Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability

Chitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, u...

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Main Authors: Georgia Michailidou, Nina Maria Ainali, Eleftheria Xanthopoulou, Stavroula Nanaki, Margaritis Kostoglou, Emmanuel N. Koukaras, Dimitrios N. Bikiaris
Format: Article
Language:English
Published: MDPI AG 2020-05-01
Series:Polymers
Subjects:
Online Access:https://www.mdpi.com/2073-4360/12/5/1101
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author Georgia Michailidou
Nina Maria Ainali
Eleftheria Xanthopoulou
Stavroula Nanaki
Margaritis Kostoglou
Emmanuel N. Koukaras
Dimitrios N. Bikiaris
author_facet Georgia Michailidou
Nina Maria Ainali
Eleftheria Xanthopoulou
Stavroula Nanaki
Margaritis Kostoglou
Emmanuel N. Koukaras
Dimitrios N. Bikiaris
author_sort Georgia Michailidou
collection DOAJ
description Chitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, using also poly(vinyl alcohol) (PVA) as a surfactant. Scanning electron microscopy (SEM) micrographs revealed that spherical nanoparticles were successfully prepared with average sizes range between 363 and 543 nm, as were measured by dynamic light scattering (DLS), while zeta potential verified their positive charged surface. X-ray diffraction (XRD) patterns revealed that BUD was encapsulated in crystalline state in nanoparticles but with a lower degree of crystallinity than the neat drug, which was also proven by differential scanning calorimetry (DSC) and melting peak measurements. This could be attributed to interactions that take place between BUD and CS, which were revealed by FTIR and by an extended computational study. An in vitro release study of budesonide showed a slight enhancement in the BUD dissolution profile, compared to the neat drug. However, drug release was substantially increased by introducing PVA during the nanoencapsulation procedure, which is attributed to the higher amorphization of BUD on these nanoparticles. The release curves were analyzed using a diffusion model that allows estimation of BUD diffusivity in the nanoparticles.
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spelling doaj.art-d31b8ed773964b518f066598afe2c9762023-11-20T00:10:33ZengMDPI AGPolymers2073-43602020-05-01125110110.3390/polym12051101Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved BioavailabilityGeorgia Michailidou0Nina Maria Ainali1Eleftheria Xanthopoulou2Stavroula Nanaki3Margaritis Kostoglou4Emmanuel N. Koukaras5Dimitrios N. Bikiaris6Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Inorganic Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Quantum and Computational Chemistry, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceLaboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, GreeceChitosan (CS) is a polymer extensively used in drug delivery formulations mainly due to its biocompatibility and low toxicity. In the present study, chitosan was used for nanoencapsulation of a budesonide (BUD) drug via the well-established ionic gelation technique and a slight modification of it, using also poly(vinyl alcohol) (PVA) as a surfactant. Scanning electron microscopy (SEM) micrographs revealed that spherical nanoparticles were successfully prepared with average sizes range between 363 and 543 nm, as were measured by dynamic light scattering (DLS), while zeta potential verified their positive charged surface. X-ray diffraction (XRD) patterns revealed that BUD was encapsulated in crystalline state in nanoparticles but with a lower degree of crystallinity than the neat drug, which was also proven by differential scanning calorimetry (DSC) and melting peak measurements. This could be attributed to interactions that take place between BUD and CS, which were revealed by FTIR and by an extended computational study. An in vitro release study of budesonide showed a slight enhancement in the BUD dissolution profile, compared to the neat drug. However, drug release was substantially increased by introducing PVA during the nanoencapsulation procedure, which is attributed to the higher amorphization of BUD on these nanoparticles. The release curves were analyzed using a diffusion model that allows estimation of BUD diffusivity in the nanoparticles.https://www.mdpi.com/2073-4360/12/5/1101chitosan nanoparticlessustain releasebudesonidedrug releasedrug dissolution enhancementCOPD treatment
spellingShingle Georgia Michailidou
Nina Maria Ainali
Eleftheria Xanthopoulou
Stavroula Nanaki
Margaritis Kostoglou
Emmanuel N. Koukaras
Dimitrios N. Bikiaris
Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
Polymers
chitosan nanoparticles
sustain release
budesonide
drug release
drug dissolution enhancement
COPD treatment
title Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
title_full Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
title_fullStr Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
title_full_unstemmed Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
title_short Effect of Poly(vinyl alcohol) on Nanoencapsulation of Budesonide in Chitosan Nanoparticles via Ionic Gelation and Its Improved Bioavailability
title_sort effect of poly vinyl alcohol on nanoencapsulation of budesonide in chitosan nanoparticles via ionic gelation and its improved bioavailability
topic chitosan nanoparticles
sustain release
budesonide
drug release
drug dissolution enhancement
COPD treatment
url https://www.mdpi.com/2073-4360/12/5/1101
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