Biodegradable double-targeted PTX-mPEG-PLGA nanoparticles for ultrasound contrast enhanced imaging and antitumor therapy in vitro.
Biodegradable double-targeted PTX-mPEG-PLGA nanoparticles for ultrasound contrast enhanced imaging and antitumor therapy in vitro.
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可生物降解的双靶向 PTX-mPEG-PLGA 纳米粒子用于体外超声对比增强成像和抗肿瘤治疗
DOI：
10.18632/oncotarget.13243
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发表时间：
2016-11-29
期刊：
影响因子：
--
通讯作者：
Du LF
中科院分区：
文献类型：
--
作者：
Ma J;Shen M;Xu CS;Sun Y;Duan YR;Du LF
以单甲氧基聚乙二醇-聚乳酸-羟基乙酸共聚物（mPEG-PLGA）为原料制备多孔纳米超声造影剂（UCA），并分别用抗癌胚抗原（CEA）和抗糖链抗原19-9（CA 19 -9）双靶向抗体进行修饰，制成双靶向纳米粒（NPs）。抗肿瘤药物紫杉醇（PTX）被封装在双靶向纳米颗粒（NPs）中。并对其形态和释放曲线进行了表征。我们通过细胞毒性实验验证了PTX纳米粒具有一定的抗癌作用。细胞摄取结果表明，在体外，超声（US）或超声靶向微泡破坏（UTMD）瞬时声孔作用可以促进更多的NP进入细胞或组织。研究了体外和体内超声造影图像。与SonoVue相比，纳米粒在兔肾脏和裸鼠肿瘤中的成像时间延长，这使得纳米粒在肿瘤区域的保留时间延长，从而进一步增强抗肿瘤作用成为可能。具有超声造影和抗肿瘤双重靶向功能的新型纳米粒有望成为临床应用的新途径。
A porous-structure nano-scale ultrasound contrast agent (UCA) was made of monomethoxypoly (ethylene glycol)-poly (lactic-co-glycolic acid) (mPEG-PLGA), and modified by double-targeted antibody: anti-carcinoembryonic antigen (CEA) and anti-carbohydrate antigen 19-9 (CA19-9), as a double-targeted nanoparticles (NPs). Anti-tumor drug paclitaxel (PTX) was encapsulated in the double-targeted nanoparticles (NPs). The morphor and release curve were characterized. We verified a certain anticancer effect of PTX-NPs through cytotoxicity experiments. The cell uptake result showed much more NPs may be facilitated to ingress the cells or tissues with ultrasound (US) or ultrasound targeted microbubble destruction (UTMD) transient sonoporation in vitro. Ultrasound contrast-enhanced images in vitro and in vivo were investigated. Compared with SonoVue, the NPs prolonged imaging time in rabbit kidneys and tumor of nude mice, which make it possible to further enhance anti-tumor effects by extending retention time in the tumor region. The novel double-targeted NPs with the function of ultrasound contrast enhanced imaging and anti-tumor therapy can be a promising way in clinic.