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Related Experiment Videos

Studies on liposome-encapsulated heparin.

T D Kim, M Sakon, T Kawasaki

    Thrombosis Research
    |September 15, 1986
    PubMed
    Summary

    Encapsulating heparin into liposomes (lipo-heparin) prolongs its anticoagulant activity in vivo. This lipo-heparin formulation shows potential for clinical applications, pending further safety studies.

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    Area of Science:

    • Biomedical Engineering
    • Pharmacology
    • Drug Delivery Systems

    Background:

    • Heparin is a widely used anticoagulant.
    • Short in vivo duration limits heparin's therapeutic efficacy.
    • Liposome encapsulation offers a strategy to modify drug pharmacokinetics.

    Purpose of the Study:

    • To develop and evaluate liposome-encapsulated heparin (lipo-heparin) for prolonged anticoagulant activity.
    • To assess the stability and in vivo efficacy of lipo-heparin.
    • To determine the potential clinical applicability of this formulation.

    Main Methods:

    • Heparin was encapsulated into large multilamellar vesicles (liposomes).
    • Liposome-heparin activity, recovery, and stability were assessed.
    • In vivo anticoagulant activity was evaluated in rats after intravenous administration.
    • Neutralization by protamine sulfate was investigated.

    Main Results:

    • Liposome-encapsulated heparin (lipo-heparin) was successfully prepared with particle sizes of 0.5-4.0 microns.
    • The formulation exhibited stable anticoagulant activity at 4°C for at least two weeks.
    • Intravenous administration in rats demonstrated a threefold prolongation of anticoagulant activity compared to unfractionated heparin.
    • Lipo-heparin's activity was effectively neutralized by protamine sulfate.

    Conclusions:

    • Liposome encapsulation significantly prolongs the in vivo anticoagulant effect of heparin.
    • Lipo-heparin demonstrates potential for clinical use as an anticoagulant.
    • Further research is required to evaluate potential side effects associated with liposome administration.

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