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用于将紫杉醇递送至人肺癌A549细胞的载药壳聚糖空心纳米颗粒的研制。

Development of drug-loaded chitosan hollow nanoparticles for delivery of paclitaxel to human lung cancer A549 cells.

作者信息

Jiang Jie, Liu Ying, Wu Chao, Qiu Yang, Xu Xiaoyan, Lv Huiling, Bai Andi, Liu Xuan

机构信息

a Pharmacy School, Jinzhou Medical University , Jinzhou , PR China.

出版信息

Drug Dev Ind Pharm. 2017 Aug;43(8):1304-1313. doi: 10.1080/03639045.2017.1318895. Epub 2017 Apr 27.

Abstract

In this study, biodegradable chitosan hollow nanospheres (CHN) were fabricated using polystyrene nanospheres (PS) as templates. CHN were applied to increase the solubility of poorly water-soluble drugs. The lung cancer drug paclitaxel (PTX), which is used as a model drug, was loaded into CHN by the adsorption equilibrium method. The drug-loaded sample (PTX-CHN) offered sustained PTX release and good bioavailability. The state characterization of PTX by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) showed that the PTX absorbed into CHN existed in an amorphous state. An in vitro toxicity experiment indicated that CHN were nontoxic as carriers of poorly water-soluble drugs. The PTX-CHN produced a marked inhibition of lung cancer A549 cells proliferation and encouraged apoptosis. A cell uptake experiment indicated that PTX-CHN was successfully taken up by lung cancer A549 cells. Furthermore, a degradation experiment revealed that CHN were readily biodegradable. These findings state clearly that CHN can be regarded as promising biomaterials for lung cancer treatment.

摘要

在本研究中,以聚苯乙烯纳米球(PS)为模板制备了可生物降解的壳聚糖中空纳米球(CHN)。CHN用于提高难溶性药物的溶解度。将肺癌药物紫杉醇(PTX)作为模型药物,通过吸附平衡法载入CHN。载药样品(PTX-CHN)实现了PTX的持续释放并具有良好的生物利用度。通过差示扫描量热法(DSC)、X射线衍射(XRD)和傅里叶变换红外光谱(FTIR)对PTX进行的状态表征表明,吸附到CHN中的PTX以无定形状态存在。体外毒性实验表明,CHN作为难溶性药物的载体无毒。PTX-CHN对肺癌A549细胞的增殖产生了显著抑制并促进了细胞凋亡。细胞摄取实验表明,PTX-CHN被肺癌A549细胞成功摄取。此外,降解实验表明CHN易于生物降解。这些发现清楚地表明,CHN可被视为用于肺癌治疗的有前景的生物材料。

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