Surfactant-free amorphous solid dispersion with high dissolution for bioavailability enhancement of hydrophobic drugs: a case of quercetin
نویسندگان
چکیده
Abstract At present, saccharides as hydrophilic matrixes, have been gradually used in amorphous solid dispersions (ASD) for dispersing poorly water-soluble drugs without surfactants. In this study, an chitosan oligosaccharide (COS) was applied a matrix to form surfactant-free ASD via the ball milling vitrify quercetin (QUE) and enhance dissolution bioavailability. Solid-state characterization (DSC, XRPD, FTIR, SEM PLM) physical stability assessments verified that prepared ASDs showed excellent with complete amorphization due potential interactions between QUE COS. vitro sink tests suggested all QUE-COS (w:w, 1:1, 1:2 1:4) significantly enhanced rate of QUE. Meanwhile, non-sink exhibited maximum supersaturated concentration ranged from 112.62 138.00 µg/mL ASDs, which much higher than pure Besides, supersaturation kept at least 24 h. rat pharmacokinetics, oral bioavailability 1.64 ? 2.25 times increase compared (p < .01). Hence, present study confirms COS could be promising enhancing performance
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ژورنال
عنوان ژورنال: Drug Development and Industrial Pharmacy
سال: 2021
ISSN: ['0363-9045', '1520-5762']
DOI: https://doi.org/10.1080/03639045.2020.1862173