载顺铂、唾液酸 Lewis X 修饰的脂质体：药物释放、生物分布及抗肿瘤疗效
Cisplatin-loaded, Sialyl Lewis X-Modified Liposomes: Drug Release, Biodistribution and Antitumor Efficacy.
作者信息
Kishimoto Shuichi, Fujitani Nobuhito, Ohnishi Takanori, Aoki Hiroki, Suzuki Ryosuke, Fukushima Shoji
机构信息
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Kobe, Japan.
出版信息
Anticancer Res. 2017 Nov;37(11):6055-6061. doi: 10.21873/anticanres.12053.
BACKGROUND/AIM: The aim of this study was to evaluate the characteristics of two cisplatin (CDDP)-loaded, sialyl Lewis X-modified liposomes (CDDP-SLX-LIP) with different particle size. Each had the same lipid composition and CDDP concentration, but a different drug-to-lipid ratio.
MATERIALS AND METHODS
The amount of platinum in the filtrates was determined by the ICP method. The antitumor effect was assessed using rats bearing MRMT-1 tumor.
RESULTS
CDDP release was faster from the larger liposome formulation (L-LIP) than from the smaller one (S-LIP). Treatment with the two CDDP-SLX-LIPs resulted in comparable antitumor effects without obvious side-effects, but treatment with CDDP solution resulted in significant weight loss and an elevated BUN. Tumor accumulation of CDDP-SLX-LIP was clearly greater than that of CDDP solution and accumulation of S-LIP was greater than that of L-LIP.
CONCLUSION
CDDP-SLX-LIP exhibited antitumor effects depending on their release behavior and tumor accumulation.
背景/目的：本研究旨在评估两种载有顺铂（CDDP）的、唾液酸化路易斯X修饰的脂质体（CDDP-SLX-LIP）的特性，这两种脂质体粒径不同。每种脂质体具有相同的脂质组成和CDDP浓度，但药物与脂质的比例不同。
材料与方法
采用电感耦合等离子体质谱法测定滤液中的铂含量。使用荷MRMT-1肿瘤的大鼠评估抗肿瘤效果。
结果
较大脂质体制剂（L-LIP）中CDDP的释放速度比较小脂质体制剂（S-LIP）更快。两种CDDP-SLX-LIP治疗产生了相当的抗肿瘤效果，且无明显副作用，但CDDP溶液治疗导致大鼠体重显著减轻和血尿素氮升高。CDDP-SLX-LIP在肿瘤中的蓄积明显大于CDDP溶液，且S-LIP的蓄积大于L-LIP。
结论
CDDP-SLX-LIP根据其释放行为和肿瘤蓄积表现出抗肿瘤作用。
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