Abstract

Present work was investigated for enhancement of solubility, bioavailability and anti-cancer activity of curcumin, a potent natural anticancer agent. Solid microdispersion of curcumin was prepared by melt granulation technique using Gelucire® 50/13 as a hydrophilic carrier followed by adsorbtion on Aeroperl® 300 Pharma. Compatibility among curcumin and excipients were checked using FT-IR, DSC and XRD analysis. The prepared microdispersion was characterized for percent drug content, entrapment efficiency, surface morphology, particle size, solubility, bio-availability and anticancer activity. DSC analysis study had shown complete encapsulation of raw curcumin which was further supported by XRD study showing flat peaks. A 32 full factorial response surface quadratic model demonstrated the positive effect upon change in the concentration of independent variables viz. Gelucire® 50/13 and Aeroperl® 300 Pharma on dependent variables particle size; % entrapment efficiency. TEM analysis confirmed the nano particulate dispersion upon dilution in distilled water with many fold increased in solubility. Maximum solubility was observed in acidic buffer pH 1.2. In vivo study revealed increased in bio-availability in Wistar rats as compared to raw curcumin by HPLC analysis. In MTT assay study, curcumin microdispersion has shown more prominent anti-cancer activity than raw curcumin on breast cancer cell line culture, MCF-7. From above study, it may be concluded that implementation of this innovative approach could be a better alternative for oral nanocurcumin delivery to improve the quality of life patients suffering from cancer.

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