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pH-sensitive liposomes: possible clinical implications

M B Yatvin, W Kreutz, B A Horwitz

    Science (New York, N.Y.)
    |December 12, 1980
    PubMed
    Summary
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    pH-sensitive liposomes loaded with palmitoyl homocysteine (PHC) enable targeted drug delivery. These liposomes release drugs effectively in lower pH environments, such as tumors and inflamed tissues, for enhanced therapeutic efficacy.

    Area of Science:

    • Biochemistry
    • Materials Science
    • Pharmacology

    Background:

    • Liposomes are versatile drug delivery vehicles.
    • pH-sensitive liposomes offer potential for targeted drug release.
    • Specific lipid compositions can modulate liposome responsiveness to pH changes.

    Purpose of the Study:

    • To construct and characterize liposomes incorporating the pH-sensitive lipid palmitoyl homocysteine (PHC).
    • To evaluate the pH-dependent drug release profile of these liposomes near physiological temperatures.
    • To assess the potential clinical utility of PHC-liposomes for targeted drug delivery.

    Main Methods:

    • Liposomes were formulated with the pH-sensitive lipid palmitoyl homocysteine (PHC).
    • Drug release assays were performed across a pH gradient (6.0 to 7.4) near physiological temperature.

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  • Liposome characteristics and drug release kinetics were analyzed.
  • Main Results:

    • Liposomes containing PHC demonstrated significant pH-dependent drug release.
    • The greatest pH differential for drug release was observed between pH 6.0 and 7.4.
    • Release profiles were optimized near physiological temperatures.

    Conclusions:

    • PHC-containing liposomes are effective pH-sensitive drug delivery systems.
    • These liposomes show promise for targeted drug delivery to acidic physiological sites.
    • Potential clinical applications include cancer therapy and treatment of inflammatory conditions.