Lactoferrin-conjugated PEG-PLA nanoparticles with improved brain delivery: In vitro and in vivo evaluations
Lactoferrin-conjugated PEG-PLA nanoparticles with improved brain delivery: In vitro and in vivo evaluations
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DOI：
10.1016/j.jconrel.2008.10.016
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发表时间：
2009-02-20
影响因子：
10.8
通讯作者：
Jiang, Xinguo
中科院分区：
文献类型：
--
作者：
Hu, Kaili;Li, Jingwei;Jiang, Xinguo
本文构建了乳铁蛋白（Lf）聚乙二醇-聚乳酸纳米粒（Lf-NP），并对其体内外给药性能进行了评价。将Lf硫醇化并缀合至聚乙二醇化纳米颗粒上周围的远端马来酰亚胺官能团以形成Lf-NP。通过TEM观察和XPS分析证实了Lf-NP表面上Lf的存在。Lf ELISA结果证实了偶联程序后Lf的生物降解活性，并表明每个纳米颗粒上偶联的Lf的平均数量为约55。为了评估Lf-NP的脑递送性质，将荧光探针香豆素-6掺入bEnd.3细胞中。静脉给药后，Lf-NP携带的香豆素-6在小鼠脑中的含量是NP携带的近3倍。细胞活力实验结果证实了可生物降解的Lf-NP具有良好的安全性。显著的体内外实验结果表明Lf-NP是一种有前途的低毒脑给药系统。(c)2008 Elsevier B. V.保留所有权利。
The lactoferrin (Lf) conjugated poly (ethyleneglycol)-poly (lactide) nanoparticle (Lf-NP) was constructed in this paper as a novel biodegradable brain drug delivery system with evaluation of its in vitro and in vivo delivery properties. Lf was thiolated and conjugated to the distal maleimide functions surrounding on the pegylated nanoparticles to form the Lf-NP. The existence of Lf on the surface of Lf-NP was verified by TEM observation and XPS analysis. The Lf ELISA results confirmed the biorecognitive activity of Lf after the coupling procedure and suggested the average number of Lf conjugated on each nanoparticle was around 55. a fluorescent probe, coumarin-6 was incorporated into To evaluate the brain delivery properties of the Lf-NP, it. The uptake of Lf-NP by bEnd.3 cells was shown significantly higher than that of unconjugated nanoparticle (NP). Following an intravenous administration, a near 3 folds of coumarin-6 were found in the mice brain carried by Lf-NP compared to that carried by NP. Cell viability experiment results confirmed good safety of the biodegradable Lf-NP. The significant in vitro and in vivo results suggest that Lf-NP is a promising brain drug delivery system with low toxicity. (c) 2008 Elsevier B.V. All rights reserved.