Phytosomal Nanoparticles Preparation of Curcuminoids to Enhance Cellular Uptake of Curcuminoids on Breast Cancer Cell Line MCF-7

Objective: Curcuminoids, the bioactive compounds extracted from Curcuma longa consisting of Curcumin (CUR), demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), have shown promising biological effects, including anticancer activity. This study sought to prepare a physically stable phytosomal nanoparticles of curcuminoids (Curs-Phyto) to facilitate uptake of curcuminoids on breast cancer cells line, and further increase the cytotoxicity against cancer cells. Methods: The evaporation combined extrusion technique was employed to prepare phytosomal curcuminoids nanoparticles. The interaction between curcuminoids and phospholipid by a hydrogen bond was confirmed by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), fourier transform infrared (FT-IR), and ¹H nuclear magnetic resonance (¹H-NMR). Their physicochemical characterizations and stability in simulated gastric and intestinal media were investigated. The effects of Curs-Phyto on MCF-7 cells were evaluated by flow cytometry, MTS assay and cell cycle analysis. Results: We found that the Curs-Phyto were formed at a spherical shape with good size (~ 180 nm), a narrow size distribution (PDI < d0.2), high complexation rate (~ 87%, 95%, and 90% for BDMC, DMC, and CUR respectively) and high loading capacity of curcuminoids. More importantly, the Curs-Phyto showed the increased cellular uptake and enhanced cytotoxicity against MCF- 7 cancer cells, compared to free curcuminoids. Conclusion: These results indicated that the phytosome could be a promising oral delivery system for curcuminoids for cancer treatment.