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一种将疏水性化合物封装在阳离子聚合物纳米粒子内的新方法。

A new method for encapsulating hydrophobic compounds within cationic polymeric nanoparticles.

机构信息

Department of Chemical Engineering, Technion-Israel Institute of Technology, Technion City, Haifa, Israel.

出版信息

J Microencapsul. 2013;30(6):580-8. doi: 10.3109/02652048.2013.764940. Epub 2013 Mar 14.

Abstract

Here we present the newly developed "solvent exchange" method that overcomes the challenge of encapsulating hydrophobic compounds within nanoparticle of water soluble polymers. Our studies involved the model polymer polyvinylpyrrolidone (PVP) and the hydrophobic dye Nile red. We found that the minimum molecular weight of the polymer required for nanoparticle formation was 49 KDa. Dynamic Light Scattering (DLS) and Cryo-Transmission Electron Microscopy (cryo-TEM) studies revealed spherical nanoparticles with an average diameter ranging from 20 to 33 nm. Encapsulation efficiency was evaluated using UV spectroscopy and found to be around 94%. The nanocarriers were found to be highly stable; less than 2% of Nile red release from nanoparticles after the addition of NaCl. Nanoparticles containing Nile red were able to penetrate into glioma cells. The solvent exchange method was proved to be applicable for other model hydrophobic drug molecules including ketoprofen, ibuprofen and indomethacin, as well as other solvents.

摘要

在这里,我们提出了一种新的“溶剂交换”方法,克服了将疏水性化合物封装在水溶性聚合物纳米粒子内的挑战。我们的研究涉及模型聚合物聚乙烯吡咯烷酮(PVP)和疏水性染料尼罗红。我们发现,形成纳米粒子所需的聚合物的最小分子量为 49 kDa。动态光散射(DLS)和低温传输电子显微镜(cryo-TEM)研究表明,纳米粒子呈球形,平均直径在 20 至 33nm 之间。使用紫外光谱法评估了包封效率,发现约为 94%。纳米载体非常稳定;加入 NaCl 后,从纳米粒子中释放的尼罗红不到 2%。含有尼罗红的纳米粒子能够穿透神经胶质瘤细胞。溶剂交换法被证明适用于其他模型疏水性药物分子,包括酮洛芬、布洛芬和吲哚美辛以及其他溶剂。

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