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首页> 外文期刊>Biomaterials >High-loading nanosized micelles of copoly(styrene-maleic acid)-zinc protoporphyrin for targeted delivery of a potent heme oxygenase inhibitor
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High-loading nanosized micelles of copoly(styrene-maleic acid)-zinc protoporphyrin for targeted delivery of a potent heme oxygenase inhibitor

机译：共聚（苯乙烯-马来酸）-锌原卟啉的高负载纳米胶束，用于靶向递送有效的血红素加氧酶抑制剂

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Amphiphilic styrene-maleic acid (SMA) copolymer efficiently formed micelles with a potent heme oxygenase inhibitor-zinc protoporphyrin (ZnPP). The micelles were constructed by subtle pH adjustments to form non-covalent interaction between the hydrophobic ZnPP and amphiphilic SMA. The micelles (SMA-ZnPP) thus formed were nanoparticles with narrow size distribution in water (mean diameter 176.5nm), having tunable loading (from 15% to 60% w/w of ZnPP) with remarkable aqueous solubility. SMA-ZnPP had an average molecular size of 144kDa as determined by size-exclusion chromatography (SEC), this size is a marked increase from the molecular weight of free ZnPP (626.03Da), suggesting the formation of micellar structure. The micelles showed a constant ZnPP release rate of about 0.5%/day in vitro at neutral pH. SMA-ZnPP micelles inhibited splenic microsomal HO-1 activity, in a competitive and dose-dependent manner, with an apparent inhibitory constant (K-i) of 0.12 mu m, comparable to free ZnPP and also exhibited marked cytotoxic effect on KYSE-510 human esophageal cancer cells. The unique features of SMA-ZnPP micelles are that they are nanoparticles in aqueous solution having high water solubility and loading, yet macromolecular in nature, which can be beneficial in targeted release of a potent HO-1 inhibitor. (c) 2006 Elsevier Ltd. All rights reserved.
机译：两亲性苯乙烯-马来酸（SMA）共聚物与有效的血红素加氧酶抑制剂-锌原卟啉（ZnPP）有效地形成了胶束。通过微调pH值来构建胶束，以在疏水性ZnPP与两亲性SMA之间形成非共价相互作用。由此形成的胶束（SMA-ZnPP）是在水中具有窄尺寸分布的纳米颗粒（平均直径176.5nm），具有可调节的负载（ZnPP的15％至60％w / w）和显着的水溶性。通过尺寸排阻色谱法（SEC）测定，SMA-ZnPP的平均分子大小为144kDa，该大小比游离ZnPP的分子量（626.03Da）显着增加，表明形成了胶束结构。胶束在中性pH下体外显示出约0.5％/天的恒定ZnPP释放速率。 SMA-ZnPP胶束以竞争性和剂量依赖性方式抑制脾微粒体HO-1的活性，其表观抑制常数（Ki）为0.12μm，与游离ZnPP相当，并且对KYSE-510人食道也显示出明显的细胞毒性作用癌细胞。 SMA-ZnPP胶束的独特特征是它们是水溶液中的纳米颗粒，具有高水溶性和高载量，但本质上是大分子的，这对于有效释放强效HO-1抑制剂可能是有益的。 （c）2006 Elsevier Ltd.保留所有权利。

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