Supramolecular organization and release properties of phospholipid-hyaluronan microparticles encapsulating dexamethasone
| Autor: | Carolina Gómez-Gaete, Amélie Bochot, Nicolas Tsapis, Madeleine Besnard, Elias Fattal, Claudie Bourgaux, Lídia Silva |
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| Rok vydání: | 2008 |
| Předmět: |
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2-Dipalmitoylphosphatidylcholine Stereochemistry Chemistry Pharmaceutical Drug Compounding Kinetics Anti-Inflammatory Agents Phospholipid Pharmaceutical Science Crystallography X-Ray Dexamethasone chemistry.chemical_compound Differential scanning calorimetry Hyaluronic acid Technology Pharmaceutical Hyaluronic Acid Particle Size Microparticle Solubility Drug Carriers Microscopy Confocal Calorimetry Differential Scanning Chemistry technology industry and agriculture General Medicine Microscopy Fluorescence Spray drying Biophysics Liberation lipids (amino acids peptides and proteins) Powders Biotechnology |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 70:116-126 |
| ISSN: | 0939-6411 |
| Popis: | We describe the supramolecular organization of hybrid microparticles encapsulating dexamethasone (DXM) prepared by spray drying 1,2-Dipalmitoyl-sn-Glycero-3-Phosphocholine (DPPC) and hyaluronic acid (HA). The effect of DXM concentration on size distribution and encapsulation efficacy was evaluated as a function of HA concentration. In the absence of HA, DXM leads to a strong particle aggregation, whereas in the presence of HA, the aggregation is practically suppressed. DXM percentage of encapsulation is high (95 ± 6%), independently of composition. Drug-excipient interactions were analyzed by differential scanning calorimetry (DSC) and X-ray diffraction. DSC demonstrates that only a small fraction of DXM interacts with DPPC, whereas X-ray diffraction does not detect this interaction. Finally, in vitro release studies show that HA does not influence DXM release kinetics. In all cases, a burst release of DXM is observed during the first hour. Under sink conditions, powder concentration in the release medium governs the extent of the burst. Under non sink conditions, DXM release is mostly governed by DXM solubility in the release medium. In the dry microparticles, DXM is probably mostly in amorphous domains within the DPPC-HA matrix. Upon hydration, the majority of the drug is released and only a small amount of DXM interacts with DPPC. |
| Databáze: | OpenAIRE |
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