Co-spraying of carriers (mannitol-lactose) as a method to improve aerosolization performance of salbutamol sulfate dry p
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ORIGINAL ARTICLE
Co-spraying of carriers (mannitol-lactose) as a method to improve aerosolization performance of salbutamol sulfate dry powder inhaler Mickey Socrates Ferdynand 1 & Ali Nokhodchi 1,2
# The Author(s) 2020
Abstract Although in dry powder inhaler (DPI) formulations a single carrier is used, a single carrier is not able to provide an excellent aerosolization performance when it is used in DPI formulations. Thereby, the aim of this study was to engineer a suitable ternary mixture of mannitol-lactose-leucine to be used in a DPI formulation with enhanced aerosolization performance. To this end, binary mixtures of mannitol:lactose containing a constant amount of leucine (5% w/w of carriers) were spray-dried as a single solution. Spray-dried samples were blended with salbutamol sulfate to determine the efficiency of their aerosolization performance. Interestingly, note that lactose was in its amorphous state stabilized by the presence of mannitol in the samples. Spraydried mannitol without lactose showed a combination of the α- and β-polymorphic forms which was the case in all other ratios of mannitol:lactose. It was shown that the highest fine particle fraction (FPF) was 62.42 ± 4.21% which was obtained for the distinct binary mixtures (1:3 mannitol:lactose) compared to a single carrier. This study opens a new window to investigate further the implementation of binary mixtures of sugar carriers containing leucine in DPI formulations to overcome poor aerosolization performance the mentioned DPI formulations. Keywords Spray-dried carriers . Leucine . Inhalation performance . Dry powder inhaler . Salbutamol sulfate . Polymorphism . Ternary mixtures
Introduction β2-Adrenergic receptor agonists, such as salbutamol sulfate, act on the β2-adrenergic receptor to facilitate smooth muscle relaxation and dilation of bronchial passages [1]. This enables patients suffering from a disease like that of asthma, which is a chronic inflammatory disease characterized by the obstruction of airflow due to bronchial airway constriction in response to a stimulus [2], the ability to breathe. Such process, however, is achieved via the delivery of a successful therapeutic dosage of salbutamol sulfate to be deposited more peripherally (in the middle and small airway) [3, 4]. Therefore, aerosolization performance becomes a significant factor in the development and implementation of any given dry powder inhaler (DPI) * Ali Nokhodchi [email protected] 1
Pharmaceutics Research Laboratory, School of Life Sciences, University of Sussex, Brighton BN1 9QJ, UK
2
Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
formulation given that inter-particulate forces are directly influenced by particle density, morphology, surface roughness, particle-size distribution, presence of fine particle excipients, surface energy, carrier flow, and the type of carrier chosen [5, 6]. It has been shown that spray drying can be used to manipulate the properties of a carrier to achieve a better
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