Preparation of Curcumin Solid Lipid Nanoparticle and Studies on Its Anti- Cancer Effect and Pharmacokinetics in Rats
Purpose: The aim of this study was to encapsulate curcumin into solid lipid nanoparticle (SLN) to improve its aqueous solubility and stability, as well as to modify its anti-cancer activity and pharmacokinetics. Methods: Curcumin-loaded SLNs (CSLN) were prepared by high-pressure homogenization. Morphology, physiochemical stability and release profile of curcumin in the optimized formulation were investigated. The anti-cancer activity and intracellular uptake were evaluated on MCF-7 breast cancer cell by SRB and flow cytometry analysis. The pharmacokinetic profiles of curcumin in SLN after intravenous administration were studied in rats. Results: An optimized formulation consisting of Dynasan 114?, Sefso1-218?, Pluronic F68? and curcumin (630:70:300:8,w/w) and loaded with 0.8％ drug were prepared, which could dispersed into water with a mean particle size of 152.8 ± 4.7 nm and high entrapment efficiency (~ 90％). Curcumin showed a two-phase sustained release profile from C-SLN with improved chemical stability. C-SLN exhibited a prolonged inhibition activity to cancer cells, which was close to curcumin solubilized solution. A time- dependent increased intracellular uptake of curcumin was observed for C-SLN. Following intravenous administration to rats, both bioavailability and clearance of curcumin increased by 1.25-fold compared with unformulated drug. Conclusion: C-SLN with improved dispensability and chemical stability in aqueous system has been successfully developed. Compared to unformulated drug, C-SLN exhibited a prolonged inhibition to breast cancer cell in vitro and significant higher plasma concentrations in rats after intravenous administration.
solid lipid nanoparticles curcumin stability sustained release anti-cancer pharmacokinetics
Ying Zheng Jiabei Sun Shaoping Sun Qingwen Zhang
The State Key Laboratory for Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau SAR, China.
国际会议
The Second Asian Symposium on Pharmaceutical Sciences and Technology(第二届亚洲药物制剂科学研讨会)
西安
英文
59-60
2011-09-19（万方平台首次上网日期，不代表论文的发表时间）