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 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.
Nutritional Science Program, Texas Tech University, Box 41240, Lubbock, TX 79409, USA.
Ming
M
Sun
Nutritional Science Program, Texas Tech University, Box 41240, Lubbock, TX 79409, USA.
Shufang
S
Nie
Department of Electrical and Computer Engineering and Nano Tech Center, Texas Tech University, Lubbock, TX 79409, USA.
Xuan
X
Pan
Department of Pharmaceutical Sciences, Texas Tech University Health Sciences Center, Amarillo, TX 79106, USA.
Ruiwen
R
Zhang
Department of Electrical and Computer Engineering and Nano Tech Center, Texas Tech University, Lubbock, TX 79409, USA.
Zhaoyang
Z
Fan
Nutritional Science Program, Texas Tech University, Box 41240, Lubbock, TX 79409, USA. Electronic address: shu.wang@ttu.edu.
Shu
S
Wang
D000975:Antioxidants / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D011794:Quercetin / Q000737:chemistry* / Q000494:pharmacology*; D014961:X-Ray Diffraction
D000975:Antioxidants; D004337:Drug Carriers; D008055:Lipids; D011794:Quercetin
Apoptosis; Breast cancer; Cellular uptake; Cytotoxicity; Nanostructured lipid carriers; Quercetin