Particles for inhalation having sustained release properties
View Patent ↗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. 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 in dry powder form comprising a bioactive agent in association with a charged lipid wherein the charged lipid is present in an amount from 10 to about 99% by weight and has an overall negative net charge and wherein release of the agent is sustained, wherein the lipid is a 1,2-diacyl-sn-glycero-3-[phospho-rac-(1-glycerol)] or a 1,2-diacyl-sn-glycerol-3-phosphate.
2. The method of claim 1 , wherein the 1,2-diacyl-sn-glycero-3-[phospho-rac-(1-glycerol)] lipid is represented by Formula I:
wherein,
R 1 and R 2 are independently an aliphatic group having from about 3 to about 24 carbons.
3. The method of claim 1 , wherein the 1,2-diacyl-sn-glycero-3-[phospho-rac-(1-glycerol)] lipid is 1,2-distearoyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DSPG), 1,2-dimyristoyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DMPG), 1,2-dipalmitoyl-sn-glycero-3-phospho-rac-(1-glycerol)] (DPPG), 1,2-dilauroyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DLPG), 1,2-dioleoyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DOPG) or any combination thereof.
4. The method of claim 1 , wherein the 1,2-diacyl-sn-glycerol-3-phosphate is represented by the Formula II:
wherein,
R 1 and R 2 are independently an aliphatic group having from about 3 to about 24 carbons.
5. The method of claim 1 , wherein the 1,2-diacyl-sn-glycerol-3-phosphate lipid is 1,2-dimyristoyl-sn-glycero-3-phosphate (DMPA), 1,2-dipalmitoyl-sn-glycero-3-phosphate (DPPA), 1,2-dilauroyl-sn-glycero-3-phosphate (DLPA), 1,2-dioleoyl-sn-glycero-3-phosphate (DOPA), 1,2-distearoyl-sn-glycero-3-phosphate (DSPA) or any combination thereof.