Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats.
Pharmacokinetics of Quercetin-Loaded Methoxy Poly(ethylene glycol)-b-poly(L-lactic acid) Micelle after Oral Administration in Rats.
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槲皮素甲氧基聚乙二醇-b-聚(L-乳酸)胶束大鼠口服后的药代动力学
DOI：
10.1155/2017/1750895
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发表时间：
2017
影响因子：
--
通讯作者：
Huang X
中科院分区：
文献类型：
--
作者：
Lv L;Liu C;Li Z;Song F;Li G;Huang X
本研究的目的是评估胶束改变槲皮素（QUT）药代动力学的潜力，主要目的是提高其口服生物利用度。采用薄膜水合法制备了QUT负载甲氧基聚乙二醇-b-聚乳酸胶束（QUT负载MPEG-b-PLLA胶束），粒径为88.5 nm。建立了测定大鼠血浆中QUT浓度的液相色谱-串联质谱法（LC-MS/MS）。色谱柱为Agilent C18（4.6 mm × 50 mm，3.5 μm），移动的相为水：甲醇（30：70，v/v），流速为0.4 mL/min，QUT在2.5 ~ 2000 ng/mL范围内线性关系良好。大鼠单次口服该胶束，评价其药代动力学参数，并与QUT水混悬液给药进行比较。结果表明，与QUT水悬浮液相比，胶束能够将QUT的口服生物利用度提高9倍。这些结果表明，甲氧基聚乙二醇-b-聚（L-乳酸）是一个潜在的载体QUT的口服。
The purpose of this study was to evaluate the potential of micelle to change the pharmacokinetics of quercetin (QUT), with a primary goal of enhancing its oral bioavailability. QUT-loaded methoxy poly(ethylene glycol)-b-poly(L-lactic acid) micelle (QUT-loaded MPEG-b-PLLA micelle) was prepared by a thin-film hydration method, resulting in a particle size of 88.5 nm. A liquid chromatography tandem-mass spectrometry (LC-MS/MS) method was developed and validated for determination of QUT in rat plasma. The chromatographic separation was performed on an Agilent Eclipse-C18 (4.6 mm × 50 mm, 3.5 μm) with an isocratic mobile phase system consisting of water and methanol (30 : 70, v/v) at a flow rate of 0.4 mL/min. Calibration curves were linear over the concentration ranges of 2.5–2000 ng/mL for QUT. The micelle was orally administered at a single does in rats, and the pharmacokinetic parameters were evaluated and compared with that administered with the QUT aqueous suspension. The results show that the micelle was able to increase the QUT's oral bioavailability 9-fold compared to the QUT aqueous suspension. These results suggest that methoxy poly(ethylene glycol)-b-poly(L-lactic acid) is a potential carrier for the oral delivery of QUT.
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影响因子：
6.2
作者：
Bensaid, Fethi;du Boullay, Olivier Thillaye;Bourissou, Didier
通讯作者：
Bourissou, Didier
影响因子：
3.4
作者：
Mohsen, Amira Mohamed;AbouSamra, Mona Mahmoud;ElShebiney, Shaimaa Ahmed
通讯作者：
ElShebiney, Shaimaa Ahmed
影响因子：
10.8
作者：
Li, HouLi;Zhao, XiaoBin;Lou, HongXiang
通讯作者：
Lou, HongXiang
DOI：
10.1016/j.jchromb.2017.02.029
发表时间：
2017-04-01
影响因子：
3
作者：
Maher, Hadir M.;Alzoman, Nourah Z.;Abahussain, Ashwag O.
通讯作者：
Abahussain, Ashwag O.
DOI：
10.4103/0973-7847.194044
发表时间：
2016-07
期刊：
Pharmacognosy reviews
影响因子：
--
作者：
Anand David AV;Arulmoli R;Parasuraman S
通讯作者：
Parasuraman S