Anthracycline drugs on modified surface of quercetin-loaded polymer nanoparticles: a dual drug delivery model for cancer treatment

Polymer nanoparticles are vehicles used for delivery of hydrophobic anti-cancer drugs, like doxorubicin, paclitaxel or chemopreventors like quercetin (Q). The present study deals with the synthesis and characterisation of nano formulations (NFs) from Q loaded PLGA (poly lactic-co-glycolic acid) nano particles (NPs) by surface modification. The surface of Q-loaded (NPs) is modified by coating with biopolymers like bovine serum albumin (BSA) or histones (His). Conventional chemotherapeutic drugs adriamycin (ADR) and mitoxantrone (MTX) are bound to BSA and His respectively before being coated on Q-loaded NPs to nano formulate NF1 and NF2 respectively. The sizes of these NFs are in the range 400-500 nm as ascertained by SEM and DLS measurements. Encapsulation of Q in polymer NPs is confirmed from shifts in FT-IR, TGA and DSC traces of Q-loaded NPs compared to native PLGA and Q. Surface modification in NFs is evidenced by three distinct regions in their TEM images; the core, polymer capsule ...

聚合物纳米颗粒（polymer nanoparticles）是一类递送载体，可用于递送疏水性抗肿瘤药物（如多柔比星、紫杉醇）及槲皮素（Q）等化学预防剂。本研究围绕通过表面修饰技术由负载槲皮素的聚乳酸-羟基乙酸共聚物（poly lactic-co-glycolic acid，PLGA）纳米颗粒（NPs）制备得到的纳米制剂（NFs）的合成与表征展开。负载槲皮素的纳米颗粒表面通过涂布牛血清白蛋白（bovine serum albumin，BSA）或组蛋白（histones，His）等生物聚合物完成修饰。传统化疗药物阿霉素（adriamycin，ADR）与米托蒽醌（mitoxantrone，MTX）分别与牛血清白蛋白、组蛋白结合后，再涂布于负载槲皮素的纳米颗粒表面，分别制备得到纳米制剂NF1与NF2。通过扫描电子显微镜（scanning electron microscope，SEM）与动态光散射（dynamic light scattering，DLS）测试证实，上述纳米制剂的粒径分布在400~500 nm范围内。与纯PLGA及游离槲皮素相比，负载槲皮素的纳米颗粒的傅里叶变换红外光谱（Fourier Transform Infrared Spectroscopy，FT-IR）、热重分析（Thermogravimetric Analysis，TGA）及差示扫描量热法（Differential Scanning Calorimetry，DSC）曲线发生位移，由此证实槲皮素已被包封于聚合物纳米颗粒中。纳米制剂的透射电子显微镜（Transmission Electron Microscopy，TEM）图像中可见三个清晰区域：核心、聚合物囊壳……，由此证实其表面修饰已完成。