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Supercritical Antisolvent Precipitation of Corticosteroids/β‐Cyclodextrin Inclusion Complexes
Version 1
: Received: 27 November 2023 / Approved: 27 November 2023 / Online: 27 November 2023 (16:10:37 CET)
A peer-reviewed article of this Preprint also exists.
Mottola, S.; De Marco, I. Supercritical Antisolvent Precipitation of Corticosteroids/β-Cyclodextrin Inclusion Complexes. Polymers 2024, 16, 29. Mottola, S.; De Marco, I. Supercritical Antisolvent Precipitation of Corticosteroids/β-Cyclodextrin Inclusion Complexes. Polymers 2024, 16, 29.
Abstract
In this paper, corticosteroid–β-cyclodextrin (β-CD) inclusion complexes have been prepared by Supercritical AntiSolvent (SAS) precipitation to enhance the dissolution rate of dexamethasone (DEX) and prednisolone (PRED), which are poorly water-soluble drugs. The processing of the active principles in the absence of a carrier led to the almost complete extraction of the active principle (the small amount of obtained material precipitates in the form of crystals). The coprecipitation of the ingredients in the presence of β-CD was investigated at different concentrations, pressures, and molar ratios. For both the corticosteroids, the optimized operating conditions were 40 °C, 120 bar, an equimolar ratio, and a concentration in DMSO of 20 mg/mL; these conditions led to the attainment of microparticles with a mean diameter equal to 0.197±0.180 μm and 0.131±0.070 μm in the case of DEX and PRED, respectively. The Job’s method confirmed the formation of inclusion complexes in correspondence with the 1/1 mol/mol ratio. Compared to the pure ingredients, the obtained powders have an improved release rate, which is about 3 times faster in both cases.
Keywords
Corticosteroid; inclusion complex; β-cyclodextrin; SAS micronization; controlled release; supercritical carbon dioxide; supercritical antisolvent
Subject
Engineering, Chemical Engineering
Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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