Selective uptake of surface-modified phospholipid vesicles by bone marrow macrophages in vivo

Keitaro Sou, Beth Goins, Shinji Takeoka, Eishun Tsuchida, William T. Phillips

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    46 Citations (Scopus)

    Abstract

    An advantage of using vesicles (liposomes) as drug delivery carriers is that their pharmacokinetics can be controlled by surface characteristics, which can permit specific delivery of the encapsulated agents to organs or cells in vivo. Here we report a vesicle formulation which targets the bone marrow after intravenous injection in rabbits. Surface modification of the vesicle with an anionic amphiphile; l-glutamic acid, N-(3-carboxy-1-oxopropyl)-, 1,5-dihexadecyl ester (SA) results in significant targeting of vesicles to bone marrow. Further incorporation of as little as 0.6 mol% of poly(ethylene glycol)-lipid (PEG-DSPE) passively enhanced the distribution of SA-vesicles into bone marrow and inhibited hepatic uptake. In this model, more than 60% of the intravenously injected vesicles were distributed to bone marrow within 6 h after administration of a small dose of lipid (15 mg/kg b.w.). Histological evidence indicates that the targeting was achieved due to uptake by bone marrow macrophages (BMMφ). The efficient delivery of encapsulated scintigraphic and fluorescent imaging agents to BMMφ suggests that vesicles are promising carriers for the specific targeting of BMMφ and may be useful for delivering a wide range of therapeutic agents to bone marrow.

    Original languageEnglish
    Pages (from-to)2655-2666
    Number of pages12
    JournalBiomaterials
    Volume28
    Issue number16
    DOIs
    Publication statusPublished - 2007 Jun

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    Keywords

    • Bone marrow
    • Drug delivery
    • Liposome
    • Macrophage
    • Nanoparticle
    • Surface modification

    ASJC Scopus subject areas

    • Biotechnology
    • Bioengineering
    • Biomedical Engineering

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