Water-Resistant Drug–Polymer Interaction Contributes to the Formation of Nano-Species during the Dissolution of Felodipine Amorphous Solid Dispersions

Drug–polymer interactions are of great importance in amorphous solid dispersion (ASD) formulation for both dissolution performance and physical stability considerations. In this work, three felodipine ASD systems with drug loading ranging from 5 to 20% were prepared using PVP, PVP-VA, or HPMC-AS as...

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Veröffentlicht in:Molecular pharmaceutics 2022-08, Vol.19 (8), p.2888-2899
Hauptverfasser: Liu, Lei, Chen, Linc, Müllers, Wouter, Serno, Peter, Qian, Feng
Format: Artikel
Sprache:eng
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Zusammenfassung:Drug–polymer interactions are of great importance in amorphous solid dispersion (ASD) formulation for both dissolution performance and physical stability considerations. In this work, three felodipine ASD systems with drug loading ranging from 5 to 20% were prepared using PVP, PVP-VA, or HPMC-AS as the polymer matrix. The amorphization and homogeneity were confirmed by differential scanning calorimetry and powder X-ray diffraction. The intrinsic dissolution behavior of these ASDs was studied in 0.05 M HCl and phosphate-buffered saline (PBS) (pH 6.5). In 0.05 M HCl, PVP-VA ASDs with low drug loading (
ISSN:1543-8384
1543-8392
DOI:10.1021/acs.molpharmaceut.2c00250