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Details for Patent: 8,080,263

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Details for Patent: 8,080,263

Title:Dispersion for pulmonary delivery of a bioactive agent
Abstract: Stabilized dispersions are provided for the delivery of a bioactive agent. The dispersions preferably comprise a plurality of perforated microstructures dispersed in a suspension medium that typically comprises a liquid fluorochemical. As density variations between the suspended particles and suspension medium are minimized and attractive forces between microstructures are attenuated, the disclosed dispersions are particularly resistant to degradation, such as by settling or flocculation. In particularly preferred embodiments the stabilized dispersions may be directly administered to the lung of a patient using an endotracheal tube or bronchoscope.
Inventor(s): Dellamary; Luis A. (San Marcos, CA), Tarara; Thomas E. (Burlingame, CA), Kabalnov; Alexey (Corvallis, OR), Weers; Jeffry G. (Belmont, CA), Schutt; Ernest G. (San Diego, CA)
Assignee: Novartis AG (Basel, CH)
Filing Date:May 27, 2008
Application Number:12/154,731
Claims:1. A stabilized dispersion for the pulmonary delivery of a bioactive agent comprising a nonaqueous liquid suspension medium having dispersed therein a plurality of porous perforated microstructures having a mean diameter of 1-30 .mu.m, said perforated microstructures comprising at least one bioactive agent wherein said suspension medium permeates said perforated microstructures, said dispersion characterized by a refractive index differential of less than 0.5, a density differential of less than 0.6 g/cm.sup.3, and a creaming time of greater than 1 minute.

2. A dispersion according to claim 1 wherein the permeable microstructures comprise at least one of a phospholipid, nonionic detergent, nonionic block copolymer, ionic surfactant, biocompatible fluorinated surfactant or combinations thereof.

3. A dispersion according to claim 1 wherein the permeable microstructures comprise a phospholipid.

4. A dispersion according to claim 3 wherein the phospholipid is present in the perforated microstructures in an amount greater than 20%.

5. A dispersion according to claim 3 wherein the permeable microstructures comprise an inorganic salt.

6. A dispersion according to claim 5 wherein the inorganic salt comprises calcium chloride.

7. A dispersion according to claim 5 wherein the gel to liquid transition temperature of the permeable microstructures is greater than 40.degree. C.

8. A dispersion according to claim 3, further comprising a fluorocarbon blowing agent.

9. A dispersion according to claim 8 wherein a ratio of blowing agent to phospholipid is at least 20.

10. A dispersion according to claim 1 wherein the permeable microstructures have a mean density selected to provide a density differential with that of the suspension medium of less than 0.6 g/cm.sup.3.

11. A dispersion according to claim 1 wherein the suspension medium comprises a fluorochemical.

12. A dispersion according to claim 1 wherein the bioactive agent comprises one or more of antiallergics, bronchodilators, pulmonary lung surfactants, analgesics, antibiotics, leukotriene inhibitors or antagonists, antihistamines, anti-inflammatories, antineoplastics, anticholinergics, anesthetics, anti-tuberculars, imaging agents, cardiovascular agents, enzymes, steroids, genetic material, viral vectors, antisense agents, proteins, peptides or combinations thereof.

13. A dispersion according to claim 1 wherein a mean porosity of the perforated microstructures is greater than 20% of the microstructure surface area.

14. A dispersion according to claim 1, wherein the bioactive agent is gentamicin.

15. A dispersion according to claim 1, wherein the bioactive agent is beclamethasone dipropionate.

16. A dispersion according to claim 1, wherein the bioactive agent is triamicinolone acetonide.

17. A dispersion according to claim 1, wherein the bioactive agent is DNAse I.

18. A dispersion according to claim 1, wherein the bioactive agent is albuterol sulfate.

19. A dispersion according to claim 1, wherein the bioactive agent is insulin.

20. A dispersion according to claim 1, wherein the creaming time is greater than 30 minutes.

21. A dispersion according to claim 1, wherein the dispersion comprises a homodispersion.

22. A dispersion according to claim 1, wherein the perforated microstructures are further characterized by a packing value of 0.3 or greater.
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