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Cyclosporine-loaded solid lipid nanoparticles (SLN): Drug-lipid physicochemical interactions and characterization of drug incorporation
- Solid lipid nanoparticles (SLN) were produced loaded with cyclosporine A in order to develop an improved oral formulation. In this study, the particles were characterized with regard to the structure of the lipid particle matrix, being a determining factor for mode of drug incorporation and drug release. Differential scanning calorimetry (DSC) and wide-angle X-ray scattering (WAXS) measurements were employed for the analysis of the polymorphic modifications and mode of drug incorporation. Particles were produced using Imwitor®900 as lipid matrix (the suspension consisted of 10% particles, 8% Imwitor®900, 2% cyclosporine A), 2.5% Tagat S, 0.5% sodium cholate and 87% water. DSC and WAXS were used to analyse bulk lipid, bulk drug, drug incorporated in the bulk and unloaded and drug-loaded SLN dispersions. The processing of the bulk lipid into nanoparticles was accompanied by a polymorphic transformation from the ß to the α-modification. After production, the drug-free SLN dispersionsSolid lipid nanoparticles (SLN) were produced loaded with cyclosporine A in order to develop an improved oral formulation. In this study, the particles were characterized with regard to the structure of the lipid particle matrix, being a determining factor for mode of drug incorporation and drug release. Differential scanning calorimetry (DSC) and wide-angle X-ray scattering (WAXS) measurements were employed for the analysis of the polymorphic modifications and mode of drug incorporation. Particles were produced using Imwitor®900 as lipid matrix (the suspension consisted of 10% particles, 8% Imwitor®900, 2% cyclosporine A), 2.5% Tagat S, 0.5% sodium cholate and 87% water. DSC and WAXS were used to analyse bulk lipid, bulk drug, drug incorporated in the bulk and unloaded and drug-loaded SLN dispersions. The processing of the bulk lipid into nanoparticles was accompanied by a polymorphic transformation from the ß to the α-modification. After production, the drug-free SLN dispersions converted back to ß-modification, while the drug-loaded SLN stayed primarily in α-modification. After incorporation of cyclosporine A into SLN, the peptide lost its crystalline character. Based on WAXS data, it could be concluded that cyclosporine is molecularly dispersed in between the fatty acid chains of the liquid-crystalline α-modification fraction of the loaded SLN.…
Autor*innen: | R.H. Müller, S.A. Runge, V. Ravelli, Andreas ThünemannORCiD, W. Mehnert, E.B. Souto |
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Dokumenttyp: | Zeitschriftenartikel |
Veröffentlichungsform: | Verlagsliteratur |
Sprache: | Englisch |
Titel des übergeordneten Werkes (Englisch): | European journal of pharmaceutics and biopharmaceutics |
Jahr der Erstveröffentlichung: | 2008 |
Herausgeber (Institution): | Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik |
Verlag: | Elsevier |
Verlagsort: | Amsterdam |
Jahrgang/Band: | 68 |
Ausgabe/Heft: | 3 |
Erste Seite: | 535 |
Letzte Seite: | 544 |
Freie Schlagwörter: | Characterization; Cyclosporine A; Lipid polymorphism; Oral bioavailability; Solid lipid nanoparticles |
DOI: | 10.1016/j.ejpb.2007.07.006 |
ISSN: | 0939-6411 |
ISSN: | 1873-3441 |
Verfügbarkeit des Dokuments: | Physisches Exemplar in der Bibliothek der BAM vorhanden ("Hardcopy Access") |
Bibliotheksstandort: | Sonderstandort: Publica-Schrank |
Datum der Freischaltung: | 19.02.2016 |
Referierte Publikation: | Ja |
Datum der Eintragung als referierte Publikation: | 05.06.2008 |