Development of nonionic sulfactant/phospholipid o/w emulsion as a paclitaxel delivery system
Development of nonionic sulfactant/phospholipid o/w emulsion as a paclitaxel delivery system
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DOI：
10.1016/s0168-3659(98)00164-3
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发表时间：
1999-04-19
影响因子：
10.8
通讯作者：
Chu, IM
中科院分区：
文献类型：
--
作者：
Kan, P;Chen, ZB;Chu, IM
紫杉醇是一种低水溶性的抗癌剂。由于缺乏适当的递送工具，这种药物的更广泛的临床应用在一定程度上延迟了。在混合乳化剂体系稳定的三酰基甘油中掺入紫杉醇，尝试采用0 /w乳液作为药物载体。本研究找到了合适的配方：紫杉醇0.75 mg/ml, 10% （w/v）混合油，4% (w/v) EPC, 3% (w/v) Tween 80在2.25% （w/v）甘油溶液中。配制的乳状液在4℃条件下贮存时具有很好的稳定性，紫杉醇包封率可保持在95%以上，乳状液平均直径可保持在150 nm左右至少3个月。紫杉醇乳剂在30 nM处对HeLa细胞具有IC50的细胞毒性。紫杉醇乳剂能显著延长腹水荷瘤小鼠的平均寿命（P < 0.05）。该乳液是紫杉醇等亲脂性药物的理想载体。(C) 1999 Elsevier Science B.V.版权所有
Paclitaxel is an anticancer agent with low aqueous solubility. More extensive clinical use of this drug is somewhat delayed due to lack of appropriate delivery vehicles. An attempt was made to adopt an o/w emulsion as the drug carrier which incorporated paclitaxel in the triacylglycerol stabilized by a mixed-emulsifier system. A suitable formulation was found in this study: 0.75 mg/ml paclitaxel, 10% (w/v) oil blend, 4% (w/v) EPC, 3% (w/v) Tween 80 in 2.25% (w/v) glycerol solution. The formulated emulsion has very good stability when stored at 4 degrees C, and the paclitaxel containment efficiency can be maintained above 95% and the mean emulsion diameter around 150 nm for at least 3 months. Paclitaxel-emulsion displayed cytotoxicity against HeLa cells with IC50 at 30 nM. The average life span of ascitic-tumor-bearing mice was prolonged significantly by the treatment of paclitaxel-emulsion (P < 0.05). The formulated emulsion is a promising carrier for paclitaxel and other lipophilic drugs. (C) 1999 Elsevier Science B.V. All rights reserved.