Factors affecting the pharmacokinetics and pharmacodynamics of liposomal drugs

J Liposome Res. 2012 Sep;22(3):177-92. doi: 10.3109/08982104.2012.655285. Epub 2012 Feb 15.


Various attempts to increase the therapeutic index of the drug while minimizing side effects have been made in drug delivery systems. Among several promising strategies, liposomes represent an advanced technology to target active molecules to the site of action. Rapid clearance of circulating liposomal drugs administered intravenously has been a critical issue because circulation time in the blood affects drug exposure at the target site. The clinical use of liposomal drugs is complicated by large intra- and interindividual variability in their pharmacokinetics (PK) and pharmacodynamics (PD). Thus, it is important to understand the factors affecting the PK/PD of the liposomal formulation of drugs and to elucidate the mechanisms underlying the variability in the PK/PD of liposomal drugs. In this review article, we describe the characteristics of liposome formulations and discuss the effects of various factors, including liposome-associated factors, host-associated factors, and treatment on the PK/PD of liposomal agents.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Chemistry, Pharmaceutical / classification
  • Chemistry, Pharmaceutical / methods
  • Clinical Trials as Topic
  • Doxorubicin / pharmacokinetics*
  • Doxorubicin / pharmacology*
  • Drug Delivery Systems / methods*
  • Drug Interactions
  • Humans
  • Lipid Bilayers / chemistry
  • Liposomes
  • Neoplasms / drug therapy
  • Particle Size
  • Surface Properties
  • Time Factors
  • Tissue Distribution


  • Antineoplastic Agents
  • Lipid Bilayers
  • Liposomes
  • Doxorubicin