Quercetin-nanostructured lipid carriers: Characteristics and anti-breast cancer activities in vitro

Quercetin (Q), a common dietary flavonoid, has gained research attention in cancer chemo-prevention, but its low level of aqueous solubility, stability, cellular bioavailability has limited its application. We have synthesized biocompatible and biodegradable Q-nanostructured lipid carriers (Q-NLC) using a novel phase inversion-based process method. The average size of Q-NLC was 32 nm in diameter. Q-NLC had good chemical and physical stability, and showed a sustained release pattern. The encapsulation efficiency and loading capacity of Q-NLC were 95% and 11%, respectively. The aqueous solubility of Q was dramatically improved by at least 1000 folds. The results from Raman spectroscopy, powder X-ray diffraction (XRD) and differential scanning calorimetry (DSC) demonstrated that Q presented in NLC as an encapsulated molecule form. As compared to native Q Q-NLC dramatically increased cytotoxicity in a dose-dependent manner (1-50 mu M) and induced apoptosis at 20 mu M in MCF-7 and MDA-MB-231 breast cancer cells. The enhanced cytotoxicity and apoptosis were parallel to increased Q uptake by those cancer cells. Void NLC did not change the viability and apoptosis of those cancer cells as compared to phosphate buffered saline. In conclusion, Q-NLC dramatically enhanced the anti-cancer activities of Q which were associated with enhanced Qsolubility and stability, and increased Q content in those cancer cells. Q-NLC have a potential for chemo-preventive use in breast cancer. (C) 2013 Elsevier B.V. All rights reserved.