Orally administered nanocurcumin to attenuate morphine tolerance: comparison between negatively charged PLGA and partially and fully PEGylated nanoparticles.
Orally administered nanocurcumin to attenuate morphine tolerance: comparison between negatively charged PLGA and partially and fully PEGylated nanoparticles.
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口服纳米姜黄素可减弱吗啡耐受性：带负电荷的 PLGA 与部分和完全聚乙二醇化纳米颗粒之间的比较。
DOI：
10.1021/mp400358z
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发表时间：
2013
影响因子：
4.9
通讯作者：
Liu,Ying
中科院分区：
文献类型：
--
作者：
Shen,Hao;Hu,Xiaoyu;Szymusiak,Magdalena;Wang,ZaijieJim;Liu,Ying
我们将疏水性姜黄素[1,7-双-(4-羟基-3-甲氧基苯基)-1,6-庚二烯-3,5-二酮]配制成稳定的纳米颗粒悬浮液（纳米姜黄素），以克服其相对较低的生物利用度、较高的代谢率以及快速从体内消除和清除的问题。以姜黄素纳米制剂为平台，我们发现姜黄素具有减轻吗啡耐受的潜力。两种类型的稳定聚合物纳米粒子，聚乳酸-乙醇酸共聚物 (PLGA) 和聚乙二醇-b-聚乳酸 (PEG-b-PLA)，以及两者的混合物是使用闪蒸纳米沉淀与喷雾干燥相结合产生的。优化后的制剂具有高载药量（>45%）、粒径小、分布窄、表面性质可控等特点。进行小鼠行为研究（甩尾和热板测试）以验证纳米姜黄素对减弱吗啡耐受性的作用。在皮下注射吗啡后，使用口服纳米姜黄素进行甩尾和热板试验，在小鼠中观察到显着的镇痛作用。然而，相同剂量的未配制的姜黄素没有显示出效果。与聚乙二醇化纳米姜黄素相比，带负电的PLGA纳米颗粒表现出更好的功能。
We have formulated hydrophobic curcurmin [1,7-bis-(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] into stable nanoparticle suspensions (nanocurcumin) to overcome its relatively low bioavailability, high rate of metabolism, and rapid elimination and clearance from the body. Employing the curcumin nanoformulations as the platform, we discovered that curcumin has the potential to alleviate morphine tolerance. The two types of stable polymeric nanoparticles, poly(lactic-co-glycolic acid) (PLGA) and poly(ethylene glycol)-b-poly(lactic acid) (PEG-b-PLA), and the hybrid of the two were generated using flash nanoprecipitation integrated with spray drying. The optimized formulations have high drug loading (>45%), small particles size with narrow distribution, and controlled surface properties. Mice behavioral studies (tail-flick and hot-plate tests) were conducted to verify the effects of nanocurcumin on attenuating morphine tolerance. Significant analgesia was observed in mice during both tail-flick and hot-plate tests using orally administered nanocurcumin following subcutaneous injections of morphine. However, unformulated curcumin at the same dose showed no effect. Compared with PEGylated nanocurcumin, negatively charged PLGA nanoparticles showed better functionality.
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影响因子：
56.9
作者：
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通讯作者：
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作者：
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DOI：
--
发表时间：
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期刊：
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影响因子：
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DOI：
--
发表时间：
2012
期刊：
Journal of Pharmacy and Science
影响因子：
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作者：
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