Gemcitabine-loaded albumin nanospheres (GEM-ANPs) inhibit PANC-1 cells in vitro and in vivo.
Gemcitabine-loaded albumin nanospheres (GEM-ANPs) inhibit PANC-1 cells in vitro and in vivo.
复制标题
负载吉西他滨的白蛋白纳米球 (GEM-ANP) 在体外和体内抑制 PANC-1 细胞
DOI：
10.1186/1556-276x-8-176
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发表时间：
2013-04-17
影响因子：
--
通讯作者：
Ni Q
中科院分区：
文献类型：
--
作者：
Li J;Di Y;Jin C;Fu D;Yang F;Jiang Y;Yao L;Hao S;Wang X;Subedi S;Ni Q
随着纳米技术的发展，纳米材料在肿瘤治疗中的应用受到了特别的关注。在这里，一种改进的去溶剂化交联方法被成功地应用于制造吉西他滨负载白蛋白纳米球（GEM-ANP），分别具有110和406 nm的平均直径。本研究的目的是评估GEM-ANPs在体内的药物分布、副作用和抗肿瘤活性。代谢活性和流式细胞仪分析表明，两种GEM-ANP，尤其是406 nm GEM-ANP，在体外均能有效抑制人胰腺癌（PANC-1）的代谢和增殖，并促进细胞凋亡。静脉注射406 nm GEM-ANP显示Sprague-Dawley大鼠胰腺、肝脏和脾脏中吉西他滨显著增加（p 0.05）。此外，尽管使用了高剂量（200 mg/kg）的GEM-ANP，但在施用3周后没有观察到通过血液参数变化分析的毒副作用迹象。此外，在PANC-1诱导的肿瘤小鼠中，与游离吉西他滨相比，静脉注射406-nm GEM-ANP也可以有效地减小肿瘤体积。因此，载白蛋白纳米球的方法可能有效地提高吉西他滨的抗肿瘤活性，并且疗效与GEM-ANPs的大小相关。
With the development of nanotechnology, special attention has been given to the nanomaterial application in tumor treatment. Here, a modified desolvation-cross-linking method was successfully applied to fabricate gemcitabine-loaded albumin nanospheres (GEM-ANPs), with 110 and 406 nm of mean diameter, respectively. The aim of this study was to assess the drug distribution, side effects, and antitumor activity of GEM-ANPs in vivo. The metabolic viability and flow cytometry analysis revealed that both GEM-ANPs, especially 406-nm GEM-ANPs, could effectively inhibit the metabolism and proliferation and promote the apoptosis of human pancreatic carcinoma (PANC-1) in vitro. Intravenous injection of 406-nm GEM-ANPs exhibited a significant increase of gemcitabine in the pancreas, liver, and spleen of Sprague–Dawley rats (p 0.05). Moreover, no signs of toxic side effects analyzed by blood parameter changes were observed after 3 weeks of administration although a high dose (200 mg/kg) of GEM-ANPs were used. Additionally, in PANC-1-induced tumor mice, intravenous injection of 406-nm GEM-ANPs also could effectively reduce the tumor volume by comparison with free gemcitabine. With these findings, albumin nanosphere-loading approach might be efficacious to improve the antitumor activity of gemcitabine, and the efficacy is associated with the size of GEM-ANPs.