(T1330-01-06) Statistical Optimization of Stable Quercetin Nanoparticles for Tumor Targeting

Purpose: The aim of this study is to create stable quercetin nanoparticles that can target tumor cells within the body.

Methods: Using solvent emulsification technique, quercetin nanoparticles were synthesized with varying concentrations of zein, beta-cyclodextrin, and pectin. These formulations were optimized using factorial response surface analysis. The stability of the optimized quercetin nanoparticles in conditioned media, which collected from the subculture of colorectal cancer cell line HCT-116 , was compared to the stability of the drug in powder form over 24 h. Furthermore, the cytotoxic effect of the quercetin powder and the optimized quercetin nanoparticles were evaluated against two colorectal cancer cell lines (HT-29 and HCT-116) using MTT assay under normoxic conditions. A flow cytometric analysis was performed using Annexin V/FITC apoptotic assay to detect the number of cells that underwent apoptosis.

Results: The optimized quercetin nanoparticles consists of 10 mg of zein and 31.35 mg beta-cyclodextrin without pectin, resulting in a particle size of 221 nm, a polydispersity index of 0.115, and a zeta potential of 7.65 mV. Compared to the free drug powder, the optimized quercetin nanoparticles were significantly more stable in the conditioned media of HCT-116 over 24 hours. In HT-29, the optimized nanoparticles and the free drug had IC50 values of of 29.33 µM and 60.78 µM, respectively. In HCT-116, optimized nanoparticles and the free drug had IC50 values 31.11 µM and 59.20 µM , respectively. The flow cytometric analysis after annexin-V/FITC staining revealed that the optimized quercetin nanoparticles significantly induced greater apoptosis in both cell lines compared to the free drug powder and plain nanoparticles.

Conclusion: In Conclusion, the optimized quercetin nanoparticles were found to have the potential to increase the drug stability in physiological fluids and improve cytotoxic effect against the two colorectal cancer cell lines by apoptosis induction when compared to the drug in powder form as well as plain nanoparticles.