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An efficient method for loading indium-111 into liposomes using acetylacetone

P L Beaumier, K J Hwang

    Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
    |September 1, 1982
    PubMed
    Summary
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    Acetylacetone efficiently loads Indium-111 (In-111) into liposomes by mediating ion transport. This method successfully concentrates In-111 within liposomes, which remain stable in serum.

    Area of Science:

    • Nanotechnology
    • Radiochemistry
    • Biomedical Engineering

    Background:

    • Liposomes are widely used drug delivery systems.
    • Efficiently encapsulating radioisotopes like Indium-111 (In-111) into liposomes is crucial for imaging and therapy.
    • Current methods face challenges in achieving high loading efficiency and stability.

    Purpose of the Study:

    • To develop an efficient method for loading high levels of In-111 into liposomes.
    • To investigate the mechanism of In-111 transport and retention within liposomes.
    • To assess the stability of In-111 loaded liposomes in biological conditions.

    Main Methods:

    • Utilized acetylacetone, a water-soluble lipophilic chelate, to form an acetylacetone-In-111 complex.
    • Incubated the complex with liposomes pre-loaded with nitrilotriacetic acid (NTA).

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  • Conducted loading in isotonic saline with Tris-HCl buffer at room temperature.
  • Evaluated liposome stability by incubating loaded liposomes in serum at 37°C for 24 hours.
  • Main Results:

    • Achieved efficient loading of high In-111 levels into the inner aqueous compartment of liposomes.
    • Acetylacetone mediated the transport of In-111 across the lipid bilayer to the encapsulated NTA.
    • Up to 90% of acetylacetone-chelated In-111 was internalized and bound by NTA.
    • Loaded liposomes demonstrated excellent retention of In-111 when incubated with serum.

    Conclusions:

    • Acetylacetone is an effective agent for the efficient loading of In-111 into liposomes.
    • The developed method ensures high encapsulation efficiency and stability of In-111 within liposomes.
    • These findings support the potential of In-111 loaded liposomes for biomedical applications.