Department of Biology, Lakehead University, Thunder Bay, ON, Canada.
Can J Physiol Pharmacol. 2010 Dec;88(12):1172-80. doi: 10.1139/Y10-097.
Paclitaxel is an effective chemotherapeutic agent that is widely used for the treatment of several cancers, including breast, ovarian, and non-small-cell lung cancer. Due to its high lipophilicity, paclitaxel is difficult to administer and requires solubilization with Cremophor EL (polyethoxylated castor oil) and ethanol, which often lead to adverse side effects, including life-threatening anaphylaxis. Incorporation of paclitaxel in dimyristoylphosphatidylcholine:dimyristoylphosphatidylglycerol (DPPC:DMPG) liposomes can facilitate its delivery to cancer cells and eliminate the adverse reactions associated with the Cremophor EL vehicle. Accordingly, the effectiveness of liposomal paclitaxel on MCF-7 breast cancer cells was examined. The results from this study showed that (i) the lipid components of the liposomal formulation were nontoxic, (ii) the cytotoxic effects of liposomal paclitaxel were improved when compared with those seen with conventional paclitaxel, and (iii) the intracellular paclitaxel levels were higher in MCF-7 cells treated with the liposomal paclitaxel formulation. The results of these studies showed that delivery of paclitaxel as a liposomal formulation could be a promising strategy for enhancing its chemotherapeutic effects.
紫杉醇是一种有效的化疗药物，广泛用于治疗多种癌症，包括乳腺癌、卵巢癌和非小细胞肺癌。由于其高亲脂性，紫杉醇难以给药，需要用聚氧乙烯蓖麻油（Cremophor EL）和乙醇溶解，这往往会导致严重的不良反应，包括危及生命的过敏反应。将紫杉醇包封在二肉豆蔻酰磷脂酰胆碱：二肉豆蔻酰磷脂酰甘油（DPPC：DMPG）脂质体中可以促进其递送到癌细胞，并消除与 Cremophor EL 载体相关的不良反应。因此，研究了脂质体紫杉醇对 MCF-7 乳腺癌细胞的作用。研究结果表明：（i）脂质体制剂的脂质成分无毒；（ii）与普通紫杉醇相比，脂质体紫杉醇的细胞毒性作用得到改善；（iii）用脂质体紫杉醇处理的 MCF-7 细胞内紫杉醇水平更高。这些研究结果表明，将紫杉醇制成脂质体制剂可以成为增强其化疗效果的一种有前途的策略。
