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Techniques for encapsulating bioactive agents into liposomes.

L D Mayer, M B Bally, M J Hope

    Chemistry and Physics of Lipids
    |June 1, 1986
    PubMed
    Summary
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    Efficiently trapping hydrophilic and hydrophobic compounds in liposomes is crucial for drug delivery. This review covers passive and active liposome entrapment techniques, including ion gradients for near-100% efficiency with cationic drugs.

    Area of Science:

    • Pharmaceutical Sciences
    • Biotechnology
    • Drug Delivery Systems

    Background:

    • Liposomes are essential for delivering biologically active agents.
    • Efficient and rapid entrapment of therapeutic compounds is a prerequisite for liposome applications.
    • Existing methods for encapsulating diverse compounds into liposomes require comprehensive review.

    Purpose of the Study:

    • To review available techniques for entrapping hydrophilic and hydrophobic compounds into liposomes.
    • To discuss factors influencing the selection of appropriate liposomal systems and entrapment methods.
    • To highlight advanced active trapping procedures for enhanced drug encapsulation.

    Main Methods:

    • Review of passive entrapment techniques for multilamellar vesicles (MLVs) and unilamellar vesicles (UVs).

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  • Analysis of active trapping procedures utilizing charged lipids and transmembrane ion gradients.
  • Evaluation of methods for concentrating lipophilic cationic drugs within liposomes.

    • Main Results:

    • Various passive and active methods exist for liposome entrapment of diverse compounds.
    • Transmembrane ion gradients enable highly efficient (approaching 100%) trapping of lipophilic cationic drugs.
    • Selection of method depends on compound properties and desired liposomal characteristics.

    Conclusions:

    • Efficient liposome entrapment is critical for successful drug delivery applications.
    • Active trapping methods, particularly ion gradients, offer superior efficiency for specific drug types.
    • This review provides a guide for selecting optimal liposome preparation techniques.