Formulation of inhalable lipid-based salbutamol sulfate microparticles by spray drying technique |
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Authors: | Zahra Daman Kambiz Gilani Abdolhossein Rouholamini Najafabadi Hamid Reza Eftekhari Mohammad Ali Barghi |
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Institution: | 1.Aerosol Research Laboratory, Department of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;2.Medicinal Plants Research Center, Tehran University of Medical Sciences, Tehran, Iran;3.XRD Research Laboratory, School of Sciences, Tehran University, Tehran, Iran |
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Abstract: | BackgroundThe aim of this work was to develop dry powder inhaler (DPI) formulations of salbutamol sulfate (SS) by the aid of solid lipid microparticles (SLmPs), composed of biocompatible phospholipids or cholesterol.MethodsThe SLmPs were prepared by using two different solvent systems (ethanol and water-ethanol) and lipid carriers (dipalmitoylphosphatidylcholine (DPPC) and cholesterol) with/without L-leucine in the spray drying process. The spray-dried microparticles were physically-mixed with coarse lactose monohydrate in order to make our final DPI formulations and were investigated in terms of physical characteristics as well as in vitro drug release profile and aerosolization behavior.ResultsWe observed significant differences in the sizes, morphologies, and in vitro pulmonary depositions between the formulations. In particular, the SS-containing SLmPs prepared with water-ethanol (30:70 v/v) solution of DPPC and L-leucine which had then been blended with coarse lactose (1:9 w/w) exhibited the highest emitted dose (87.9%) and fine particle fraction (42.7%) among the formulations. In vitro drug release study indicated that despite of having a significant initial burst release for both cholesterol and DPPC-based microparticles, the remained drug released more slowly than the pure drug.ConclusionThis study demonstrated the potential of using lipid carriers as well as L-leucine in DPI formulations of SS to improve its aerosolization behavior and retard the release profile of the drug. |
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Keywords: | Dry powder inhalation Spray drying Salbutamol sulfate Solid lipid microparticles Particle engineering L-leucine |
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