Abstract
The delivery of a dexamethasone formulation directly into the lung appears as an appropriate strategy to strengthen the systemic administration, reducing the dosage in the treatment of lung severe inflammations. For this purpose, a hyaluronic acid-dexamethasone formulation was developed, affording an inhalable reconstituted nanosuspension suitable to be aerosolized. The physico-chemical and biopharmaceutical properties of the formulation were tested: size, stability, loading of the spray-dried dry powder, reconstitution capability upon redispersion in aqueous media. Detailed structural insights on nanoparticles after reconstitution were obtained by light and X-ray scattering techniques. (1) The size of the nanoparticles, around 200 nm, is in the proper range for a possible engulfment by macrophages. (2) Their structure is of the core-shell type, hosting dexamethasone nanocrystals inside and carrying hyaluronic acid chains on the surface. This specific structure allows for nanosuspension stability and provides nanoparticles with muco-inert properties. (3) The nanosuspension can be efficiently aerosolized, allowing for a high drug fraction potentially reaching the deep lung. Thus, this formulation represents a promising tool for the lung administration via nebulization directly in the pipe of ventilators, to be used as such or as adjunct therapy for severe lung inflammation.
Highlights
Academic Editor: Department of Medical Biotechnology and Translational Medicine, Università degli Studi di Milano, LITA, Instituto de Investigaciones en Fisicoquímica de Córdoba (INFIQC), Consejo Nacional de Investigaciones
The ethanol/water suspension (45:55 v/v fraction) of mixed hyaluronic acid (HYA):DEX at 0.06:99.94 mole fraction (55:45 mass fraction) and 5 mg/mL total concentration was observed by small and wide angle X-ray scattering (SAXS and Wide Angle X-ray Scattering (WAXS)) experiments to assess the degree of dispersion of DEX just before spray drying
Results on HYA conformation in solution allowed for the quantification of the free and complexed HYA fractions in nanoparticles solutions after reconstitution of dry microparticles
Summary
The delivery of a dexamethasone formulation directly into the lung appears as an appropriate strategy to strengthen the systemic administration, reducing the dosage in the treatment of lung severe inflammations For this purpose, a hyaluronic acid-dexamethasone formulation was developed, affording an inhalable reconstituted nanosuspension suitable to be aerosolized. (2) Their structure is of the core-shell type, hosting dexamethasone nanocrystals inside and carrying hyaluronic acid chains on the surface This specific structure allows for nanosuspension stability and provides nanoparticles with muco-inert properties. (3) The nanosuspension can be efficiently aerosolized, allowing for a high drug fraction potentially reaching the deep lung This formulation represents a promising tool for the lung administration via nebulization directly in the pipe of ventilators, to be used as such or as adjunct therapy for severe lung inflammation. Introduction with regard to jurisdictional claims in Dexamethasone (DEX) is a synthetic glucocorticoid used in a wide range of diseases [1,2,3,4], when related with lung, from occlusive airway conditions such as asthma [5]
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