新型树状大分子-多烯紫杉醇纳米粒的制备、表征及体外细胞毒作用

发布时间：2019-04-22 09:39

【摘要】：目的新型树状大分子(PAMAM-co-0.25OEG,PGD)作稳定剂制备多烯紫杉醇(Docetaxel,DTX)纳米粒,以提高多烯紫杉醇的溶解度和生物利用度。方法将多烯紫杉醇(DTX)、PGD按药载比8:1,采用超声沉淀联合高压均质法制备DTX-PGD纳米粒,动态光散射测定载药纳米粒粒径及电位;考察37℃条件下,DTX-PGD纳米粒在生理盐水、5%葡萄糖、PBS及血浆中的稳定性及DTX-PGD纳米粒的溶血性。X射线粉末衍射法测定DTX在纳米粒中的晶型形式。透析法测定DTX-PGD纳米粒的体外释放度,MTT法检测DTX-PGD纳米粒对4T1细胞的杀伤作用。结果多烯紫杉醇在水中的溶解度提高到1.6 mg/m L(原药在水中几乎不溶),纳米粒载药量达65.7%。DTX-PGD纳米粒粒径270.7 nm,PDI值为0.112,电位28.6 m V。DTX-PGD纳米粒在5%葡萄糖及血浆中稳定存在。扫描电镜观察纳米粒为片状,XRD图谱显示,多烯紫杉醇在纳米粒中以晶体形式存在。DTX-PGD纳米粒在PBS缓冲液中释放缓慢,有较好的缓释效果。溶血实验得知,DTX-PGD纳米粒无溶血现象,可采用静脉注射法给药。MTT结果表明,DTX-PGD纳米粒对4T1细胞较多烯紫杉醇溶液具有更强的杀伤作用。结论 PGD树状大分子可以作为一种有效的稳定剂应用到多烯紫杉醇纳米粒的制备中,DTX-PGD纳米粒有望作为一种新型的药物输送系统应用到癌症的临床治疗中。
[Abstract]:Aim to prepare docetaxel (Docetaxel,DTX) nanoparticles by using new dendrimer (PAMAM-co-0.25OEG,PGD) as stabilizer in order to improve the solubility and bioavailability of docetaxel. Methods DTX-PGD nanoparticles were prepared by ultrasonic precipitation combined with high pressure homogenization with docetaxel (DTX), PGD at a drug loading ratio of 8 渭 1. The particle size and potential of drug-loaded nanoparticles were measured by dynamic light scattering (DLS). The stability of DTX-PGD nanoparticles in normal saline, 5% glucose, PBS and plasma and the hemolysis of DTX-PGD nanoparticles were investigated at 37 鈩，

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