Monteagudo E, Gándola Y, González L, Bregni C, Carlucci A M
Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Junín 956, 1113 Buenos Aires, Argentina.
J Drug Deliv. 2012;2012:236713. doi: 10.1155/2012/236713. Epub 2012 Jan 5.
Microemulsions (MEs) were designed by an innovative rational development, characterized, and used to load up to 20 mM of Tamoxifen citrate (TMX). They were made with acceptable and well-characterized excipients for all the routes of administration. Some of their properties, such as nanometric mean size and long stability shelf life, make them interesting drug delivery systems. The results obtained after the in vitro inhibition of estradiol-induced proliferation in MCF-7 breast cancer cells demonstrated a significant effect in cell growth. A decreasing of at least 90% in viable cells was shown after the incubation with MEs containing 20 mM of TMX. Besides, two compositions which loaded 10 mM of drug showed a cytotoxic effect higher than 70%. These results encourage the evaluation of alternative protocols for this drug administration, not only for estrogen receptor (ER) positive tumors, but also for ER negative.
微乳剂（MEs）是通过创新的合理开发设计而成，进行了表征，并用于负载高达20 mM的柠檬酸他莫昔芬（TMX）。它们由适用于所有给药途径且特性良好的辅料制成。它们的一些特性，如纳米级平均粒径和较长的稳定保质期，使其成为有趣的药物递送系统。在体外抑制MCF-7乳腺癌细胞中雌二醇诱导的增殖后获得的结果表明对细胞生长有显著影响。在用含有20 mM TMX的MEs孵育后，活细胞数量至少减少了90%。此外，两种负载10 mM药物的组合物显示出高于70%的细胞毒性作用。这些结果鼓励评估这种药物给药的替代方案，不仅适用于雌激素受体（ER）阳性肿瘤，也适用于ER阴性肿瘤。
