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題 名 | Use of Phospholipids to Enhance the Intestinal Absorption of Epirubicin=使用磷脂質於劑型中以促進Epirubicin之小腸吸收 |
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作 者 | 駱雨利; | 書刊名 | 嘉南學報 |
卷 期 | 25 1999.11[民88.11] |
頁 次 | 頁139-146 |
分類號 | 418.2216 |
關鍵詞 | 磷脂質; 微脂粒; 結腸腺癌細胞; P醣蛋白; 多重抗藥性; Epirubicin; Phospholipids; Liposomes; Caco-2; P-glycoprotein; Multidrug resistance; |
語 文 | 英文(English) |
中文摘要 | 磷脂質常被用來當作藥物之攜帶體。抗癌藥物若以磷脂質做成之微脂粒包裝,常 可降低毒性、增加療效。因此我們研究微脂粒包埋、空的微脂粒或磷脂質對於EPirubicin 於人類結腸腺癌細胞(Caco-2)之積聚及運送之效應。使用流式細胞分析儀分析,發現微脂粒 包埋或空的微脂粒明顯增進Epirubicin於Caco-2細胞之積聚。以Caco-2細胞為模型,發現 微脂粒包埋或空的微脂粒可顯著促進Epirubicin於吸收方向之運輸及明顯減少Epirubicin 於排出方向之運輸。實驗結果顯示抑制小腸P醣蛋白或其他排出藥物之蛋白質可能跟 Epirubicin之增加吸收及減少排出有關。總結,使用磷脂質做成藥物之微脂粒劑型可以經由 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。微脂粒包 裝可應用於拮抗癌症化學療法上之多重抗藥性。 |
英文摘要 | Studies using cancer chemotherapeutic agents such as epirubicin encapsulated in liposomes, made of phospholipids and other Ingredients, have generally shown reduced toxicity and enhanced therapeutic efficacy. This study investigated the effects of liposomal encapsulation, empty liposome or free lipid addition on the uptake and transport of epirubicin in the human colon adenocar-cinoma (Caco-2) cell line. The flow cytometric experiments showed that liposomal encapsulation or empty liposome addition significantly increased the intracellular accumulation of epirubicin in Caco-2 cells. Use of liposomes, made of dipalmitoyl phosphatidyicholine (DPPC), substantially enhanced apical to basolateral absorption of epirubicin across Caco-2 monolayers. Furthermore, except free DPPC addition, epirubicin encapsulated in DPPC liposomes or empty DPPC liposome addition significantly reduced the basolateral to apical effiux of epirubicin across Caco-2 monolayers. The study suggests that inhibition or P-gp or other transporter proteins located in the intestines may be, at least partially, involved in the reduction of epirubicin ef flux. In conclusion, the therapeutic efficacy or epirubicin may be improved by the use or phospholipids as excipients and MDR modulators in the formulations. Liposomal encapsulation may have significant impilcations to circumvent drug resistance in cancer chemotherapy. |
本系統中英文摘要資訊取自各篇刊載內容。