Tumor targeting using liposomal antineoplastic drugs

For highly lipophilic drugs, such as many antineoplastic agents, specific formulation strategies are needed to allow for oral or parenteral administration

Joerg Huwyler

2010

Scholarcy highlights

  • For highly lipophilic drugs, such as many antineoplastic agents, specific formulation strategies are needed to allow for oral or parenteral administration
  • They include the use of synthetic phospholipids, which are conjugated to gangliosides or polyethylene glycol
  • Grafting of the liposome with the inert and biocompatible polymer PEG leads to the formation of a protective, hydrophilic layer on the surface of the liposomes
  • Pegylation of liposomes results in an up to 50-fold decrease in the volume of distribution to values similar to the plasma volume, a 200-fold decrease in systemic plasma clearance from 22 to 0.1 l/hour and a nearly 100-fold increase in area under the time-concentration curve
  • Pegylated liposomes conjugated to the OX26 monoclonal antibodies were used previously to target the brain vascular endothelium in vivo and to transport incorporated drugs across the blood-brain barrier by receptor-mediated transcytosis
  • In view of the rapid and promising advances in the field of specific liposomal tumor targeting during the last years, a clinical use of vector-conjugated liposomes or immunoliposomes should be envisaged
  • Once optimized production processes are available, a new generation of vector-conjugated liposomal carriers will allow for an active targeting of metastatic or chemoresistant tumors, for which at present no efficient therapeutic options are available

Need more features? Save interactive summary cards to your Scholarcy Library.