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Published:
Jun 22, 2021Keywords:
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Main Article Content
Soluble curcumin prepared by solid dispersion using four different carriers: Phase solubility, molecular modelling and physicochemical characterization
Abstract
Purpose: To prepare curcumin solid dispersions (SDs) using four different carriers, evaluate their thermodynamic properties, and carry out physicochemical characterization on them.
Methods: Solid dispersions (SDs) of curcumin were prepared using hot melt method. Hydrophilic carriers, including poloxamers (P-407 and P-188), gelucire 50/13 and mannitol were used in the ratios of 1:3, 1:4, 1:5, 1:6 and 1:7 (curcumin : carrier). The new formulations were characterized in the liquid state by phase solubility studies (PSS), and in the solid state using Fourier transform infrared (FTIR) spectroscopy, powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM). Molecular modelling (MM) was also performed on the SDs.
Results: The results of PSS revealed an AL-type phase-solubility profile with spontaneous binding process, indicating 1:1 stoichiometry. The stability constant (Ka) of curcumin with various carriers at 25 and 37 °C were in the order: P-407 (631.9 and 524.9 M-1 ) > P-188 (436.48 and 388.28 M-1 ) > gelucire (100.14 and 112.05 M-1 ) > mannitol (10.88 and 11.90 M-1 ). The maximum stability constants of P-407 at 25 and 37 °C were 631 and 524 M-1 , respectively, which produced an accurate fit on MM (in silico model). Curcumin-P-407 complex produced enhanced solubility property (318 ± 14.46-fold). Physicochemical characterization revealed a shift in curcumin structure from crystalline to amorphous form without any chemical alterations, thereby enhancing solubility.
Conclusion: These results shown that the solubility of curcumin is greatly improved after its complexation with P-407 in SD, and the drug is converted into amorphous form without significant chemical modification.
