Xu Shi, Xu Qian, Zhou Jiahua, Wang Junying, Zhang Niping, Zhang Ling
Key Laboratory of Environmental Medicine and Engineering, Ministry of Education, Southeast University, Nanjing, 210009, China.
J Nanosci Nanotechnol. 2013 Jan;13(1):129-38. doi: 10.1166/jnn.2013.6794.
For the purpose of achieving targeted chemotherapy of pancreatic cancer, we prepared core-shell nanoparticles by coaxial electrospray technology, with folate-chitosan as the polymeric coating material and gemcitabine as the encapsulated drug. The effects of various solution properties and processing parameters on nanoparticles formation were investigated. By optimizing the electrospray parameters, the diameter of the core-shell nanoparticles was in the range of 200-300 nm with drug loading and encapsulation efficiency of 3.91 +/- 0.12% and 85.37 +/- 4.9%. The drug release kinetics revealed a controlled initial burst release followed by a sustained release over a period of 72 h at pH 7.4 and pH 5.0, and at pH 5.0 the drug released more quickly. Moreover, the cellular uptake experiment confirmed that the folate conjugated core-shell nanoparticles had high pancreatic cancer (BXPC3) cells uptake efficiency. And the cell cytotoxicity test displayed that they had remarkable cytotoxicity towards BXPC3 cells. This study indicates that coaxial electrospray is a facile technique in producing core-shell nanoparticles encapsulating hydrophilic small molecule drugs, and clearly infers that the folate conjugated core-shell nanoparticles is very much effective to use as a pancreatic tumor-targeted delivery carrier for anticancer drugs.
为实现胰腺癌的靶向化疗，我们采用同轴电喷雾技术制备了核壳纳米颗粒，以叶酸-壳聚糖作为聚合物包覆材料，吉西他滨作为包封药物。研究了各种溶液性质和加工参数对纳米颗粒形成的影响。通过优化电喷雾参数，核壳纳米颗粒的直径在200-300nm范围内，载药量和包封率分别为3.91±0.12%和85.37±4.9%。药物释放动力学表明，在pH 7.4和pH 5.0条件下，药物初始呈现可控的突释，随后在72小时内持续释放，且在pH 5.0时药物释放更快。此外，细胞摄取实验证实，叶酸偶联的核壳纳米颗粒对胰腺癌（BXPC3）细胞具有较高的摄取效率。细胞毒性试验表明，它们对BXPC3细胞具有显著的细胞毒性。本研究表明，同轴电喷雾是一种制备包封亲水性小分子药物的核壳纳米颗粒的简便技术，并且明确推断叶酸偶联的核壳纳米颗粒作为抗癌药物的胰腺肿瘤靶向递送载体非常有效。
