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载鬼臼毒素的硬脂酸-γ-壳寡糖聚合物胶束的体外抗肿瘤活性。

In vitro antitumour activity of stearic acid-g-chitosan oligosaccharide polymeric micelles loading podophyllotoxin.

机构信息

Department of Pharmacy, School of Medicine Science, Jiaxing University, Jiaxing, Zhejiang, China.

出版信息

J Microencapsul. 2012;29(1):1-8. doi: 10.3109/02652048.2011.621551. Epub 2012 Jan 9.

DOI:10.3109/02652048.2011.621551
PMID:22229874
Abstract

Development of successful formulations for poorly water-soluble drugs remains a longstanding critical and challenging issue in cancer therapy. The stearic acid-g-chitosan oligosaccharide (CSO-SA) micelles have been presented as potential candidates for intracellular antitumour agent delivery carrier. Herein, podophyllotoxin (PPT) loaded CSO-SA micelles (CSO-SA/PPT) were prepared by a dialysis method. The drug encapsulation efficiency could reach a higher level, the micellar size and the zeta potential increased with increasing charged amounts of drug. The cumulative release percentage of PPT drug from micelles enhanced with decreasing PPT content in the micelles. The cytotoxicities of CSO-SA/PPT micelles against human breast carcinoma (MCF-7) cells, human lung cancer cells (A549) and human hepatoma cell line (Bel-7402) were higher than that of free PPT formulation. The higher cytotoxicities were due to the faster PPT transport into tumour cells mediated by CSO-SA micelles. Overall, CSO-SA micelles might be a promising carrier for PPT delivery in cancer therapy.

摘要

开发水溶性差的药物的成功制剂仍然是癌症治疗中长期存在的关键和具有挑战性的问题。硬脂酸-g-壳聚糖寡糖（CSO-SA）胶束已被提出作为细胞内抗肿瘤药物输送载体的潜在候选物。本文通过透析法制备了负载鬼臼毒素（PPT）的 CSO-SA 胶束（CSO-SA/PPT）。药物包封效率可以达到更高的水平，随着药物荷电量的增加，胶束的粒径和zeta 电位增加。从胶束中释放的 PPT 药物的累积百分比随着胶束中 PPT 含量的降低而增加。CSO-SA/PPT 胶束对人乳腺癌（MCF-7）细胞、人肺癌细胞（A549）和人肝癌细胞系（Bel-7402）的细胞毒性高于游离 PPT 制剂。更高的细胞毒性是由于 CSO-SA 胶束介导的 PPT 更快地进入肿瘤细胞。总的来说，CSO-SA 胶束可能是癌症治疗中 PPT 递送的一种有前途的载体。

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