Role of the pharmaceutical excipients in the tamoxifen activity on MCF-7 and vero cell cultures.
Role of the pharmaceutical excipients in the tamoxifen activity on MCF-7 and vero cell cultures.
复制标题
DOI：
--
复制
发表时间：
2009-11
影响因子：
2
通讯作者：
T. Rossi;V. Iannuccelli;G. Coppi;E. Bruni;G. Baggio
中科院分区：
文献类型：
--
作者：
T. Rossi;V. Iannuccelli;G. Coppi;E. Bruni;G. Baggio
微粒用于受控药物递送。为了提高三苯氧胺的生物利用度和选择性毒性，研究了海藻酸钙/壳聚糖微球包埋三苯氧胺的活性。材料和方法将单独的他莫昔芬和包埋在用来自Kelco（62%甘露糖醛酸和38%古洛糖醛酸）和来自Fluka（30%甘露糖醛酸和70%古洛糖醛酸）的海藻酸钠制备的微粒中的他莫昔芬加入MCF-7和Vero培养物中，并通过MTT试验评价抗增殖活性。结果使用Kelco或Fluka藻酸盐在Vero和MCF-7培养物上产生不同的LD（50）值，显示出对用包埋在Kelco微粒中的他莫昔芬处理的Vero细胞的更高的细胞毒性（25 μ M对MCF-7细胞的48 μ M），但Fluka微粒对Vero和MCF-7细胞的选择性毒性（分别为25 μ M和10 μ M）。结论：海藻酸钠不同的化学组成可以显著改变药物的活性和毒性，因此，微粒制剂可以提高药物的选择性毒性。
BACKGROUND Microparticles are used for controlled drug delivery. With the aim of improving both bioavailability and tamoxifen selective toxicity, the activity of tamoxifen embedded in calcium alginate/chitosan microparticles was studied. MATERIALS AND METHODS Tamoxifen alone and embedded in microparticles prepared with sodium alginate from Kelco (62% mannuronic acid and 38% guluronic acid) and from Fluka (30% mannuronic acid and 70% guluronic acid) was added to MCF-7 and Vero cultures and evaluated for antiproliferative activity by the MTT test. RESULTS The use of Kelco or Fluka alginate resulted in different LD(50) values on Vero and MCF-7 cultures, showing a higher cytotoxicity toward Vero cells treated with tamoxifen embedded in Kelco microparticles (25 microM vs. 48 microM on MCF-7 cells) but a selective toxicity with Fluka microparticles (25 microM and 10 microM on Vero and MCF-7 cells respectively). CONCLUSION Microparticle formulation may improve selective toxicity according to the alginate employed: differences in the chemical alginate composition can dramatically change both drug activity and toxicity.