Uptake of adriamycin into large unilamellar vesicles in response to a pH gradient

Biochim Biophys Acta. 1986 May 9;857(1):123-6. doi: 10.1016/0005-2736(86)90105-7.

Abstract

Previous work has shown that adriamycin can be accumulated into large unilamellar vesicle (LUV) systems in response to K+ diffusion potential established by valinomycin. It is demonstrated here that adriamycin can also be rapidly and efficiently accumulated into egg phosphatidylcholine (egg PC) and egg PC-cholesterol (1:1) LUVs in response to a transmembrane pH gradient (interior acidic) in the absence of ionophores. This 'active' loading gives rise to trapping efficiencies as high as 98%, interior drug concentrations as high as 100 mM and significantly enhances drug retention within the vesicles. This procedure may be of general utility for loading liposomal systems for in vivo drug delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Carbonyl Cyanide m-Chlorophenyl Hydrazone
  • Cholesterol
  • Doxorubicin*
  • Egg Yolk
  • Hydrogen-Ion Concentration
  • Kinetics
  • Liposomes*
  • Models, Biological
  • Phosphatidylcholines*
  • Potassium

Substances

  • Liposomes
  • Phosphatidylcholines
  • Carbonyl Cyanide m-Chlorophenyl Hydrazone
  • Doxorubicin
  • Cholesterol
  • Potassium