Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets

Microstructure consolidation of pellets is envisaged to enable a reduction of drug release in early dissolution phase. This study examines the effects of processing air pressure on drug release property of pellets and their mechanistic modifications on the matrices. The pellets were prepared using a...

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Published in:Chemical Engineering Research and Design
Main Author: Hanafi N.; Wong T.W.
Format: Article
Language:English
Published: Institution of Chemical Engineers 2015
Online Access:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84955440391&doi=10.1016%2fj.cherd.2015.09.009&partnerID=40&md5=e25d3ff9d1b8bc964d714adb68939b57
id 2-s2.0-84955440391
spelling 2-s2.0-84955440391
Hanafi N.; Wong T.W.
Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
2015
Chemical Engineering Research and Design
104

10.1016/j.cherd.2015.09.009
https://www.scopus.com/inward/record.uri?eid=2-s2.0-84955440391&doi=10.1016%2fj.cherd.2015.09.009&partnerID=40&md5=e25d3ff9d1b8bc964d714adb68939b57
Microstructure consolidation of pellets is envisaged to enable a reduction of drug release in early dissolution phase. This study examines the effects of processing air pressure on drug release property of pellets and their mechanistic modifications on the matrices. The pellets were prepared using a high shear mixer at the jacket temperatures of 55 °C and 75 °C denoting thermoplastic and melt agglomeration, respectively with alginate, polyethylene glycol, calcium acetate and chlorpheniramine maleate as hydrophilic matrix polymer, meltable binder, crosslinker and water-soluble model drug. The formed pellets were subjected to size, shape, morphology, drug content, drug release, calcium content, and molecular pharmaceutics analysis in their fresh state or after undergoing dissolution process. Low jacket temperature agglomeration was characterized by prolonged massing, extensive non-meltable solid particle rearrangement, core-to-surface binder migration and ease of pellet fragmentation at early dissolution phase due to improved matrix wetting by water-soluble surface binder. Air-pressurized agglomeration similarly promoted core-to-surface binder migration and ease of pellet fragmentation. At 75 °C instead of 55 °C, matrix pressurization by air was accompanied by core consolidation. It led to fast pellet breakup into dense fragments that exhibited a sustained drug release behavior. At 55 °C, matrix pressurization by air failed to consolidate the pellets due to air bubbling of core with prolonged massing, and no significant drug release retardation was observed. The processing air pressure can aid to consolidate pellets prepared by melt instead of thermoplastic agglomeration technique and reduce their drug release propensity. © 2015 The Institution of Chemical Engineers.
Institution of Chemical Engineers
02638762
English
Article

author Hanafi N.; Wong T.W.
spellingShingle Hanafi N.; Wong T.W.
Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
author_facet Hanafi N.; Wong T.W.
author_sort Hanafi N.; Wong T.W.
title Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
title_short Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
title_full Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
title_fullStr Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
title_full_unstemmed Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
title_sort Melt pelletization of alginate: Effects of air pressurization on consolidation and drug release property of pellets
publishDate 2015
container_title Chemical Engineering Research and Design
container_volume 104
container_issue
doi_str_mv 10.1016/j.cherd.2015.09.009
url https://www.scopus.com/inward/record.uri?eid=2-s2.0-84955440391&doi=10.1016%2fj.cherd.2015.09.009&partnerID=40&md5=e25d3ff9d1b8bc964d714adb68939b57
description Microstructure consolidation of pellets is envisaged to enable a reduction of drug release in early dissolution phase. This study examines the effects of processing air pressure on drug release property of pellets and their mechanistic modifications on the matrices. The pellets were prepared using a high shear mixer at the jacket temperatures of 55 °C and 75 °C denoting thermoplastic and melt agglomeration, respectively with alginate, polyethylene glycol, calcium acetate and chlorpheniramine maleate as hydrophilic matrix polymer, meltable binder, crosslinker and water-soluble model drug. The formed pellets were subjected to size, shape, morphology, drug content, drug release, calcium content, and molecular pharmaceutics analysis in their fresh state or after undergoing dissolution process. Low jacket temperature agglomeration was characterized by prolonged massing, extensive non-meltable solid particle rearrangement, core-to-surface binder migration and ease of pellet fragmentation at early dissolution phase due to improved matrix wetting by water-soluble surface binder. Air-pressurized agglomeration similarly promoted core-to-surface binder migration and ease of pellet fragmentation. At 75 °C instead of 55 °C, matrix pressurization by air was accompanied by core consolidation. It led to fast pellet breakup into dense fragments that exhibited a sustained drug release behavior. At 55 °C, matrix pressurization by air failed to consolidate the pellets due to air bubbling of core with prolonged massing, and no significant drug release retardation was observed. The processing air pressure can aid to consolidate pellets prepared by melt instead of thermoplastic agglomeration technique and reduce their drug release propensity. © 2015 The Institution of Chemical Engineers.
publisher Institution of Chemical Engineers
issn 02638762
language English
format Article
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record_format scopus
collection Scopus
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