均一纳米颗粒提高疏水性药物降脂作用效率的研究 应用固态 NMR 技术进行表征
Homogeneous nanoparticles to enhance the efficiency of a hydrophobic drug, antihyperlipidemic probucol, characterized by solid-state NMR.
机构信息
College of Pharmacy, Nihon University, Chiba 274-8555, Japan.
出版信息
Mol Pharm. 2010 Feb 1;7(1):299-305. doi: 10.1021/mp900254y.
Abstract
A low absorption in the gastrointestinal tract of hydrophobic pharmaceutical compounds in use today considerably limits their bioavailability, and therefore they are taken in large doses in order to reach the therapeutic plasma concentration, which inevitably results in undesired side effects. In this study, we demonstrate a new nanoparticle approach to overcome this problem, and our experimental results show that this approach has a high efficiency of drug loading and is easily adaptable to industrial scale. Characterization of nanoparticles containing a cholesterol-lowering hydrophobic drug, probucol, using a variety of biophysical techniques revealed higher homogeneity of these particles compared to those prepared using other approaches. Intermolecular interactions of these nanoparticles are probed at high resolution by magic angle spinning solid-state NMR experiments.
摘要
目前使用的疏水性药物化合物在胃肠道中的吸收率较低，这极大地限制了它们的生物利用度，因此为了达到治疗性血浆浓度，这些药物往往需要大剂量服用，这不可避免地会导致不良的副作用。在本研究中，我们展示了一种克服这个问题的新的纳米颗粒方法，我们的实验结果表明，这种方法具有很高的药物负载效率，并且很容易适应工业规模。使用各种生物物理技术对含有降胆固醇疏水性药物普罗布考的纳米颗粒进行表征，结果表明这些颗粒比使用其他方法制备的颗粒具有更高的均一性。通过魔角旋转固态 NMR 实验以高分辨率探测这些纳米颗粒的分子间相互作用。
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