Investigation and correlation of drug polymer miscibility and molecular interactions by various approaches for the preparation of amorphous solid dispersions

[Display omitted] Curcumin (CUR) was used as a poorly soluble drug whereas polyvinyl pyrrolidone K90 (PVP), Eudragit EPO (EPO), hydroxypropyl methylcellulose E5 (HPMC) and polyethylene glycol 8000 (PEG) were used as hydrophilic polymers. CUR polymer miscibility was evaluated by solubility parameter,...

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Bibliographic Details
Published in:European journal of pharmaceutical sciences 2015-04, Vol.71, p.12-24
Main Authors: Meng, Fan, Trivino, Anne, Prasad, Dev, Chauhan, Harsh
Format: Article
Language:English
Subjects:
Amorphous
Curcumin
Curcumin - chemistry
Drug Compounding
Miscibility
Models, Molecular
Molecular interactions
Polymers
Polymers - chemistry
Solid dispersion
Solubility
Thermogravimetry
Transition Temperature
X-Ray Diffraction
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Summary:[Display omitted] Curcumin (CUR) was used as a poorly soluble drug whereas polyvinyl pyrrolidone K90 (PVP), Eudragit EPO (EPO), hydroxypropyl methylcellulose E5 (HPMC) and polyethylene glycol 8000 (PEG) were used as hydrophilic polymers. CUR polymer miscibility was evaluated by solubility parameter, melting point depression and glass transition temperature (Tg) measurements. Molecular interactions between CUR and polymers were determined by Fourier-transform infrared spectroscopy (FTIR) and Raman. Amorphous solid dispersions were prepared with CUR–polymer ratio of 70:30 (w/w) by solvent evaporation technique and were evaluated for dissolution enhancement using USP II method. Physical states of solid dispersions were characterized by X-ray diffraction (XRD) whereas thermal behaviors were investigated using modulated differential scanning calorimetry (MDSC). CUR–EPO system showed good miscibility through all the approaches, whereas immiscibility was found in other CUR–polymer systems. CUR–EPO and CUR–HPMC systems showed significant molecular interactions whereas CUR–PVP and CUR–PEG showed no molecular interactions. All solid dispersions showed significant dissolution enhancement with CUR–EPO showing highest dissolution rate during first 1h whereas CUR–HPMC was effective in maintaining high CUR concentrations for 6h. The study highlights the importance of investigating and correlating drug polymer miscibility and molecular interactions by various approaches for successful formulation of amorphous solid dispersions.
ISSN:0928-0987
1879-0720
DOI:10.1016/j.ejps.2015.02.003