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題 名 | Use of Cremophor EL as a MDR Reversing Agent to Enhance Intestinal Absorption of Epirubicin in Everted Gut Sacs of Rats and Human Intestinal Epithelial Caco-2 Cell Layers=使用Cremophor EL為多重抗藥性抑制劑以促進Epirubicin於老鼠小腸及人類結腸腺癌細胞之吸收 |
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作 者 | 駱雨利; 許立人; 宋家玲; 蔡宜芳; 陳嘉銘; 吳東和; | 書刊名 | 嘉南學報 |
卷 期 | 24 1998.11[民87.11] |
頁 次 | 頁142-149 |
分類號 | 418.2216 |
關鍵詞 | P醣蛋白; 老鼠小腸; 結腸腺癌細胞; P-glycoprotein; Epirubicin; Cremophor EL; Everted gut sacs; Caco-2; |
語 文 | 英文(English) |
中文摘要 | P醣蛋白可排出許多抗癌藥物,因而降低抗癌藥物例如 Epirubicin 之療效。如能 使用多重抗藥性抑制劑抑制小腸 P 醣蛋白之功能, 將有助於促進 Epirubicin 之生體可 用率。 Cremophor EL 為一無藥理活性之界面活性劑,具有無全身性副作用之優點。我們之 前使用流式細胞分析儀分析,發現 Cremophor EL 明顯增進 Epirubicin 於 Caco-2 癌細胞 之積聚。 因此在這篇研究中,我們使用老鼠小腸及人類結腸腺癌細胞以評估 Crempohor EL 是否可促進 Epirubicin 於小腸之吸收。 以人類結腸腺癌細胞為模型,發現 Cremophor EL 可促進 Epirubicin 於吸收方向之運輸及減少 Epirubicin 於排出方向之運輸。總結,實驗 結果顯示 Cremophor EL 為有效之多重抗藥性抑制劑,能以體內試驗可用之濃度以促進抗癌 藥物 Epirubicin 於老鼠小腸之吸收及結腸腺癌細胞之運輸。使用 Cremophor EL 於賦形劑 中可以經由抑制 P 醣蛋白之機轉以促進藥物之小腸吸收,並增進 P 醣蛋白受質之生體可用 率。 |
英文摘要 | P-glycoprotein (P-gp) actively pumps out a number of anticncer drugs, such as epirubicin, from tumor cells. P-gp also expresses in the small intestine at normal physiological conditions. Inhibition of intestinal P-gp function using MDR reversing agents may enhance oral bioavailability of some chemotherapeutic agents. Cremophor EL is a pharmacologically inert surfactant and has the advantage of no systemic side effect. Our previous flow cytometric study showed that Cremophor EL might have MDR reversing effects and increased the intracellular accumulation of epirubicin in Caco-2 cells. In this study, the effect of Cremophor EL as a MDR reversing agent on the enhancement of intestinal absorption of epirubicin was investigated in both everted gut sacs of rats and human intestinal epithelial Caco-2 cell layers. The epirubicin concentrations measured in everted gut sacs pretreated with cremophor EL were signigicantly higher than those in epirubicin control for both the jejunum and the ileum. The addition of Cremophor EL significantly increased apical-to-basolateral permeability and reduced basolateral-to-apical permeability of epirubicin across Caco-2 cells. In conclusion, our results demonstrate that Cremophor EL is a potent MDR modifier of epirubicin in both human colon adenocarcinoma cells and everted gut sacs of rats at concentration that could be achieved in vivo. Use of Cremophor EL as excipient may increase intestinal absorption of some drugs through the mechanism of P-gp inhibition and thus improve drug bioavaiability for P-gp substrates. |
本系統中英文摘要資訊取自各篇刊載內容。