Use of simple amino acids to form porous particles

Abstract

Particles having a tap density of less than 0.4 g/cm 3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

1 . A method of preparing particles having a tap density less than 0.4 g/cm 3  comprising:
 (a) forming a mixture including a therapeutic, prophylactic or diagnostic agent, or any combination thereof, and an amino acid or a salt thereof; and   (b) spray-drying said mixture to produce particles having a tap density less than about 0.4 g/cm 3 .   
     
     
         2 . The method of  claim 1 , wherein the particles have a median geometric diameter of between about 5 micrometers and about 30 micrometers. 
     
     
         3 . The method of  claim 1 , wherein the particles have an aerodynamic diameter of between about 1 and about 5 microns. 
     
     
         4 . The method of  claim 3 , wherein the particles have an aerodynamic diameter of between about 1 and about 3 microns. 
     
     
         5 . The method of  claim 3 , wherein the particles have an aerodynamic diameter of between about 3 and 5 microns. 
     
     
         6 . The method of  claim 1 , wherein the amino acid is hydrophobic. 
     
     
         7 . The method of  claim 6 , wherein the hydrophobic amino acid is selected form the group consisting of leucine, isoleucine, alanine, valine, phenylalanine and any combination thereof. 
     
     
         8 . The method of  claim 3 , wherein the hydrophobic amino acid is present in the particles in an amount of at least 10% weight. 
     
     
         9 . The method of  claim 1 , wherein the therapeutic, prophylactic or diagnostic agent is present in the particles in an amount ranging from about 1 to about 90% weight. 
     
     
         10 . The method of  claim 1 , wherein the mixture comprises a surfactant. 
     
     
         11 . The method of  claim 1 , wherein the mixture comprises a phospholipid. 
     
     
         12 . The method of  claim 11 , wherein the phospholipid is endogenous to the lung. 
     
     
         13 . The method of  claim 11 , wherein the phospholipid is selected from the group consisting of phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phosphatidylserines, phosphatidylinositols and combinations thereof. 
     
     
         14 . The method of  claim 1 , wherein the mixture comprises an organic solvent. 
     
     
         15 . The method of  claim 1 , wherein the mixture comprises a co-solvent including an organic solvent and an aqueous solvent.