Particles for inhalation having sustained release properties

Abstract

The invention generally relates to a method for pulmonary delivery of therapeutic, prophylactic and diagnostic agents to a patient wherein the agent is released in a sustained fashion, and to particles suitable for use in the method. In particular, the invention relates to a method for the pulmonary delivery of a therapeutic, prophylactic or diagnostic agent comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising a therapeutic, prophylactic or diagnostic agent or any combination thereof in association with a charged lipid, wherein the charged lipid has an overall net charge which is opposite to that of the agent upon association with the agent. Release of the agent from the administered particles occurs in a sustained fashion.

1 - 47 . (canceled) 
     
     
         48 . A method for delivery via the pulmonary system comprising:
 administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles consisting of:   insulin, sodium citrate and a phospholipid.   
     
     
         49 . The method of  claim 48 , wherein the phospholipid is a 1,2-diacyl-sn-glycero-3-phosphocholine. 
     
     
         50 . The method of  claim 49 , wherein the 1,2-diacyl-sn-glycero-3-phosphocholine is 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC). 
     
     
         51 . The method of  claim 48 , wherein the insulin is present in the amount from about 10% by weight to 50% by weight. 
     
     
         52 . The method of  claim 48 , wherein the phospholipid is present in the amount from about 40% by weight to 70% by weight. 
     
     
         53 . The method of  claim 48 , wherein sodium citrate is present in the amount of 10% by weight. 
     
     
         54 . The method of  claim 48 , wherein the particles have a tap density less than about 0.4 g/cm 3 . 
     
     
         55 . The method of  claim 54 , wherein the particles have a tap density less than about 0.1 g/cm 3 . 
     
     
         56 . The method of  claim 48 , wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers. 
     
     
         57 . The method of  claim 48 , wherein the particles have an aerodynamic diameter of from about 1 to about 5 microns. 
     
     
         58 . The method of  claim 57 , wherein the particles have an aerodynamic diameter of from about 1 to about 3 microns. 
     
     
         59 . The method of  claim 57 , wherein the particles have an aerodynamic diameter of from about 3 to about 5 microns. 
     
     
         60 . The method of  claim 48 , wherein delivery to the pulmonary system includes delivery to the deep lung. 
     
     
         61 . A method of administering insulin to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles consisting of:
 insulin, sodium citrate and a phospholipid.   
     
     
         62 . The method of  claim 61 , wherein the phospholipid is a 1,2-diacyl-sn-glycero-3-phosphocholine. 
     
     
         63 . The method of  claim 62 , wherein the 1,2-diacyl-sn-glycero-3-phosphocholine is 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC). 
     
     
         64 . The method of  claim 61 , wherein the insulin is present in the amount from about 10% by weight to 50% by weight. 
     
     
         65 . The method of  claim 61 , wherein the phospholipid is present in the amount from about 40% by weight to 70% by weight. 
     
     
         66 . The method of  claim 61 , wherein sodium citrate is present in the amount of 10% by weight. 
     
     
         67 . The method of  claim 61 , wherein the particles have a tap density less than about 0.4 g/cm 3 . 
     
     
         68 . The method of  claim 67 , wherein the particles have a tap density less than about 0.1 g/cm 3 . 
     
     
         69 . The method of  claim 61 , wherein the particles have a median geometric diameter of from about 5 micrometers to about 30 micrometers. 
     
     
         70 . The method of  claim 61 , wherein the particles have an aerodynamic diameter of from about 1 to about 5 microns. 
     
     
         71 . The method of  claim 70 , wherein the particles have an aerodynamic diameter of from about 1 to about 3 microns. 
     
     
         72 . The method of  claim 70 , wherein the particles have an aerodynamic diameter of from about 3 to about 5 microns.