Solid dispersion of quercetin in cellulose derivative matrices influences both solubility and stability

► Amorphous solid dispersions up to 50% quercetin in carboxyl-containing cellulose esters. ► Carboxyl-containing cellulose esters stabilize amorphous quercetin in solid, solution phases. ► Amorphous dispersion in PVP prevents quercetin chemical degradation in solution. ► PVP strongly enhances querce...

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Bibliographic Details
Published in:Carbohydrate polymers 2013-02, Vol.92 (2), p.2033-2040
Main Authors: Li, Bin, Konecke, Stephanie, Harich, Kim, Wegiel, Lindsay, Taylor, Lynne S., Edgar, Kevin J.
Format: Article
Language:English
Subjects:
Amorphous solid dispersion
Applied sciences
Bioavailability
Biological and medical sciences
Cellulose - chemistry
Cellulose acetate adipate propionate
Cellulose and derivatives
CMCAB
Drug Carriers - chemistry
Drug Stability
Exact sciences and technology
General pharmacology
HPMCAS
Medical sciences
Natural polymers
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Physicochemistry of polymers
Povidone - chemistry
Quercetin
Quercetin - chemistry
Solubility
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Summary:► Amorphous solid dispersions up to 50% quercetin in carboxyl-containing cellulose esters. ► Carboxyl-containing cellulose esters stabilize amorphous quercetin in solid, solution phases. ► Amorphous dispersion in PVP prevents quercetin chemical degradation in solution. ► PVP strongly enhances quercetin solution concentration but releases at low pH. Amorphous solid dispersions (ASD) of quercetin (Que) in cellulose derivative matrices, carboxymethylcellulose acetate butyrate (CMCAB), hydroxypropylmethylcellulose acetate succinate (HPMCAS), and cellulose acetate adipate propionate (CAAdP) were prepared with the goal of identifying an ASD that effectively increased Que aqueous solution concentration. Crystalline quercetin and Que/poly(vinylpyrrolidinone) (PVP) ASD were evaluated for comparison. Powder X-ray diffraction (XRPD) and differential scanning calorimetry (DSC) were used to examine the crystallinity of ASDs, physical mixtures (PM) and quercetin. ASDs were amorphous up to 50wt% Que. Que stability against crystallization and solution concentrations from these ASDs were significantly higher than those observed for physical mixtures and crystalline Que. PVP stabilizes against both Que degradation and recrystallization; in contrast, these carboxylated cellulose derivatives inhibit recrystallization but release Que slowly. PVP ASDs afforded fast and complete drug release, while ASDs using these three cellulose derivatives provide slow, incomplete, pH-triggered drug release.
ISSN:0144-8617
1879-1344
DOI:10.1016/j.carbpol.2012.11.073