Druckluftinhalator zur pulmonalen Applikation liposomalen Pulver-Aerosols sowie dafuer geeignete Pulver-Aerosole

WO 200045878 A UPAB: 20001001 NOVELTY - A pressurized air inhaler for pulmonary administration of a liposomal powder aerosol comprises: (i) a container for aqueous liposome suspension, linked via a liquid dosing device with an atomizing nozzle and with a drying unit (e.g. nebulization chamber) for spray drying the liposomes; (ii) a mouthpiece outlet; and (iii) separate lines for supplying pressurized air and liposome dispersion to the atomizing nozzle. DETAILED DESCRIPTION - INDEPENDENT CLAIMS are included for the following: (a) a powder aerosol consisting of liposomes and/or nanoparticles, which is free of moisture and cryoprotective agents and comprises spherical, amorphous or crystalline particles of size 0.5-10 mu m or is prepared by pressurized air nebulization of liposomes and/or a nanoparticle dispersion via a 2-component nozzle at a nebulization pressure of 1-5 bars and a dispersion concentration of 0.2-1%; (b) liposomal powder aerosols comprising: (1) phospholipids, cholesterol, natural or artificial pulmonary surfactant or cationic amphiphiles and active agent; (2) large multilamellar vesicles (MLV) or small unilamellar vesicles (SUV) as liposomes; (3) hydrogenated soya phosphatidyl choline and cholesterol in molar ratio 1 : 0.25, plus SUV's prepared by ultrasonication or MLV's prepared by homogenization; (4) hydrogenated soya phosphatidyl choline, cholesterol and polyethylene glycol in molar ratio 1 : 1 : 0.1, plus SUV's prepared by ultrasonication or MLV's prepared by shaking a lipid film; (5) phosphatidyl choline and cholesterol in molar ratio 1 : 0.5 charged with 5,6-carboxyfluorescein, plus SUV's prepared by ultrasonication; or (6) DAC-Chol and DOPE in weight ratio 2 : 3 (optionally complexed with protamine sulfate or poly-L-lysine); and (c) nanoparticulate powder aerosols, consisting exclusively of active agent crystals of polymer particles charged with active agent. USE - For treating pulmonary disease (claimed), e.g. asthma, bronchitis or lung cancer. Liposomes containing active agents for treating respiratory tract diseases can be delivered to the trachea and large bronchia, to the small bronchia or to the bronchioles and alveoli by using powder aerosol of particle size 5-10 micro m, 3-5 micro m or 0.3-3 micro m respectively. The various liposome and aerosol formulations are suitable for use in the inhaler. ADVANTAGE - Pulmonary administration of liposomes is possible without compulsory 'breathing maneuvers'. The active agent reaches the required site of action in adequate amounts, without loss. The inhaler uses aqueous liposome dispersions, which are easily prepared (even on a large scale) and have low toxicity and high stability compared with dispersions in organic media. No carrier gas is used, and the aerosol particles have a controllable size. No multiple nebulization occurs and all the sprayed material is dried to powder in situ and inhaled. The formulation is not placed under elevated stress