Pharmacokinetics of long-circulating liposomes

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Abstract

Association of drugs with carriers such as liposomes has marked effects on both the pharmacokinetic profiles of the carrier and of the carrier-associated drug. In general, association of drugs with liposomes delays drug absorption, alters and restricts drug biodistribution, decreases the volume of distribution, delays clearance and retards drug metabolism. Surface modification of liposomes by the inclusion of hydrophilic components (e.g., carbohydrates, glycolipids or polymers) to form long-circulating liposomes causes changes in the pharmacokinetic pattern seen for unmodified (classical) liposomes. While classical liposomes have non-linear, saturable kinetics, long-circulating liposomes possess dose-independent, non-saturable, log-linear kinetics. The log-linear kinetics for long-circulating liposomes results from a significant decrease in the first phase of clearance into a high affinity, low capacity system, probably the cells of the mononuclear phagocyte system. An understanding of the pharmacokinetics of liposome-associated drugs is critical to the development of rationale strategies for therapeutic applications of long-circulating liposomes.

References (91)

  • M.R. Mauk et al.

    Preparation of lipid vesicles containing high levels of radioactive cations

    Anal. Biochem.

    (1979)
  • K.J. Hwang et al.

    Encapsulation, with high efficiency, of radioactive metal ions in liposomes

    Biochim. Biophys. Acta

    (1982)
  • E.F. Sommerman et al.

    125I labelled inulin: a convenient marker for deposition of liposomal contents in vivo

    Biochem. Biophys. Res. Commun.

    (1984)
  • J.F. Bridges et al.

    The uptake of liposome-entrapped 125I-labelled poly-vinylpyrrolidone by rat jejunum in vitro

    Biochim. Biophys. Acta

    (1978)
  • R.M. Abra et al.

    Liposome disposition in vivo. III. Dose and vesicle-size effects

    Biochim. Biophys. Acta

    (1981)
  • H. Ellens et al.

    In vivo fate of large unilamellar sphingomyelin-cholesterol liposomes after intraperitoneal and intravenous injection into rats

    Biochim. Biophys. Acta

    (1981)
  • T.M. Allen et al.

    Subcutaneous administration of liposomes: a comparison with the intravenous and intraperitoneal routes in injection

    Biochim. Biophys. Acta

    (1993)
  • T.M. Allen et al.

    Liposomes with prolonged circulation times: factors affecting uptake by reticuloendothelial and other tissues

    Biochim. Biophys. Acta

    (1989)
  • A.L. Klibanov et al.

    Activity of amphipathic poly(ethylene glycol) 5000 to prolong the circulation time of liposomes depends on the liposome size and is unfavourable for immunoliposomes binding to target

    Biochim. Biophys. Acta

    (1991)
  • D.C. Litzinger et al.

    Amphipathic poly(ethylene glycol) 5000-stabilized dioleoylphosphatidylethanolamine liposomes accumulate in spleen

    Biochim. Biophys. Acta

    (1992)
  • D.C. Litzinger et al.

    Effect of liposome size on the circulation time and intraorgan distribution of amphipathic poly(ethylene glycol)-containing liposomes

    Biochim. Biophys Acta

    (1994)
  • D. Liu et al.

    Large liposomes containing ganglioside GM1 accumulate effectively in spleen

    Biochim. Biophys. Acta

    (1991)
  • K. Maruyama et al.

    Proteins and peptides bound to long-circulating liposomes

    Biochim. Biophys. Acta

    (1991)
  • K. Maruyama et al.

    Prolonged circulation time in vivo of large unilamellar liposomes composed of distearoylphosphatidylcholine and cholesterol containing amphipathic poly(ethylene glycol)

    Biochim. Biophys. Acta

    (1992)
  • A. Mori et al.

    Influence of the steric barrier activity of amphipathic poly(ethyleneglycol) and ganglioside GM1 on the circulation time of liposomes and on the target binding of immunoliposomes in vivo

    FEBS Lett.

    (1991)
  • M.J. Parr et al.

    Factors influencing the retention and chemical stability of poly(ethyleneglycol)-lipid conjugates incorporated into large unilamellar liposomes

    Biochim. Biophys. Acta

    (1994)
  • M.C. Woodle et al.

    Versatility in lipid composition showing prolonged circulation with sterically stabilized liposomes

    Biochim. Biophys. Acta

    (1992)
  • M.C. Woodle et al.

    Sterically stabilized liposomes

    Biochim. Biophys. Acta

    (1992)
  • R.L. Juliano et al.

    Effects of particle size and charge on the clearance of liposomes and liposome-encapsulated drugs

    Biochem. Biophys. Res. Commun.

    (1975)
  • D. Liu et al.

    Role of liposome size and RES blockade in controlling biodistribution and tumor uptake of GM1-containing liposomes

    Biochim. Biophys. Acta

    (1992)
  • J.H. Senior et al.

    Interaction of positively charged liposomes with blood: implications for their applications in vivo

    Biochim. Biophys. Acta

    (1991)
  • M.J. Parr et al.

    The presence of GM1 in liposomes with entrapped doxorubicin does not prevent RES blockade

    Biochim. Biophys. Acta

    (1993)
  • I.A.J.M. Bakker-Woudenberg et al.

    Enhanced localization of liposomes with prolonged blood circulation time in infected lung tissue

    Biochim. Biophys. Acta

    (1992)
  • S. Kim

    Liposomes as carriers of cancer chemotherapy: current status and future prospects

    Drugs

    (1994)
  • M.R. Niesman

    The use of liposomes as drug carriers in ophthalmology

    Crit. Rev. Ther. Drug Carrier Syst.

    (1992)
  • I.A. Bakker-Woudenberg et al.

    Liposomes as carriers of antimicrobial agents or immunomodulatory agents in the treatment of infections

    Eur. J. Clin. Microbiol. Infect. Dis.

    (1993)
  • S.E. Seltzer

    The role of liposomes in diagnostic imaging

    Radiology

    (1989)
  • K.J. Hwang

    Liposome pharmacokinetics

  • D.D. Lasic

    Liposomes: from Physics to Applications

    (1993)
  • Y. Namba et al.

    Glucuronate-modified liposomes with prolonged circulation time

    Chem. Pharm. Bull. (Tokyo)

    (1990)
  • S. Mumtaz et al.

    Design of liposomes for circumventing the reticuloendothelial cells

    Glycobiology

    (1991)
  • D. Papahadjopoulos et al.

    Sterically stabilized liposomes: improvements in pharmacokinetics and antitumor therapeutic efficacy

  • A. Gabizon et al.

    An improved method for in vivo tracing and imaging of liposomes using a gallium 67-desferoximine complex

    J. Liposome Res.

    (1989)
  • A. Gabizon et al.

    Preclinical and clinical experience with a doxorubicin-liposome preparation

    J. Liposome Res.

    (1990)
  • A. Gabizon et al.

    Pharmacokinetics and tissue distribution of doxorubicin encapsulated in stable liposomes with long circulation times

    J. Natl. Cancer Inst.

    (1989)
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