Mapping multiple phases in curcumin binary solid dispersions by fluorescence contrasting  

作　　者：Ying Xu Chengying Shen Hailong Yuan Wei Wu 

机构地区：[1]Key Laboratory of Smart Drug Delivery of MOE,School of Pharmacy,Fudan University,Shanghai 201203,China [2]Center for Medical Research and Innovation,Shanghai Pudong Hospital,Fudan University Pudong Medical Center,Shanghai 201399,China [3]Department of Pharmacy,Air Force Medical Center,PLA,Beijing 100142,China [4]Jiangxi Provincial People’s Hospital,The First Affiliated Hospital of Nanchang Medical College,Nanchang 330006,China

出　　处：《Chinese Chemical Letters》2024年第9期266-272,共7页中国化学快报（英文版）

基　　金：supported by the Science and Technology Commission of Shanghai Municipality(No.21430760800).

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.

关 键 词：Solid dispersion CURCUMIN PEG PVP POLOXAMER FLUORESCENCE Environment-responsive Confocal laser scanning microscopy 

分 类 号：O657.3[理学—分析化学] TQ460.1[理学—化学] R313[化学工程—制药化工]