Development of innovative controlled released dry powders for inhalation based on budesonide for a once daily administration
Le Van Bui1, Elena Menchi1, Ismaël Hennia1, Karim Amighi1 & Nathalie Wauthoz1
1 Unit of Pharmaceutics and Biopharmaceutics, Department of Pharmacotherapy and Pharmaceutics, Faculty of Pharmacy, Université libre de Bruxelles (ULB), Boulevard du Triomphe CP207, B-1050 Brussels, Belgium. *equal contribution, Le.Bui@ulb.be
Summary
Introduction. Dry powder inhalers (DPIs) in the treatment of non-communicable chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) are one of the most widely used devices used by the patients. However, the appropriate use or choice of inhalable medications can be challenging for patients and healthcare professionals. Poor adherence due to high frequency of administration, errors in inhalation technique and/or use of DPIs may cause the loss of asthma or COPD control. In the present study, we aim to develop a dry powder for inhalation (DPI) formulation based on controlled release of budesonide (BUD) using a lipid matrix based on hydrogenated castor oil (HCO) and tocopherol polyethylene glycol 1000 succinate (TPGS) to decrease the administration frequency. Methods. BUD formulations were produced using the spray-drying particle engineering technique. The aerodynamic properties were assessed using the Next Generation Impactor (NGI) according to the European Pharmacopeia. The release properties of BUD were assessed using a paddle apparatus with a Fast Screening Impactor cassette for dissolution. Results. The formulations showed optimal aerodynamic properties with a fine particle fraction related to the nominal dose (FPFn) comprised between 52.5% to 53.5% as well as drug releases that decreased depending on the content of HCO (20 (% w:v) or 95 (% w:v)) and TPGS (5% (w:w) of the excipients). Conclusion. Our results suggest that the content of the lipid matrix in HCO and TPGS is responsible of the extended drug release in PBS – 0.02% Tween20 (w:v) and fine particle ratio (FPF).