Study objective: To test the tolerance and safety of single doses of beclomethasone dipropionate (Bec)-dilauroylphosphatidylcholine (DLPC) liposome aerosol in volunteers.
Design: Single-dose inhalations of liposome preparations of Bec-DLPC and DLPC alone were administered for 15 min from a jet nebulizer (Puritan-Bennett, modified twin jet; mass median aerodynamic diameter of 1.6 µm) under close clinical and laboratory surveillance. Two dose levels (0.5 mg Bec/12.5 mg DLPC per milliliter, and 1.0 mg Bec and 25 mg DLPC per milliliter in the reservoirs, respectively) were administered. The Bec doses were selected to approximate the dosages of this glucocorticoid used with metered-dose inhalers (MDIs). First, four volunteers were exposed to an initial low dose; the mean (±SD) inhaled doses were 0.56±0.07 mg of Bec and/or 14.0±1.8 mg of DLPC. Subsequently, a second group of six volunteers was exposed to a higher dose; the mean (±SD) inhaled doses were 1.29±0.14 mg of Bec and/or 34.6±6.8 mg of DLPC.
Setting: Outpatient and inpatient.
Patients: Normal male (n=6) and female (n=4) adult volunteers.
Interventions: Inhalation of Bec-DLPC and DLPC liposome aerosols in a single-dose tolerance study involving 10 normal volunteers.
Measurements and results: Spirometry, clinical observations, clinical chemistry, and hematology were monitored. No adverse clinical or laboratory events were observed.
Conclusions: Bec-DLPC liposome aqueous aerosol was well tolerated in doses equivalent to those currently administered by MDIs and dry powder inhalers for treatment of asthma.