Liposomes with entrapped doxorubicin exhibit extended blood residence times

Biochim Biophys Acta. 1990 Mar 30;1023(1):133-9. doi: 10.1016/0005-2736(90)90018-j.

Abstract

The blood residence time of liposomes with entrapped doxorubicin is shown to be significantly longer than for identically prepared empty liposomes. Liposomal doxorubicin systems with a drug-to-lipid ratio of 0.2 (w/w) were administered at a dose of 100 mg lipid/kg. Both doxorubicin and liposomal lipid were quantified in order to assess in vivo stability and blood residence times. For empty vesicles composed of phosphatidylcholine (PC)/cholesterol (55:45, mole ratio) and sized through filters of 100 nm pore size, 15-25% of the administered lipid dose was recovered in the blood 24 h after i.v. injection. The percentage of the dose retained in the circulation at 24 h increased 2-3-fold when the liposomes contain entrapped doxorubicin. For 100 nm distearoyl PC/chol liposomal doxorubicin systems, as much as 80% of the injected dose of lipid and drug remain within the blood compartment 24 h after i.v. administration.

MeSH terms

  • Animals
  • Cholesterol / blood
  • Doxorubicin / blood*
  • Drug Carriers
  • Drug Compounding
  • Female
  • Kinetics
  • Liposomes*
  • Mice
  • Mice, Inbred DBA
  • Phosphatidylcholines / blood

Substances

  • Drug Carriers
  • Liposomes
  • Phosphatidylcholines
  • Doxorubicin
  • Cholesterol