功能化硼纳米双载药复合物的制备及其体外药物释放  

Preparation and in vitro drug release of functionalized boron dual drug-loaded nanocomposite

作　　者：付梓 张雪静 朱利民[1] FU Zi;ZHANG Xuejing;ZHU Limin(College of Chemistry,Chemical Engineering and Biotechnology,Donghua Universit,Shanghai 201620,China)

机构地区：[1]东华大学化学化工与生物工程学院,上海201620

出　　处：《精细化工》2020年第4期779-784,792,共7页Fine Chemicals

基　　金：上海市科学技术委员会国际资助项目(16410723700);生物医用纺织材料“111工程”中国教育部(B07024)。

摘　　要：通过耦合热氧化蚀刻与液相剥离技术制备了硼纳米片(B NSs),随后用氨基化PEG(H2N-PEG-NH2)对B NSs进行改性制备了改性聚乙二醇化硼纳米片(B-PEG NSs),再以环精氨酸-甘氨酸-天冬氨酸(c RGD)三肽为单体,1-(3-二甲氨基丙基)-3-乙基碳二亚胺盐酸盐(EDC)与N-羟基琥珀酰亚胺(NHS)为引发剂制备了B-PEG-c RGD复合材料。最后,B-PEG-c RGD与阿霉素(DOX)和热休克蛋白90抑制剂17-丙烯胺基-17-去甲氧基格尔德霉素(17AAG)共混得到DOX-17AAG@B-PEG-cRGD纳米载药复合物。采用透射电子显微镜(TEM)、紫外分光光度计及动态光散射仪(DLS)对BNSs和载药复合物的形貌、结构进行了表征。结果表明,功能化硼载药复合物的流体动力学平均直径约为184nm,具有良好的稳定性。体外释药研究表明,DOX-17AAG@B-PEG-cRGD复合物具有近红外光(NIR)和pH双响应性以及良好的药物缓释效果。当体外微环境pH=5.0且存在NIR时,DOX和17AAG在72 h内的累计释放率最高达66.53%和73.01%。Boron nanosheets(B NSs) were prepared by coupling thermal oxidation etching and liquid exfoliation technology. Then, they were modified by H2 N-PEG-NH2 to obtain B-PEG nanosheets(B-PEG NSs). Subsequently, B-PEG-cRGD composite was prepared using cyclic RGD(cRGD) tripeptide as monomer, 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide(EDC) and N-hydroxysuccinimide(NHS) as initiators. Finally, DOX-17 AAG@B-PEG-cRGD nano drug-loaded composite was obtained by blending B-PEGc RGD with doxorubicin(DOX) and heat shock protein 90 inhibitor, 17-allylamin,17-demethoxygeldanamycin(17 AAG). The structure and morphology of B NSs and DOX-17 AAG@B-PEG-cRGD composite were characterized by transmission electron microscopy(TEM), ultraviolet spectrophotometer and dynamic light scattering(DLS). The results show that DOX-17 AAG@B-PEG-cRGD composite has good stability with a hydrodynamic average diameter of about 184 nm. The in vitro drug release studies reveal that the composite has near-infrared light(NIR) and pH double responsiveness, as well as exhibits good drug sustained release effect. When the in vitro drug release experiment was carried out at pH=5.0 and NIR irradiation for 72 h, the cumulative release rates of DOX and 17 AAG were up to 66.53% and 73.01%, respectively.

关 键 词：硼纳米片 近红外光/pH响应 药物缓释 医药原料 

分 类 号：O613.81[理学—无机化学]