TY - JOUR
T1 - Quercetin-nanostructured lipid carriers
T2 - Characteristics and anti-breast cancer activities in vitro
AU - Sun, Ming
AU - Nie, Shufang
AU - Pan, Xuan
AU - Zhang, Ruiwen
AU - Fan, Zhaoyang
AU - Wang, Shu
N1 - Funding Information:
This work was supported by College of Human Sciences at Texas Tech University, USA .
PY - 2014/1/1
Y1 - 2014/1/1
N2 - 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. μM) and induced apoptosis at 20. μM 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 Q solubility and stability, and increased Q content in those cancer cells. Q-NLC have a potential for chemo-preventive use in breast cancer.
AB - 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. μM) and induced apoptosis at 20. μM 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 Q solubility and stability, and increased Q content in those cancer cells. Q-NLC have a potential for chemo-preventive use in breast cancer.
KW - Apoptosis
KW - Breast cancer
KW - Cellular uptake
KW - Cytotoxicity
KW - Nanostructured lipid carriers
KW - Quercetin
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U2 - 10.1016/j.colsurfb.2013.08.032
DO - 10.1016/j.colsurfb.2013.08.032
M3 - Article
C2 - 24060926
AN - SCOPUS:84884383222
SN - 0927-7765
VL - 113
SP - 15
EP - 24
JO - Colloids and Surfaces B: Biointerfaces
JF - Colloids and Surfaces B: Biointerfaces
ER -