Controlled release of verapamil hydrochloride from waxy microparticles prepared by spray congealing

In this work, the potential of waxes for preparing with the ultrasonic spray congealing technique microparticles for controlling the in vitro release of verapamil HCl was investigated. The first part of the study encompassed the optimisation of the formulation to achieve an efficient drug incorporat...

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Bibliographic Details
Published in:Journal of controlled release 2003-03, Vol.88 (2), p.263-275
Main Authors: Passerini, Nadia, Perissutti, Beatrice, Albertini, Beatrice, Voinovich, Dario, Moneghini, Mariarosa, Rodriguez, Lorenzo
Format: Article
Language:English
Subjects:
Algorithms
Antiarythmic agents
Biological and medical sciences
Calcium Channel Blockers - administration & dosage
Calorimetry, Differential Scanning
Cardiovascular system
Chemical Phenomena
Chemistry, Physical
Controlled release
Delayed-Action Preparations
Drug Compounding
Excipients
General pharmacology
Kinetics
Medical sciences
Microscopy, Electron, Scanning
Microspheres
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Solubility
Spectrometry, X-Ray Emission
Spray congealing
Ultrasonic atomizer
Verapamil - administration & dosage
Verapamil HCl
Waxes
Waxy microparticles
X-Ray Diffraction
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Summary:In this work, the potential of waxes for preparing with the ultrasonic spray congealing technique microparticles for controlling the in vitro release of verapamil HCl was investigated. The first part of the study encompassed the optimisation of the formulation to achieve an efficient drug incorporation together with a satisfactory in vitro drug release rate. In particular, microcrystalline wax, stearyl alcohol and mixtures of the two were used. Also a surfactant (soya lecithin) was added to the formulations. After the particle size analysis, the characterisation of the microparticles involved the study of the solid state of drug and carriers in the systems (DSC, HSM and XRD) and the morphological and chemical analyses of the microparticle surface (SEM and XPS). Finally, the drug release mechanism from these devices was evaluated using the statistical moment analysis. The results of this study show that by selecting the type and the amount of the carriers, microparticles with a spherical shape and a good encapsulation efficiency were observed. These particles showed a zero-order release for 8 h, without modifying the solid state properties of the drug. Therefore, waxy microparticles prepared by the ultrasonic spray congealing technique are promising solvent-free devices for controlling the release of verapamil HCl.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(03)00009-9