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Role of plasma lipoproteins in modifying the toxic effects of water-insoluble drugs: Studies with cyclosporine A

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Abstract

Lipoproteins are a heterogeneous population of macromolecular aggregates of lipids and proteins that are responsible for the transport of lipids through the vascular and extravascular fluids from their site of synthesis or absorption to peripheral tissues. Lipoproteins are involved in other biological processes as well, including coagulation and tissue repair, and serve as carriers of a number of hydrophobic compounds within the systemic circulation. It has been well documented that disease states (eg, AIDS, diabetes, cancer) significantly influence circulating lipoprotein content and composition. Therefore, it appears possible that changes in the lipoprotein profile would affect not only the ability of a compound to associate with lipoproteins but also the distribution of the compound within the lipoprotein subclasses. Such an effect could alter the pharmacokinetics and pharmacological action of the drug. This paper reviews the factors that influence the interaction of one model hydrophobic compound, cyclosporine A, with lipoproteins and the implications of altered plasma lipoprotein concentrations on the pharmacological behavior of this compound.

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Authors and Affiliations

  1. Division of Pharmaceutics and Biopharmaceutics, Faculty of Pharmaceutical Sciences, The University of British Columbia, V6T 1Z3, Vancouver, British Columbia, Canada

    Kishor M. Wasan, Manisha Ramaswamy, Mona Kwong & Kathy D. Boulanger

Authors
  1. Kishor M. Wasan
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  2. Manisha Ramaswamy
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  3. Mona Kwong
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  4. Kathy D. Boulanger
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Corresponding author

Correspondence to Kishor M. Wasan.

Additional information

Published: October 7, 2002

Note: This article was presented in part at the 2002 AAPS Pharmaceutics and Drug Delivery Conference, Arlington, VA, April 22–24, 2002.

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Wasan, K.M., Ramaswamy, M., Kwong, M. et al. Role of plasma lipoproteins in modifying the toxic effects of water-insoluble drugs: Studies with cyclosporine A. AAPS J 4, 30 (2002). https://doi.org/10.1208/ps040430

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  • DOI: https://doi.org/10.1208/ps040430

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