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Targeting of lipid vesicles: specificity of carbohydrate receptor analogues for leukocytes in mice

M R Mauk, R C Gamble, J D Baldeschwieler

    Proceedings of the National Academy of Sciences of the United States of America
    |August 1, 1980
    PubMed

    Insights

    Surface carbohydrate modifications significantly impact vesicle stability and tissue targeting in mice. Specific 6-aminomannose modifications enhance vesicle integrity and influence distribution after administration.

    Area of Science:

    • Biomedical Engineering
    • Materials Science
    • Pharmacology

    Background:

    • Unilamellar distearoyl phosphatidylcholine vesicles are utilized for drug delivery.
    • Understanding vesicle stability and tissue specificity is crucial for effective in vivo applications.

    Purpose of the Study:

    • To investigate how surface carbohydrate modifications affect vesicle stability and tissue distribution in mice.
    • To determine the role of specific carbohydrate structures in vesicle targeting and clearance.

    Main Methods:

    • Utilized gamma-ray probe (111In3+) for tissue distribution analysis via gamma counting.
    • Employed perturbed angular correlation spectroscopy to assess vesicle structural integrity.
    • Administered modified vesicles intravenously and subcutaneously to mice.

    Main Results:

    • 6-aminomannose modification led to initial lung retention and subsequent liver/spleen concentration of intact vesicles after intravenous injection.
    • Subcutaneous administration of 6-aminosugar vesicles resulted in accumulation in polymorphonuclear leukocytes.
    • 6-aminomannose-labeled vesicles exhibited superior in vivo stability compared to other tested systems.

    Conclusions:

    • Surface carbohydrate modifications dramatically influence vesicle stability and tissue specificity.
    • Specific receptor topography is important for vesicle transport and elimination.
    • 6-aminomannose modification represents a promising strategy for enhancing vesicle in vivo performance.

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