Drug Release and Targeting: the Versatility of Polymethacrylate Nanoparticles for Peroral Administration Revealed by Using an Optimized In Vitro-Toolbox
| Autor: | Nerea Ferreirós, Thomas Ulshöfer, Michael J. Parnham, Sylvia Wagner, Matthias G. Wacker, Susanne Beyer, Astrid S. Kahnt, Aline Moosmann |
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| Rok vydání: | 2015 |
| Předmět: |
Drug Liberation
Anti-Inflammatory Agents Pharmaceutical Science Nanoparticle Administration Oral Pharmacology Drug Delivery Systems Polymethacrylic Acids Cell Line Tumor Humans Pharmacology (medical) Particle Size Gastrointestinal tract Drug Carriers Cyclooxygenase 2 Inhibitors Chemistry Organic Chemistry In vitro Targeted drug delivery Drug release Molecular Medicine Nanoparticles Caco-2 Cells Drug carrier Biotechnology |
| Zdroj: | Pharmaceutical research. 32(12) |
| ISSN: | 1573-904X |
| Popis: | The contribution of permeability and drug release to drug targeting were investigated in the course of development of a nanosized formulation of the anti-inflammatory compound TMP-001, for the local treatment in the gastrointestinal tract.TMP-001 was encapsulated by nanoprecipitation into Eudragit® RS 100. The permeability of these carriers was investigated in an Ussing chamber model and the release rate was determined under biorelevant conditions. Formulation toxicity and particle-cell-interaction were investigated by flow cytometry, fluorescence and electron microscopy. Furthermore, spray drying was performed.Effective internalization of Eudragit®-nanoparticles into cancer cells was demonstrated. A burst release of the nanoparticles implied poor interaction of TMP-001 with Eudragit®. A sustained release (70.5% release after 30 min compared to 98.0% for the API) was accomplished after spray drying yielded an increased particle size. Recovery rate of TMP-001 after spray drying was 94.2 ± 5.9%.The release of API from polymeric nanoparticles contributes profoundly to the in vivo-performance of drug delivery devices in the gastrointestinal tract. The impact of drug-polymer interaction and particle size was analyzed. Sustained release of TMP-001 could only be achieved by increasing particle size. Therefore, biorelevant release testing has been demonstrated to be a valid tool for nanoformulation design. |
| Databáze: | OpenAIRE |
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