Freeze-dried product and gas-filled microvesicles suspension

Abstract

Lipid formulation particularly for preparing stable gas-filled microvesicles, comprising distearoyl-phosphatidylcholine (DSPC), dipalmitoylphosphatidylethanolamine-PEG5000 (DPPE-PEG5000) and palmitic acid in an advantageous relative molar ratio. The formulation is useful in particular for therapeutic application with ultrasounds.

1 . A freeze-dried formulation, for preparing gas-filled microvesicles, comprising a lipid mixture of DSPC, DPPE-PEG and palmitic acid in a respective molar amount of 65-85/4-10/8-22. 
     
     
         2 . The freeze-dried formulation of  claim 1  wherein said respective molar amount is of 70-80/5-9/12-21. 
     
     
         3 . The freeze-dried formulation of  claim 1  wherein said respective molar amount is of 72-76/6-8/15-20. 
     
     
         4 . The freeze-dried formulation of  claim 1  wherein said respective molar amount is of 74 (+/−1)/7.5 (+/−0.5)/18.5(+/−1). 
     
     
         5 . The freeze-dried formulation of any of the preceding  claims 1  to  4  further comprising a freeze-drying protective component. 
     
     
         6 . The freeze-dried formulation according to  claim 5 , wherein freeze-drying protective component is PEG4000. 
     
     
         7 . The freeze-dried formulation according to  claim 6 , wherein the weight of the lipid mixture is of from 0.08% to 0.3% with respect to the weight of PEG4000. 
     
     
         8 . The freeze-dried formulation according to  claim 7  wherein said weight is of from 0.10% to 0.20%. 
     
     
         9 . The freeze-dried formulation according to  claim 7  wherein said weight is of from 0.12% to 0.18% by weight 
     
     
         10 . The freeze-dried formulation according to  claim 7  wherein said weight is of about 0.16%. 
     
     
         11 . A suspension of gas-filled microvesicles wherein said microvesicles comprise a mixture of DSPC, DPPE-PEG and palmitic acid in a respective molar amount of 65-85/4-10/8-22. 
     
     
         12 . The suspension of  claim 11  wherein said respective molar amount is of 70-80/5-9/12-21. 
     
     
         13 . The suspension of  claim 11  wherein said respective molar amount is of 72-76/6-8/15-20. 
     
     
         14 . The suspension of  claim 11  wherein said respective molar amount is of 74 (+/−1)/7.5 (+/−0.5)/18.5(+/−1).