Liposome drugs' loading efficiency: A working model based on loading conditions and drug's physicochemical properties

Daniel Zucker, David Marcus, Yechezkel Barenholz*, Amiram Goldblum

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

283 Scopus citations


Remote loading of liposomes by transmembrane gradients is one of the best approaches for achieving the high enough drug level per liposome required for the liposomal drug to be therapeutically efficacious. This breakthrough, which enabled the approval and clinical use of nanoliposomal drugs such as DoxilTM, has not been paralleled by an in-depth understanding that allows predicting loading efficiency of drugs. Here we describe how applying data-mining algorithms on a data bank based on Barenholz's laboratory's 15 years of liposome research experience on remote loading of 9 different drugs enabled us to build a model that relates drug physicochemical properties and loading conditions to loading efficiency. This model enables choosing candidate molecules for remote loading and optimizing loading conditions according to logical considerations. The model should also help in designing pro-drugs suitable for remote loading. Our approach is expected to improve and accelerate development of liposomal formulations for clinical applications.

Original languageAmerican English
Pages (from-to)73-80
Number of pages8
JournalJournal of Controlled Release
Issue number1
StatePublished - 1 Oct 2009

Bibliographical note

Funding Information:
This study was supported by the Barenholz Fund and Camber Fund at The Center of Nanotechnology of The Hebrew University. We would like to thank Y. Avnir, S. Clerc, R. Cohen, O. Garbuzenko, A. Sigal, K. Turjeman, and V. Wasserman for sharing their knowledge and results. Mr. S. Geller is acknowledged for help in editing the manuscript.


  • Liposomes
  • Loading conditions
  • Loading efficiency
  • Physicochemical properties
  • Remote loading


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