Mechanistic study of dissolution enhancement by interactive mixtures of chitosan with meloxicam as model
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Authors
Brokesova, Jana
Slamova, Michaela
Zamostny, Petr
Koktan, Jakub
Kreicik, Lukas
Svacinova, Petra
Sklubalova, Zdenka
Vraníková, Barbora
Author (Corporation)
Publication date
01.02.2022
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Type
01A - Journal article
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Parent work
European Journal of Pharmaceutical Sciences
Special issue
DOI of the original publication
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Series
Series number
Volume
169
Issue / Number
Pages / Duration
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Publisher / Publishing institution
Elsevier
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Abstract
To enhance dissolution rate of meloxicam (MX), a poorly soluble model drug, a natural polysaccharide excipient chitosan (CH) is employed in this work as a carrier to prepare binary interactive mixtures by either mixing or co-milling techniques. The MX-CH mixtures of three different drug loads were characterized for morphological, granulometric, and thermal properties as well as drug crystallinity. The relative dissolution rate of MX was determined in phosphate buffer of pH 6.8 using the USP-4 apparatus; a significant increase in MX dissolution rate was observed for both mixed and co-milled mixtures comparing to the raw drug. Higher dissolution rate of MX was evidently connected to surface activation by mixing or milling, which was pronounced by the higher specific surface energy as detected by inverse gas chromatography. In addition to the particle size reduction, the carrier effect of the CH was confirmed for co-milling by linear regression between the MX maximum relative dissolution rate and the total surface area of the mixture (R2 = 0.863). No MX amorphization or crystalline structure change were detected. The work of adhesion/cohesion ratio of 0.9 supports the existence of preferential adherence of MX to the coarse particles of CH to form stable interactive mixtures.
Keywords
BCS class II, Interactive mixture, Dissolution rate, Co-milling, Chitosan, Meloxicam
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ISBN
ISSN
0928-0987
1879-0720
1879-0720
Language
English
Created during FHNW affiliation
Yes
Strategic action fields FHNW
Publication status
Published
Review
Peer review of the complete publication
Open access category
Gold
License
Citation
KUENTZ, Martin, Jana BROKESOVA, Michaela SLAMOVA, Petr ZAMOSTNY, Jakub KOKTAN, Lukas KREICIK, Petra SVACINOVA, Zdenka SKLUBALOVA und Barbora VRANÍKOVÁ, 2022. Mechanistic study of dissolution enhancement by interactive mixtures of chitosan with meloxicam as model. European Journal of Pharmaceutical Sciences. 1 Februar 2022. Bd. 169. DOI 10.1016/j.ejps.2021.106087. Verfügbar unter: https://doi.org/10.26041/fhnw-4120