13065_2020_664_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/6273769c9582/13065_2020_664_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/4606a203ba40/13065_2020_664_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/e60e80023393/13065_2020_664_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/b917ebf49c6d/13065_2020_664_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/a16dce949064/13065_2020_664_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/f5c46af9b1a7/13065_2020_664_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/88eae4be6d68/13065_2020_664_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/de6021621f60/13065_2020_664_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/6273769c9582/13065_2020_664_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/4606a203ba40/13065_2020_664_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/e60e80023393/13065_2020_664_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/b917ebf49c6d/13065_2020_664_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/a16dce949064/13065_2020_664_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/f5c46af9b1a7/13065_2020_664_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/88eae4be6d68/13065_2020_664_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/458f/7023730/de6021621f60/13065_2020_664_Fig8_HTML.jpg

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