Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation

The impregnation of poorly water-soluble drug onto the surface of a suitable pharmaceutical excipient, used as a hydrophilic carrier, can lead to the preparation of systems with improved dissolution properties due to the separation of drug crystal particles on the carrier surface. For this purpose,...

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Main Authors: Petr Zámostný, Michal Drahozal, Ondřej Švehla, Simona Römerová, Nikita Marinko
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Crystals
Subjects:
Online Access:https://www.mdpi.com/2073-4352/13/3/527
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author Petr Zámostný
Michal Drahozal
Ondřej Švehla
Simona Römerová
Nikita Marinko
author_facet Petr Zámostný
Michal Drahozal
Ondřej Švehla
Simona Römerová
Nikita Marinko
author_sort Petr Zámostný
collection DOAJ
description The impregnation of poorly water-soluble drug onto the surface of a suitable pharmaceutical excipient, used as a hydrophilic carrier, can lead to the preparation of systems with improved dissolution properties due to the separation of drug crystal particles on the carrier surface. For this purpose, a method based on impregnation of hydrophilic matrix by the hydrophobic poorly water-soluble drug Meloxicam (MX) solution in volatile organic solvent was used. After the evaporation of the solvent, the method resulted in coverage of the carrier surface by drug crystals. The influence of the amount and concentration of the impregnating solution on the formed MX crystal size and the dissolution rate was evaluated. Firstly, the impregnation forming crystals on the planar surface was studied and the MX maximum dissolution flux from that surface was determined. The optimum preparation method was further used to produce a volume of impregnated granules. The dissolution performance of the granules was evaluated, and the dissolution kinetics was described by mathematical models. The polymorphic modification of impregnated API and influence of impregnated drug amount on the hydrophilic carrier surface coverage were considered. From the results of this work, it is clear that the impregnated drug amount and the number of impregnations cycles can be optimized to achieve maximum drug release rate.
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spelling doaj.art-c060b0b145d24ccd9d302e4cba5202eb2023-11-17T10:30:00ZengMDPI AGCrystals2073-43522023-03-0113352710.3390/cryst13030527Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-EvaporationPetr Zámostný0Michal Drahozal1Ondřej Švehla2Simona Römerová3Nikita Marinko4Department of Organic Technology, Faculty of Chemical Technology, University of Chemistry and Technology Prague, Technická 5, Dejvice, 166 28 Prague, Czech RepublicDepartment of Organic Technology, Faculty of Chemical Technology, University of Chemistry and Technology Prague, Technická 5, Dejvice, 166 28 Prague, Czech RepublicDepartment of Organic Technology, Faculty of Chemical Technology, University of Chemistry and Technology Prague, Technická 5, Dejvice, 166 28 Prague, Czech RepublicDepartment of Organic Technology, Faculty of Chemical Technology, University of Chemistry and Technology Prague, Technická 5, Dejvice, 166 28 Prague, Czech RepublicDepartment of Organic Technology, Faculty of Chemical Technology, University of Chemistry and Technology Prague, Technická 5, Dejvice, 166 28 Prague, Czech RepublicThe impregnation of poorly water-soluble drug onto the surface of a suitable pharmaceutical excipient, used as a hydrophilic carrier, can lead to the preparation of systems with improved dissolution properties due to the separation of drug crystal particles on the carrier surface. For this purpose, a method based on impregnation of hydrophilic matrix by the hydrophobic poorly water-soluble drug Meloxicam (MX) solution in volatile organic solvent was used. After the evaporation of the solvent, the method resulted in coverage of the carrier surface by drug crystals. The influence of the amount and concentration of the impregnating solution on the formed MX crystal size and the dissolution rate was evaluated. Firstly, the impregnation forming crystals on the planar surface was studied and the MX maximum dissolution flux from that surface was determined. The optimum preparation method was further used to produce a volume of impregnated granules. The dissolution performance of the granules was evaluated, and the dissolution kinetics was described by mathematical models. The polymorphic modification of impregnated API and influence of impregnated drug amount on the hydrophilic carrier surface coverage were considered. From the results of this work, it is clear that the impregnated drug amount and the number of impregnations cycles can be optimized to achieve maximum drug release rate.https://www.mdpi.com/2073-4352/13/3/527Meloxicamdrug dissolutionimpregnationdrug release
spellingShingle Petr Zámostný
Michal Drahozal
Ondřej Švehla
Simona Römerová
Nikita Marinko
Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
Crystals
Meloxicam
drug dissolution
impregnation
drug release
title Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
title_full Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
title_fullStr Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
title_full_unstemmed Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
title_short Drug Release from Carrier Systems Comprising Meloxicam Crystals Formed by Impregnation-Evaporation
title_sort drug release from carrier systems comprising meloxicam crystals formed by impregnation evaporation
topic Meloxicam
drug dissolution
impregnation
drug release
url https://www.mdpi.com/2073-4352/13/3/527
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AT michaldrahozal drugreleasefromcarriersystemscomprisingmeloxicamcrystalsformedbyimpregnationevaporation
AT ondrejsvehla drugreleasefromcarriersystemscomprisingmeloxicamcrystalsformedbyimpregnationevaporation
AT simonaromerova drugreleasefromcarriersystemscomprisingmeloxicamcrystalsformedbyimpregnationevaporation
AT nikitamarinko drugreleasefromcarriersystemscomprisingmeloxicamcrystalsformedbyimpregnationevaporation