Modified release of beclometasone dipropionate from chitosan-based spray-dried respirable powders

Dry powders for inhalation were prepared by spray drying a 30% v/v aqueous ethanol formulation containing beclometasone dipropionate (BDP), lactose, leucine and chitosan (low, medium or high molecular weight (MW), or combinations thereof). Following physical characterisation of the powders, the aerosolisation and dissolution properties of the powders were investigated using Multi-Stage Liquid Impinger and USP II dissolution apparatus, respectively. The powders were highly dispersible, with emitted doses in excess of 90% of loaded powder aerosolised from a Spinhaler dry powder inhaler. The fine particle fraction (FPF) was observed to decrease, whereas the time for 100% drug release increased, with increasing chitosan MW. For example, the low MW formulation exhibited an FPF of 64% and a 100% dissolution time of 2 h, whereas the high MW formulation demonstrated an FPF of 54% and a dissolution time of 12 h. 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.

Highly dispersible dry powders for inhalation were prepared by spray-drying formulations containing beclometasone dipropionate, leucine as a dispersibility enhancer and chitosan as a drug release modifier. A range of molecular weights (MW) of chitosan were employed; the use of low MW chitosan resulted in a fine particle fraction (FPF) of 64% and a dissolution time of 2 h, whereas inclusion of high MW chitosan reduced the FPF to 54% and prolonged the dissolution time to 12 h. 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.Figure optionsDownload as PowerPoint slide