Speaker at Pharmaceutics and Drug Delivery Systems 2022 - Aysu Yurdasiper
Ege University, Turkey
Title : Development and characterization of salbutamol sulfate dry powder inhaler formulations for asthma management


Asthma is a chronic disease that causes inflammation of the airways and makes it difficult to breathe. The best way to manage asthma is to avoid triggers, take medication to prevent symptoms, and control asthma attacks. The inhalation route is frequently used to administer drugs for the management of respiratory diseases such as asthma. Pulmonary drug delivery systems are a fast-response system because they can deliver adequate and necessary doses of drugs to the lungs with minimal systemic side effects while avoiding the first-pass effects of the liver and targeting the drug directly to the lung. dry powder inhalers (DPI) contain drugs as inhalable powder. It has advantages such as increasing physicochemical stability, extended-release profile, and direct delivery of the drug to the site of action in the lungs. They do not require dissolution of the drug as in nebulizers, and unlike metered dose inhalers, DPIs have no propellants, so the dispersion of the powder is dependent on the patient's inhalation. Salbutamol sulfate (SS) is a β2-agonist used as a bronchodilator in chronic obstructive pulmonary diseases like asthma. By preparing DPI formulations, the short half-life of SS can be extended and the problems associated with systemic toxicity can be overcome. Also, pulmonary administration provides an alternative route of administration to avoid hepatic metabolism of SS and the local effect can be enhanced by direct targeting the lungs.

DPI formulations containing SS were prepared with chitosan, trehalose and leucine combination by using a spray dryer. Following the formulation of the drug, resultant powders were determined via scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), dynamic light scattering particle size analysis, and surface charge analysis. The in vitro aerosol dispersion performance and drug dissolution behavior was evaluated using a next-generation impactor (NGI) (using an Aerolizer at 100?L/min flow rate.) and the NGI dissolution cup, respectively. A high-performance liquid chromatography method was used for measuring the drug content. Morphologies of the spray-dried microparticles were exhibited by SEM and the particles have an irregular, corrugated surface. The optimized formulation mean volume diameter (Dv50) and zeta potentials were 3.91±0.18 μm and 11.28±0.47 respectively. The fine particle fractions from chitosan-based formulations (48.13±2.26) were significantly higher (p?<?0.001) than those of formulations without chitosan (41.07±1.35). The DPI formulation has satisfactory deposition in the airways. The mass median aerodynamic diameters (MMAD) were around 3 μm for all formulations. Chitosan-based DPI prolonged drug residence time in the lung (7 hours) and maintained a relatively high drug concentration (72.34%) for a longer time. These results supported that chitosan-loaded DPI containing SS for treatment of asthma exhibits prolonged drug retention at the targeted site. This optimized formulation might represent a plausible delivery vehicle for targeting the treatment of asthma via enhancing the therapeutic efficacy of SS and could be a promising candidate for the treatment of asthma.


Aysu Yurdasiper obtained her BSc and MSc degree in Faculty of Pharmacy from Ege University, Izmir, Turkey and respectively, followed by a Ph. D degree from Department of Pharmaceutical Technology, Ege University, studying on Nano gel delivery system invitro- in vivo studies on dermal drug delivery. Her work is focused on dry powder inhalers, dermal delivery (topical, transdermal drug systems), controlled release formulations (nanoparticles, microparticles) for drug delivery and Nanomedicine in pulmonary delivery. She is Editor in chief in the American Journal of Drug Delivery and Therapeutics and also Editor and on the Editorial Board of several International Journals. She has filed a National patent on dry powder inhaler formulation and she is a member of the Turkish Pharmaceutical Technology Scientists’ Association (TUFTAD), Turkish Pharmacists’ Association (TEB), Controlled Release Society (CRS) and American Association of Pharmaceutical Scientists (AAPS). She has been working as an Assistant Professor in the Department of Pharmaceutical Technology, Ege University. Her current research interest focus on development of novel Nano medicine including polymers and in vitro-in vivo evaluation for the treatment of respiratory diseases.