PEG化羟基磷灰石纳米体系的制备及双通道荧光成像  

Synthesis of PEGylation hydroxyapatite drug delivery system and its dual channels fluorescence imaging

作　　者：李晓静 孙文 康垚 樊江莉[1] 彭孝军[1] LI Xiaojing;SUN Wen;KANG Yao;FAN Jiangli;PENG Xiaojun(State Key Laboratory of Fine Chemicals,Dalian University of Technology,Dalian 116024,Liaoning,China)

机构地区：[1]大连理工大学精细化工国家重点实验室,辽宁大连116024

出　　处：《化工学报》2020年第10期4808-4819,共12页CIESC Journal

基　　金：国家自然科学基金项目(21925802,21878039)。

摘　　要：PEG化的药物递送系统(DDSs)可以通过增强药物的渗透性和滞留性(EPR)效应克服传统化疗的副作用。利用共沉淀法和水热法制备纳米粒子DOX@HAP,进一步通过偶联反应修饰菁染料(Cy),通过铜(I)催化的炔-叠氮化物环加成反应修饰PEG链,构建了纳米制剂DOX@HAP-Cy-PEG。通过透射电子显微镜(TEM)、扫描电子显微镜(SEM)、粒度分析仪、傅里叶红外光谱仪(FTIR)、X射线光电子能谱仪(XPS)和X射线衍射仪(XRD)对该纳米载药体系的形貌、粒径、物相组成进行表征分析。利用紫外-可见(UV-Vis)分光光度法测定了该纳米材料的药物负载量以及体外药物释放曲线。进一步,利用DOX和Cy双通道荧光成像,监测DDSs在Hela和HepG2细胞中的摄取行为。表明DOX@HAP-Cy-PEG纳米载药体系有望作为一种新型的治疗与示踪一体化的抗癌纳米制剂。PEGylated drug delivery systems(DDSs)can overcome the side effects of traditional chemotherapy by enhancing drug permeability and retention(EPR)effects.In this work,DOX@HAP(hydroxyapatite)was initially fabricated via the coprecipitation and hydrothermal method,further functionalized with Cy(cyanine)by coupling reaction of APTES and then introduced hydrophilic PEG chains by using copper(I)-catalyzed alkyne–azide cycloaddition reaction.Physicochemical properties including the morphology,particle size and phase composition,were characterized by TEM,SEM,particle size analyzer,FTIR,XPS and XRD.The encapsulation efficiency and drug release profile of DOX@HAP-Cy-PEG were analyzed by UV-Vis spectrophotometry.Furthermore,the cellular uptake of DOX@HAP-Cy-PEG nanoparticles in Hela and HepG2 cells was monitored by the dual channels fluorescence imaging of DOX and Cy.The results showed that DOX@HAP-Cy-PEG nanoparticles could be used to real-time monitor the dynamic distribution of DDSs in Hela and HepG2 cells by dual channels.

关 键 词：羟基磷灰石 载药体系 菁染料 双通道 荧光成像 

分 类 号：TQ34[化学工程—化纤工业]