Dexamethasone-loaded nanoparticle-coated microparticles: Correlation between in vitro drug release and drug transport across Caco-2 cell monolayers
| Autor: | Marcia Russman Gallas, Ulrich F. Schaefer, Eva-Maria Collnot, Claus-Michael Lehr, Ruy Carlos Ruver Beck, Cristiane Rodrigues Drago Hoffmeister, Adriana Raffin Pohlmann, S.S. Guterres |
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| Rok vydání: | 2007 |
| Předmět: |
Drug
Chemistry Pharmaceutical Drug Compounding media_common.quotation_subject Pharmaceutical Science Nanoparticle Nanotechnology Microscopy Atomic Force Dexamethasone Nanocapsules Excipients X-Ray Diffraction Humans Particle Size Microparticle media_common Models Statistical Aqueous solution L-Lactate Dehydrogenase Chemistry Biological Transport Humidity General Medicine Hydrogen-Ion Concentration Controlled release Chemical engineering Spray drying Microscopy Electron Scanning Nanoparticles Liberation Caco-2 Cells Biotechnology |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics. 67:18-30 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2007.01.007 |
| Popis: | This work reports the preparation of dexamethasone in nanoparticle-coated microparticles and the study of the influence of such microencapsulation on drug absorption across Caco-2 cell monolayers. Nanoparticle-coated microparticles were prepared by spray-drying using nanocapsules (NC) or nanospheres (NS) in aqueous suspensions as coating material. Drug contents ranged from 64 to 134 mg g −1 , yields between 49% and 67% and moisture content below 2.0%. SEM and AFM analysis demonstrated that the nanoparticle-coated microparticles (20–53 μm) show nanostructures on their surface with a similar diameter compared to the aqueous suspensions. The type of nanocoating material had a significant influence on the drug release profile and on the drug permeation across Caco-2 cells: NC-coated microparticles led to a prolonged release and slower transport across Caco-2 cell monolayers, while the NS-coated microparticles showed a faster release and Caco-2 transport compared to uncoated microparticles. The correlation between the amount of drug permeated and the drug released (%) suggests that the drug absorption from such a delivery system is controlled mainly by the release rate rather than by epithelial permeability. Caco-2 transport studies appear to be a useful characterization tool for the development of microparticulate oral controlled release systems. |
| Databáze: | OpenAIRE |
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