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Details for Patent: 7,521,068

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Details for Patent: 7,521,068

Title:Dry powder aerosols of nanoparticulate drugs
Abstract: There invention discloses aqueous dispersions of nanoparticulate aerosol formulations, dry powder nanoparticulate aerosol formulation, propellant-based aerosol formulations, methods of using the formulations in aerosol delivery devices, and methods of making such formulations. The nanoparticles of the aqueous dispersions or dry powder formulations comprise insoluble drug particles having a surface modifier on the surface thereof.
Inventor(s): Bosch; H. William (Bryn Mawr, PA), Ostrander; Kevin D. (Reading, PA), Cooper; Eugene R. (Berwyn, PA)
Assignee: Elan Pharma International Ltd. (Dublin, IE)
Filing Date:Nov 12, 1998
Application Number:09/190,138
Claims:1. A dry powder aerosol composition for pulmonary or nasal delivery comprising spherically shaped aggregates formed from spray-drying aqueous dispersions of nanoparticulate drug particles, wherein: (a) the aqueous dispersions of nanoparticulate drug particles: (i) comprise a poorly soluble crystalline drug, wherein by "poorly soluble" it is meant that the drug has a solubility in at least one liquid dispersion medium of less than about 10 mg/ml, (ii) have an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm, and (iii) have a surface modifier adsorbed on the surface thereof; and (b) the aggregates of such spray-dried drug particle dispersions are less than or equal to about 100 microns in diameter; and (c) such aggregates return to nanoparticulate drug particle dispersions upon reconstitution in an aqueous liquid medium.

2. The aerosol composition of claim 1 further comprising a diluent.

3. The aerosol composition of claim 2, wherein essentially every diluent particle comprises at least one embedded nanoparticulate drug particle having a surface modifier adhered to the surface of the drug particle.

4. The aerosol composition of claim 1, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

5. The aerosol composition of claim 4, wherein the drug is selected from the group consisting of beclomethasone dipropionate, naproxen, triamcinolone acetonide, budesonide, and an anti-emetic.

6. The aerosol composition of claim 1, wherein the nanoparticulate drug particles have an effective average particle size of less than about 400 nm.

7. The aerosol composition of claim 1, wherein the aerosol comprises a concentration of a drug in an amount of from about 0.05 mg/g up to about 900 mg/g.

8. The aerosol composition of claim 7, wherein the aerosol comprises a concentration of a drug selected from the group consisting of about 10 mg/g or more, about 100 mg/g or more, about 200 mg/g or more, about 400 mg/g or more, about 600 mg/g or more, and about 900 mg/g.

9. The aerosol composition of claim 1, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

10. The aerosol composition of claim 9, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

11. The aerosol composition of claim 10, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

12. The aerosol composition of claim 10, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

13. The aerosol composition of claim 1, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

14. The aerosol composition of claim 13, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

15. The aerosol composition of claim 13, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

16. The aerosol composition of claim 1, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

17. The aerosol composition of claim 16, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

18. The aerosol composition of claim 17, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

19. The aerosol composition of claim 17, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

20. A method of administering the aerosol of claim 1 to a patient, wherein the aerosol comprises drug at a concentration of 10 mg/g or greater, and wherein the patient delivery time for the aerosol administration is about 15 seconds or less.

21. The aerosol composition of claim 1, wherein the nanoparticulate drug particles have an effective average particle size of less than about 300 nm.

22. The aerosol composition of claim 1, wherein the nanoparticulate drug particles have an effective average particle size of less than about 250 nm.

23. The aerosol composition of claim 1, wherein the nanoparticulate drug particles have an effective average particle size of less than about 100 nm.

24. The aerosol composition of claim 1, wherein the nanoparticulate drug particles have an effective average particle size of less than about 50 nm.

25. The aerosol composition of claim 1, wherein at least 70% of the drug particles have a particle size of less than about 1000 nm.

26. The aerosol composition of claim 1, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

27. A dry powder aerosol composition for pulmonary or nasal delivery comprising spherically shaped aggregates formed from freeze-drying aqueous dispersions of nanoparticulate drug particles, wherein: (a) the aggregates of such freeze-dried drug particle dispersions are less than or equal to about 100 microns in diameter; (b) the aqueous dispersions of nanoparticulate drug particles: (i) comprise a poorly soluble crystalline drug, wherein by "poorly soluble" it is meant that the drug has a solubility in at least one liquid dispersion medium of less than about 10 mg/ml, (ii) have an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm, and (iii) have a surface modifier adsorbed on the surface thereof; and (c) such aggregates return to nanoparticulatre drug particle dispersions upon reconstitution in an aqueous liquid medium.

28. The aerosol composition of claim 27, further comprising a diluent.

29. The aerosol composition of claim 27, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

30. The aerosol composition of claim 29, wherein the drug is selected from the group consisting of beclomethasone dipropionate, naproxen, triamcinolone acetonide, budesonide, and an anti-emetic.

31. The aerosol composition of claim 27, wherein the nanoparticulate drug particles have an effective average particle size of less than about 400 nm.

32. The aerosol composition of claim 27, wherein the aerosol comprises a concentration of a drug in an amount of from about 0.05 mg/g up to about 900 mg/g.

33. The aerosol composition of claim 32, wherein the aerosol comprises a concentration of a drug selected from the group consisting of about 10 mg/g or more, about 100 mg/g or more, about 200 mg/g or more, about 400 mg/g or more, about 600 mg/g or more, and about 900 mg/g.

34. The aerosol composition of claim 27, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

35. The aerosol composition of claim 34, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

36. The aerosol composition of claim 35, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

37. The aerosol composition of claim 35, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

38. The aerosol composition of claim 27, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

39. The aerosol composition of claim 38, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

40. The aerosol composition of claim 38, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

41. The aerosol composition of claim 27, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

42. The aerosol composition of claim 41, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

43. The aerosol composition of claim 42, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

44. The aerosol composition of claim 42, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

45. The aerosol composition of claim 27, further comprising spray-dried nanoparticulate drug powder, wherein the drug of the freeze-dried nanoparticulate drug powder is either the same or different from the drug of the spray-dried nanoparticulate drug powder.

46. A method of administering the aerosol of claim 27 to a patient, wherein the aerosol comprises drug at a concentration of 10 mg/g or greater, and wherein the patient delivery time for the aerosol administration is about 15 seconds or less.

47. The aerosol composition of claim 27, wherein the nanoparticulate drug particles have an effective average particle size of less than about 300 nm.

48. The aerosol composition of claim 27, wherein the nanoparticulate drug particles have an effective average particle size of less than about 250 nm.

49. The aerosol composition of claim 27, wherein the nanoparticulate drug particles have an effective average particle size of less than about 100 nm.

50. The aerosol composition of claim 27, wherein the nanoparticulate drug particles have an effective average particle size of less than about 50 nm.

51. The aerosol composition of claim 27, wherein at least 70% of the drug particles have a particle size of less than about 1000 nm.

52. The aerosol composition of claim 27, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

53. A dry powder nanoparticulate aerosol composition for use in a propellant-based pMDI comprising (a) spherically shaped aggregates of nanoparticulate poorly soluble crystalline drug particles, wherein by "poorly soluble" it is meant that the drug has a solubility in at least one liquid dispersion medium of less than about 10 mg/ml, wherein the aggregates are less than or equal to about 100 microns in diameter, wherein such aggregates return to nanoparticulate drug particles upon reconstitution in an aqueous liquid medium, and wherein the drug particles: (i) have a surface modifier adsorbed on the surface thereof, and (ii) have an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm, and (b) a non-aqueous propellant.

54. The aerosol composition of claim 53, wherein at least 70% of the drug particles have a particle size of less than about 1000 nm.

55. The aerosol composition of claim 53, wherein the propellant is a non-CFC propellant.

56. A method of administering the aerosol of claim 53 to a patient, wherein the aerosol comprises drug at a concentration of 10 mg/g or greater, and wherein the patient delivery time for the aerosol administration is about 15 seconds or less.

57. The aerosol composition of claim 53, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

58. The aerosol composition of claim 53, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

59. The aerosol composition of any one of claims 4, 29, 11, 14, 18, 36, 39, 43, or 58 wherein the drug is selected from the group consisting of a bronchodilator, a corticosteroid, and an anti-fungal.

60. The aerosol composition of claim 53, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

61. The aerosol composition of claim 53, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

62. The aerosol composition of claim 61, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

63. The aerosol composition of claim 53, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

64. The aerosol composition of claim 53, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

65. The aerosol composition of claim 64, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

66. A method of making a dry powder nanoparticulate drug composition comprising: (a) forming an aqueous nanoparticulate dispersion of a poorly soluble drug, wherein: (i) the dispersion comprises poorly soluble crystalline drug particles and a surface modifier adsorbed on the surface thereof, wherein by "poorly soluble" it is meant that the drug has a solubility in the liquid dispersion medium of less than about 10 mg/ml, and (ii) the drug particles have an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm; and (b) spray-drying the nanoparticulate dispersion to form a dry powder of spherically shaped aggregates of the nanoparticulate drug and surface modifier particles, wherein the aggregates have a diameter of less than or equal to about 100 microns, and wherein such aggregates return to a nanoparticulate drug dispersion upon reconstitution in an aqueous liquid medium.

67. The method of claim 66, further comprising adding a diluent to the nanoparticulate dispersion prior to spray-drying, wherein following spray-drying essentially every diluent particle contains at least one embedded drug particle and a surface modifier.

68. The method of claim 66, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

69. The method of claim 66, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

70. The method of claim 66, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

71. The method of claim 70, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

72. The method of claim 66, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

73. The method of claim 66, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

74. The method of claim 73, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

75. A method of making a dry powder nanoparticulate drug aerosol formulation comprising: (a) milling under non-pressurized conditions in a non-aqueous medium having a high boiling point a dispersion comprising the following: (i) a poorly soluble crystalline drug, wherein by "poorly soluble" it is meant that the drug has a solubility in the non-aqueous medium of less than about 10 mg/ml, and (ii) a surface modifier, to obtain a nanoparticulate drug composition having an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm, and (b) evaporating the non-aqueous medium to obtain a dry powder of spherically shaped aggregates of drug and surface modifier particles, wherein the aggregates have a diameter of less than or equal to about 100 microns, and wherein such aggregates return to nanoparticulate drug particle dispersions upon reconstitution in an aqueous liquid medium.

76. The aerosol composition of claim 75, wherein at least 70% of the drug particles have a particle size of less than about 1000 nm.

77. The aerosol composition of claim 75, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

78. The method of claim 75, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

79. The method of claim 75, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

80. The method of claim 75, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

81. The method of claim 80, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

82. The method of claim 75, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

83. The method of claim 75, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

84. The method of claim 83, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

85. A method of making an aerosol composition comprising: (a) milling under pressurized conditions in a non-aqueous medium a dispersion comprising the following: (i) a poorly soluble crystalline drug, wherein by "poorly soluble" it is meant that the drug has a solubility in the non-aqueous dispersion medium of less than about 10 mg/ml, and (ii) a surface modifier, to obtain a drug having an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm; (b) evaporating the non-aqueous medium to obtain a dry powder of spherically shaped aggregates of drug and surface modifier particles, wherein the aggregates have a diameter of less than or equal to about 100 microns, and wherein such aggregates return to nanoparticulate drug particle dispersions upon reconstitution in an aqueous liquid medium; and (c) formulating the dry powder spherically shaped aggregates into an aerosol composition.

86. The aerosol composition of claim 85, wherein at least 70% of the drug particles have a particle size of less than-about 1000 nm.

87. The aerosol composition of claim 85, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

88. The method of claim 85, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

89. The method of claim 85, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

90. The method of claim 85, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

91. The method of claim 90, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

92. The method of claim 85, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

93. The method of claim 85, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

94. The method of claim 93, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.

95. A method of making a dry powder nanoparticulate drug composition comprising: (a) forming an aqueous nanoparticulate dispersion of a poorly soluble drug, wherein: (i) the dispersion comprises poorly soluble crystalline drug particles, wherein by "poorly soluble" it is meant that the drug has a solubility in the liquid dispersion medium of less than about 10 mg/ml, and wherein the drug particles have an effective average particle size of less than about 1000 nm, meaning at least 50% of the drug particles have a particle size of less than about 1000 nm, and (ii) a surface modifier adsorbed on the surface thereof; and (b) freeze-drying the nanoparticulate dispersion to form a dry powder of spherically shaped aggregates of the nanoparticulate drug and surface modifier particles, wherein the aggregates have a diameter of less than or equal to about 100 microns, and wherein such aggregates return to nanoparticulate drug particle dispersions upon reconstitution in an aqueous liquid medium.

96. The method of claim 95, further comprising adding a diluent to the nanoparticulate dispersion prior to freeze-drying, wherein following freeze-drying essentially every diluent particle contains at least one embedded drug particle and a surface modifier.

97. The aerosol composition of claim 95, wherein at least 70% of the drug particles have a particle size of less than about 1000 nm.

98. The aerosol composition of claim 95, wherein at least 90% of the drug particles have a particle size of less than about 1000 nm.

99. The method of claim 95, wherein the drug is selected from the group consisting of proteins, peptides, elastase inhibitors, analgesics, cystic-fibrosis therapies, asthma therapies, emphysema therapies, respiratory distress syndrome therapies, chronic bronchitis therapies, chronic obstructive pulmonary disease therapies, organ-transplant rejection therapies, therapies for tuberculosis and other infections of the lung, fungal infection therapies, and respiratory illness therapies associated with acquired immune deficiency syndrome, an oncology drug, an anti-emetic, and a cardiovascular agent.

100. The method of any one of claims 68, 78, 88, and 96, wherein the drug is selected from the group consisting of a bronchodilator, a corticosteroid, and an anti-fungal.

101. The method of claim 95, wherein the nanoparticulate drug particles have an effective average particle size selected from the group consisting of less than about 400 nm, less than about 300 nm, less than about 250 nm, less than about 100 nm, and less than about 50 nm.

102. The method of claim 95, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 10 microns.

103. The method of claim 102, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 2 to about 6 microns.

104. The method of claim 95, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of less than about 2 microns.

105. The method of claim 95, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 5 to about 100 .mu.m.

106. The method of claim 105, wherein the aggregates of the nanoparticulate drug particles have a mass median aerodynamic diameter of about 30 to about 60 .mu.m.
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