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Obtention and characterization of a ciclesonide: methyl-beta cyclodextrin complex

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Journal of Inclusion Phenomena and Macrocyclic Chemistry Aims and scope Submit manuscript

Abstract

Corticosteroids like ciclesonide are used to manage asthma. However, its physicochemical properties—namely water solubility—and, consequently, pharmacokinetics and pharmacodynamics could be object of improvement. One way to achieve this is by the use of cyclodextrins, a well-known group of molecules able to include water-insoluble molecules, solubilising them. The aim of this work is to verify if is possible to obtain a dry powder for inhalation containing ciclesonide included within Crysmeb (a commercially available type of methylated beta-cyclodextrin) applying the simple and inexpensive technique of kneading. Four different dry powders were obtained, varying the water content and molar ratios of drug:cyclodextrin (50 and 90 % water content and 1:1 and 1:2 M drug:cyclodextrin). The complexes were then analysed using different instrumental methods, namely, ultraviolet spectroscopy, differential scanning calorimetry and infrared spectroscopy. The physical characteristics of the powders formulated for inhalation were assessed by the particles time-of-flight (particle size analysis), and the Twin Stage Liquid Impinger (aerodynamic assessment of fine particles). The powder that best performed, overall, was the one obtained with 50 % water content and 1:1 M drug:cyclodextrin. It was concluded that the kneading method is feasible for obtention of a ciclesonide–Crysmeb inclusion complex.

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Acknowledgments

This work was partially supported by Fundação para a Ciência e Tecnologia (FCT): PTDC/SAU-FCF/098733/2008.

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  1. Faculdade de Farmácia, Instituto de Investigação do Medicamento (iMed.ULisboa), Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003, Lisbon, Portugal

    Nuno Arriagas & Helena Cabral-Marques

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  1. Nuno Arriagas
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  2. Helena Cabral-Marques
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Correspondence to Helena Cabral-Marques.

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Arriagas, N., Cabral-Marques, H. Obtention and characterization of a ciclesonide: methyl-beta cyclodextrin complex. J Incl Phenom Macrocycl Chem 80, 125–132 (2014). https://doi.org/10.1007/s10847-014-0416-4

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  • DOI: https://doi.org/10.1007/s10847-014-0416-4

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