Carbomer-modified spray-dried respirable powders for pulmonary delivery of salbutamol sulphate.
The present study investigates the feasibility of using two types of carbomer (971 and 974) to prepare inhalable dry powders that exhibit modified drug release properties. Powders were prepared by spray-drying formulations containing salbutamol sulphate, 20-50% w/w carbomer as a drug release modifier and leucine as an aerosolization enhancer. Following physical characterization of the powders, the aerosolization and dissolution properties of the powders were investigated using a Multi-Stage Liquid Impinger and a modified USP II dissolution apparatus, respectively. All carbomer 974-modified powders and the 20% carbomer 971 powder demonstrated high dispersibility, with emitted doses of at least 80% and fine particle fractions of approximately 40%. The release data indicated that all carbomer-modified powders displayed a sustained release profile, with carbomer 971-modified powders obeying first order kinetics, whereas carbomer 974-modified powders obeyed the Higuchi root time kinetic model; increasing the amount of carbomer 971 in the formulation did not extend the duration of drug release, whereas this was observed for the carbomer 974-modified powders. These powders would be anticipated to deposit predominately in the lower regions of the lung following inhalation and then undergo delayed rather than instantaneous drug release, offering the potential to reduce dosing frequency and improve patient compliance.
Aston Pharmacy School, Aston University, Birmingham, UK.
Farhan A
FA
Alhusban
Peter C
PC
Seville
D000180:Acrylic Resins / Q000737:chemistry*; D000280:Administration, Inhalation; D000336:Aerosols / Q000032:analysis / Q000737:chemistry; D000420:Albuterol / Q000032:analysis / Q000737:chemistry; D001993:Bronchodilator Agents / Q000032:analysis / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems / Q000379:methods*; D007700:Kinetics; D007930:Leucine / Q000737:chemistry; D008168:Lung; D011208:Powders
D000180:Acrylic Resins; D000336:Aerosols; D001993:Bronchodilator Agents; D011208:Powders; C479038:carbomer; D007930:Leucine; D000420:Albuterol