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Open AccessArticle

Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity

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Centre for Marine Sciences, Faculdade de Ciências e Tecnologia, Universidade do Algarve, 8005-139 Faro, Portugal
2
Centre for Biomedical Research, Universidade do Algarve, 8005-139 Faro, Portugal
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Algarve Chemistry Research Centre and Department of Chemistry and Pharmacy, Universidade do Algarve, 8005-139 Faro, Portugal
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Faculdade de Ciências e Tecnologia, Universidade do Algarve, 8005-139 Faro, Portugal
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Department of Chemical Engineering, University of Vigo, Faculty of Sciences, As Lagoas, 32004 Ourense, Spain
6
Food and Drug Department, University of Parma, 43124 Parma, Italy
*
Author to whom correspondence should be addressed.
Polymers 2020, 12(2), 425; https://doi.org/10.3390/polym12020425
Received: 30 January 2020 / Revised: 10 February 2020 / Accepted: 11 February 2020 / Published: 12 February 2020
(This article belongs to the Special Issue Biofunctional Polymer Carriers)
Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%–95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent.
Keywords: chondroitin sulphate; isoniazid; inhalable microparticles; rifabutin; solvents; spray-drying chondroitin sulphate; isoniazid; inhalable microparticles; rifabutin; solvents; spray-drying
MDPI and ACS Style

Rodrigues, S.; da Costa, A.M.R.; Flórez-Fernández, N.; Torres, M.D.; Faleiro, M.L.; Buttini, F.; Grenha, A. Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity. Polymers 2020, 12, 425.

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