Data from: 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 and the coated surface. Negative zeta potential of Q-loaded NPs shifted to positive potential on surface modification in NF1 and NF2. In vitro release of Q from the NFs lasted up to twenty days with an early burst release. NF2 is better formulation than NF1 as loading of MTX is 85% compared to 23% loading of ADR. Such NFs are expected to overcome multi-drug resistance (MDR) by reaching and treating the target cancerous cells by virtue of size, charge and retention.聚合物纳米粒（polymer nanoparticles）是递送疏水性抗癌药物（如多柔比星、紫杉醇）或化学预防剂（如槲皮素(Q)）的载体。本研究针对经表面改性制备的负载槲皮素(Q)的聚乳酸-羟基乙酸共聚物（poly lactic-co-glycolic acid, PLGA）纳米粒（nanoparticles，缩写NPs）所制成的纳米制剂（nano formulations，缩写NFs），开展合成与表征工作。负载Q的纳米粒表面通过包覆牛血清白蛋白(bovine serum albumin, BSA)或组蛋白(histones, His)等生物聚合物完成改性。传统化疗药物阿霉素(adriamycin, ADR)和米托蒽醌(mitoxantrone, MTX)分别与BSA和组蛋白结合，随后包覆于负载Q的纳米粒表面，分别制得纳米制剂NF1与NF2。经扫描电子显微镜(SEM)与动态光散射(DLS)检测证实，上述纳米制剂的粒径介于400~500 nm之间。相较于纯PLGA与游离Q，负载Q的纳米粒的傅里叶变换红外光谱(FT-IR)、热重分析(TGA)与差示扫描量热法(DSC)曲线出现特征位移，由此证实Q已被成功包埋于聚合物纳米粒中。纳米制剂的透射电子显微镜(TEM)图像可观察到三个清晰区域——核芯、聚合物囊壳与包覆层，由此证明其表面改性顺利完成。负载Q的纳米粒原本带负电的ζ电位，在制备得到NF1与NF2后转为正电位。纳米制剂中Q的体外释药过程可持续长达20天，并伴随典型的初期突释效应。NF2的制剂性能优于NF1，因其米托蒽醌负载率达85%，而阿霉素负载率仅为23%。此类纳米制剂可凭借其粒径、表面电荷与实体瘤滞留效应，靶向到达肿瘤细胞并发挥治疗作用，有望克服多药耐药性（multi-drug resistance, 缩写MDR）。