Micronization and microencapsulation of felodipine by supercritical carbon dioxide

Felodipine (FLD) is a poorly water-soluble drug. To improve its dissolution rate, the rapid expansion of supercritical solutions (RESS) technique was used to prepare micronized FLD drug particles, which were encapsulated in poly-(ethylene glycol) 4000 (PEG 4000). The physical properties of the encap...

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Bibliographic Details
Published in:Journal of microencapsulation 2006-05, Vol.23 (3), p.265-276
Main Authors: Chiou, Andy Hong-Jey, Cheng, Hsiu-Cheng, Wang, Da-Peng
Format: Article
Language:English
Subjects:
Biological and medical sciences
Carbon Dioxide - chemistry
Chemical Phenomena
Chemistry, Pharmaceutical - instrumentation
Chemistry, Pharmaceutical - methods
Chemistry, Physical
dissolution rate
Drug Compounding - instrumentation
Drug Compounding - methods
Feasibility Studies
Felodipine - chemistry
General pharmacology
Medical sciences
microparticles
Microspheres
Molecular Structure
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
physical properties
Polyethylene Glycols - chemistry
Poorly water-soluble drug
rapid expansion of supercritical solutions
Solubility
Thermodynamics
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Summary:Felodipine (FLD) is a poorly water-soluble drug. To improve its dissolution rate, the rapid expansion of supercritical solutions (RESS) technique was used to prepare micronized FLD drug particles, which were encapsulated in poly-(ethylene glycol) 4000 (PEG 4000). The physical properties of the encapsulated drug particles were characterized by a variety of analytical methods, including optical light microscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (powder-XRD) and the dissolution behaviour of FLD was studied in the microparticles. The supercritical condition of micronized FLD occurred at a relatively high pressure and moderate temperature. FLD-PEG 4000 microparticles compared well with micronized FLD. RESS was effective in reducing the particle size of FLD; spot-shaped micronized FLD and popcorn-shaped FLD-PEG 4000 microparticles were observed. The particulate properties of the microparticles included a narrow distribution and uniform size. Thermodynamic analysis showed an implantation interaction between FLD and PEG 4000 molecules, but no polymorphism in the micronized FLD or FLD-PEG 4000 microparticles. FLD-PEG 4000 microparticles had a significantly faster drug dissolution rate than micronized FLD. These data show that RESS can be used to prepare FLD-PEG 4000 microparticles with small particle size (2-6 µm) and enhanced dissolution rate.
ISSN:0265-2048
1464-5246
DOI:10.1080/02652040500435071