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.

聚合物纳米颗粒（polymer nanoparticles）是用于递送疏水性抗肿瘤药物（如多柔比星、紫杉醇）或槲皮素（Q）等化学预防剂的载体。本研究聚焦于通过表面修饰技术，制备负载槲皮素的聚乳酸-羟基乙酸共聚物（PLGA）纳米颗粒（NPs）基纳米制剂（NFs）并对其进行表征。首先，对负载槲皮素的纳米颗粒表面采用牛血清白蛋白（BSA）或组蛋白（His）等生物聚合物进行包覆修饰。随后分别将常规化疗药物阿霉素（ADR）与米托蒽醌（MTX）结合至BSA与His载体上，再将其包覆于负载槲皮素的纳米颗粒表面，分别得到纳米制剂NF1与NF2。经扫描电子显微镜（SEM）与动态光散射（DLS）检测证实，两种纳米制剂的粒径范围为400~500 nm。对比纯PLGA与游离槲皮素，负载槲皮素的纳米颗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）曲线均出现位移，由此证实槲皮素已被成功包封入聚合物纳米颗粒中。纳米制剂的表面修饰可通过其透射电子显微镜（TEM）图像中的三个清晰区域得到验证：核心、聚合物壳层与包覆表面。负载槲皮素的纳米颗粒原本带有负ζ电位，经表面修饰制备NF1与NF2后，其ζ电位转为正值。两种纳米制剂对槲皮素的体外释放可持续长达20天，且伴随早期突释现象。相较于ADR仅23%的负载率，MTX的负载率可达85%，因此NF2的制剂性能优于NF1。此类纳米制剂有望凭借自身的粒径、电荷特性与滞留效应，靶向到达肿瘤细胞并发挥治疗作用，从而克服多药耐药性（MDR）。