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Nanoparticle Processing in the Solid State Dramatically Increases the Cell Membrane Permeation of a Cholesterol-Lowering Drug, Probucol

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Download Hi-Res ImageDownload to MS-PowerPointCite This:Mol. Pharmaceutics 2009, 6, 3, 1029-1035
    Brief Article

    Nanoparticle Processing in the Solid State Dramatically Increases the Cell Membrane Permeation of a Cholesterol-Lowering Drug, Probucol
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    College of Pharmacy, Nihon University, Chiba 274-8555, Japan, and Department of Pharmaceutical Sciences, College of Pharmacy, Biophysics and Department of Chemistry, University of Michigan, Ann Arbor, Michigan 48109
    * Corresponding authors: Dr. Toshiro Fukami, Research Unit of Pharmaceutics, College of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi, Chiba 274-8555 Japan. Phone: +81-47-465-6699. Fax: +81-47-465-2158. E-mail: [email protected]. Prof. Ayyalusamy Ramamoorthy, Biophysics and Department of Chemistry, University of Michigan, Ann Arbor, MI 48109-1055. Phone: 734-647-6572. Fax: 734-615-3790. E-mail: [email protected]
    †College of Pharmacy, Nihon University.
    ‡Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan.
    §Biophysics and Department of Chemistry, University of Michigan.
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    Molecular Pharmaceutics

    Cite this: Mol. Pharmaceutics 2009, 6, 3, 1029–1035
    Click to copy citationCitation copied!
    https://doi.org/10.1021/mp9000487
    Published March 12, 2009
    Copyright © 2009 American Chemical Society
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    Abstract

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    High cholesterol levels (or hypercholesterolemia) are linked with many diseases, particularly with the risk of coronary heart diseases. Probucol is commonly used to reduce cholesterol in blood. While the effectiveness of this drug highly depends on its solubility, unfortunately, it is nearly insoluble (solubility is 5 ng/mL in water). Therefore, it is essential to develop approaches to increase its solubility and bioavailability and to enhance the efficiency of the drug. Here we show that a new method increases the solubility of probucol in water and its ability to permeate cell membranes. This new method of processing the drug in a nanoparticle utilizes the grinding of PBC probucol together with sodium dodecylsulfate and methacrylic copolymer. Solid-state NMR experiments reveal the polymorphic state of probucol and the conversion of this drug from crystalline to the amorphous state, and determine its nearness to the copolymer due to the grinding process that enables the formation of nanoparticles.

    Copyright © 2009 American Chemical Society

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    Details of the experimental procedures and additional data. This material is available free of charge via the Internet at http://pubs.acs.org.

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    Cited By

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    Molecular Pharmaceutics

    Cite this: Mol. Pharmaceutics 2009, 6, 3, 1029–1035
    Click to copy citationCitation copied!
    https://doi.org/10.1021/mp9000487
    Published March 12, 2009
    Copyright © 2009 American Chemical Society
    Request reuse permissions

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