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

Ming Sun, Shufang Nie, Xuan Pan, Ruiwen Zhang, Zhaoyang Fan, Shu Wang

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179 Scopus citations


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.

Original languageEnglish
Pages (from-to)15-24
Number of pages10
JournalColloids and Surfaces B: Biointerfaces
StatePublished - Jan 1 2014


  • Apoptosis
  • Breast cancer
  • Cellular uptake
  • Cytotoxicity
  • Nanostructured lipid carriers
  • Quercetin


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