Journal
PHARMACEUTICS
Volume 11, Issue 9, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics11090442
Keywords
Curcumin; polyvinylpyrrolidone (PVP); solid dispersions; molecular modeling; drug-polymer interactions
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Funding
- Guangdong Province Leadership Grant, China National Science Foundation [81803000]
- China Postdoctoral Science Foundation [2013M540649]
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The molecular interactions between compound and polymeric carriers are expected to highly contribute to high drug load and good physical stability of solid dispersions. In this study, a series of amorphous solid dispersions (ASD) of Curcumin (Cur) were prepared with different polymers by the solvent evaporation method. With the carrier polyvinylpyrrolidone (PVP), the amorphous solid dispersion system exhibits a better solubility and stability than that with poloxamers and HP-beta-CD due to the strong drug-polymer interaction. The drug/polymer interaction and their binding sites were investigated by combined experimental (XRD, DSC, FTIR, SEM, Raman, and 1H-NMR) and molecular dynamics simulation techniques. The Curcumin ASD demonstrated enhanced bioavailability by 11-fold and improved anti-inflammatory activities by the decrease in cytokine production (MMP-9, IL-1 beta, IL-6, VEGF, MIP-2, and TNF-alpha) compared to the raw Curcumin. The integration of experimental and modeling techniques is a powerful tool for the rational design of formulation development.
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