Mapping Multiple Phases in Curcumin Binary Solid Dispersions by Fluorescence Contrasting

Chinese Chemical Letters(2024)

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摘要
The microphases and miscibility in binary curcumin (Cur) solid dispersions (SDs) with amorphous polyvinylpyrrolidone K30 (PVP K30) and semi-crystalline poloxamer (P407) and poly(ethylene glycol) 6000 (PEG6000) as carriers were investigated by fluorescence contrasting utilizing confocal laser scanning microscopy. A super sensitive fluorophore P4 with typical aggregation-caused quenching properties was employed to stain the continuous polymer phases and contrasted with the autofluorescence of the model drug Cur. In addition, differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) were utilized to assist in explanation of the fluorescence results. In all three SD systems, there is always a homogenous polymer phase stained by P4 and it is difficult to adulterate Cur crystals by P4. Cur-enriched rather than polymer-enriched domains could be detected. In the Cur-PVP K30 system, Cur exists in an amorphous form at a Cur loading level of 50% and below, while Cur crystallines phase out and continuously grow with the increase of Cur loading from 60% to 90%. The phase behaviors in the Cur-P407 and Cur-PEG 6000 systems are similar but with minor differences. In both systems, Cur phases out as clusters of drug-enriched domains at a loading level of 20% and below, which however cannot be correlated with crystallization, as evidenced by both DSC and PXRD. There is a transition from an amorphous to a crystalline state from 20% to 30% Cur loading, above which Cur crystallines can be detected. It is interesting that a co-mix phase of both Cur- and PEG 6000-enriched domains can be identified at Cur loading levels of 10% and less. Taking together, it is concluded that contrasting Cur autofluorescence with the signals of P4 proves to be a functional strategy to reveal multiple phases in the binary SD systems investigated.
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关键词
Solid dispersion,Curcumin,PEG,PVP,Poloxamer,Fluorescence,Environment-responsive,Confocal laser scanning microscopy
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