Hu F X, Neoh K G, Kang E T
Department of Chemical and Biomolecular Engineering, National University of Singapore, Kent Ridge, Singapore 119260, Singapore.
Biomaterials. 2006 Nov;27(33):5725-33. doi: 10.1016/j.biomaterials.2006.07.014. Epub 2006 Aug 7.
The present study deals with the synthesis and characterization of tamoxifen-loaded magnetite/poly(l-lactic acid) composite nanoparticles (TMCN), and their in vitro anti-cancer activity against MCF-7 breast cancer cells. The composite nanoparticles with an average size of approximately 200 nm, were synthesized via a solvent evaporation/extraction technique in an oil/water emulsion. The superparamagnetic property (saturation magnetization value of approximately 7 emu/g) of the TMCN is provided by Fe(3)O(4) nanoparticles of approximately 6 nm encapsulated in the poly(l-lactic acid) matrix. The encapsulation efficiency of the Fe(3)O(4) and tamoxifen as a function of the concentration in the organic phase was investigated. The uptake of TMCN and tamoxifen by MCF-7 was estimated from the intracellular iron concentration. After 4h incubation of MCF-7 with TMCN, significant changes in the cell morphology were discernible from phase contrast microscopy. Cytotoxicity assay shows that while the Fe(3)O(4)-loaded poly(l-lactic acid) composite nanoparticles exhibit no significant cytotoxicity against MCF-7, approximately 80% of the these cells were killed after incubation for 4 days with TMCN.
本研究涉及载有他莫昔芬的磁铁矿/聚（L-乳酸）复合纳米颗粒（TMCN）的合成与表征，以及它们对MCF-7乳腺癌细胞的体外抗癌活性。通过油/水乳液中的溶剂蒸发/萃取技术合成了平均尺寸约为200nm的复合纳米颗粒。TMCN的超顺磁性（饱和磁化强度值约为7emu/g）由包裹在聚（L-乳酸）基质中的约6nm的Fe(3)O(4)纳米颗粒提供。研究了Fe(3)O(4)和他莫昔芬在有机相中的包封效率与浓度的关系。通过细胞内铁浓度估算了MCF-7对TMCN和他莫昔芬的摄取。用TMCN孵育MCF-7 4小时后，相差显微镜可观察到细胞形态有明显变化。细胞毒性试验表明，虽然载有Fe(3)O(4)的聚（L-乳酸）复合纳米颗粒对MCF-7没有明显的细胞毒性，但用TMCN孵育4天后，约80%的这些细胞被杀死。
