New fast-release rate Liposomal Formulation for Doxorubicin - LC100

Barenholz Yechezkel, HUJI, School of Medicine - IMRIC, Biochemistry and Molecular Biology


Current preclinical and clinical data indicate that there is negligible release of drug from circulating liposomes.

Once liposomes extravagate to extracellular tissue fluids, little is known of the processes determining drug release.

It is believed that the following all likely contribute to drug release:

  • Gradual loss of the proton gradient retaining the drug
  • Enzymatic breakdown of liposomal phospholipids
  • Endocytosis by scavenger macrophages

Doxorubicin when entrapped in Doxil™, forms a salt with the divalent sulfate anion. The salt precipitates/gels due to its low solubility in the aqueous internal liposomal compartment.

Our Innovation

The invention provides a liposomal composition where an ionizable therapeutic agent is entrapped in the internal liposomal compartment (s) in the form of an ionic salt with monovalent alkyl sulfonate anions.


  • The entrapped therapeutic agent has a faster release rate from the liposomes compared to the release rate of the agent entrapped in the liposomes in the form of an ionic salt with divalent sulfate anions.
  • The faster rate of release of the therapeutic agent from the liposomes affords flexibility to adjust dosing schedules without compromising the biological efficacy of the therapeutic agents.


This technology provides a stable composition of liposome encapsulated doxorubicin, whereas doxorubicin is remotely loaded into the liposome with ammonium alkyl sulfate salt transmembrane gradient.  Doxorubicin alkyl sulfate salt does not form distinct crystals in the intraliposome aqueous phase. Doxorubicin shows faster in-vitro release form the liposome in comparison to Doxil™ and in vivo as demonstrated by the faster in-vivo pharmacokinetic elimination of doxorubicin.



  • The invention provides a remote loading procedure for loading therapeutic agents into pre-formed liposomes against an ammonium alkyl sulfonate gradient.
  • The invention also provides extended shelf life product stability including Doxorubicin chemical stability, encapsulation and leakage stability.


Contact for more information:

Shani Bullock
VP, Business Development, Healthcare
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