Development of Eudragit® S100 based pH-responsive microspheres of zaleplon by spray-drying: Tailoring the drug release properties

The aim of this work was to develop Eudragit® S100 (ES100) based pH-responsive microspheres of zaleplon (ZAL) as a potential delivery system for treatment of an insomnia characterised by premature awaking and inability to fall asleep again. Microspheres were prepared by spray-drying of ZAL/ES100 dis...

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Bibliographic Details
Published in:Powder technology 2015-10, Vol.283, p.334-343
Main Authors: Jablan, Jasna, Jug, Mario
Format: Article
Language:English
Subjects:
Enteric microspheres
Eudragit
pH-dependent drug release
Solid state analysis
Spray-drying
Zaleplon
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Summary:The aim of this work was to develop Eudragit® S100 (ES100) based pH-responsive microspheres of zaleplon (ZAL) as a potential delivery system for treatment of an insomnia characterised by premature awaking and inability to fall asleep again. Microspheres were prepared by spray-drying of ZAL/ES100 dispersion from ethanolic (MS1) or 0.96% aqueous NH4HCO3 solution (MS2). In second case ES100 was first transformed into soluble, thermolabile ammonium salt and then regenerated by an additional thermal treatment at 85°C for 3.5h after spray-drying, as confirmed by FTIR. Preparation from ethanolic medium (MS1) resulted in higher preparation yield (75.14% vs. 56.55%; p
ISSN:0032-5910
1873-328X
DOI:10.1016/j.powtec.2015.05.045