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Homogeneous Nanoparticles To Enhance the Efficiency of a Hydrophobic Drug, Antihyperlipidemic Probucol, Characterized by Solid-State NMR

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journal contribution
posted on 01.02.2010, 00:00 by Takeshi Io, Toshiro Fukami, Kazutoshi Yamamoto, Toyofumi Suzuki, Jiadi Xu, Kazuo Tomono, Ayyalusamy Ramamoorthy
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.