Medical use of spla2 hydrolysable liposomes

Abstract

The present invention relates to medical use of liposomes, more particular the first medical use of sPLA2 hydrolysable liposomes. Such liposomes may be used for targeted delivery of therapeutic agents to cancerous tissue and in such embodiments; the therapeutic agents are typically small molecule antitumor agents. Other aspects of the inventions relates to methods of reducing the side effects of therapeutic agents, e.g. reducing nephrotoxicity, neurotoxicity and gastrointestinal toxicity of a therapeutic agent. Yet another aspect of the present invention relate to methods of prolonging the therapeutic effect of a therapeutic agent.

1 . A sPLA2 hydrolysable liposome for use as a medicament of humans. 
     
     
         2 . The liposome of  claim 1 , wherein the content of anionic lipid is between 20% and 45%, the content of polymer conjugated lipid is between 3% and 6% and the content of neutral lipids is between 40% and 75%. 
     
     
         3 . The liposome of  claim 2 , wherein the anionic lipid is DSPG, the neutral lipid is DSPC and the polymer conjugated lipid is DSPE-PEG. 
     
     
         4 . The liposome of  claim 1 , wherein the liposome is administered intravenous administration in form of bolus injection or infusion. 
     
     
         5 . The liposome of  claim 1 , wherein the liposome comprises a therapeutic agent. 
     
     
         6 . The liposome of  claim 1 , wherein the therapeutic agent is a small molecule antitumour agent is selected from the group consisting of: anthracyclin derivatives, cisplatin, oxaliplatin, carboplatin, picoplatin, doxorubicin, paclitaxel, 5-fluoruracil, exisulind, cis-retinoic acid, suldinac sulphide, methotrexate, bleomycin and vincristine. 
     
     
         7 . The liposome of  claim 1 , wherein the small molecule antitumor agent is a platinum based antitumor agent selected from the group consisting of cisplatin, oxaliplatin, picoplatin and carboplatin. 
     
     
         8 . The liposome of  claim 1 , wherein the dose of the therapeutic agent is reduced as compared to the standard dose of the free therapeutic agent. 
     
     
         9 . The liposome of  claim 1 , wherein the dose of the therapeutic agent is increased as compared to the standard dose of the free therapeutic agent. 
     
     
         10 . The liposome of  claim 1 , wherein liposome is administered at prolonged intervals as compared to the standard dose regiment of the free compound.