pH氧化还原双智能响应灵芝多糖-药物偶联物递送系统

纳米粒子作为抗癌药物的载体已被广泛研究，但设计和制备用于精确控制药物释放的智能药物释放系统仍然是一项重大挑战。在此，首次提出了一种新型的基于灵芝多糖（GLP）的芦丁羧基苯基硼酸（CPBA）-GLP-二硫代二丙酸（DPA）-双氢青蒿素（DHA）/10-羟基喜树碱（HCPT）聚合物偶联物纳米颗粒（RCGDDH-NPs），其具有pH和氧化还原双重响应性。RCGDDH NP中装载的三种药物可以通过程序释放：芦丁在酸性微环境的肿瘤组织中释放，DHA和HCPT在肿瘤细胞的氧化还原环境中释放。有趣的是，GLP作为载体，具有抗癌活性，可以增强抗癌活性。制备的RCGDDH NP的尺寸约为98nm。体外释放研究表明，在pH 5.2和10mM还原性谷胱甘肽的条件下纳米颗粒比正常生理状态高2.5倍和2.7倍。此外，纳米颗粒中的芦丁可以在微酸条件下释放，并对基质有明显的抑制作用金属蛋白酶MMP-9。此外，体外和体内实验表明，制备的RCGDDH NP可以有效地杀死肿瘤细胞，抑制肿瘤生长并引起低副作用。主要记录了灵芝多糖-芦丁-双氢青蒿素偶联物的制备、红外光谱、核磁共振，药物释放动力学、智能响应释放、细胞毒性、小鼠动物实验等

Nanoparticles as carriers for anticancer drugs have been extensively investigated, but designing and fabricating intelligent drug delivery systems (DDS) for precise spatiotemporal control of drug release remains a formidable challenge. Herein, we report for the first time a novel rutin-carboxyphenylboronic acid (CPBA)-GLP-dithiodipropionic acid (DPA)-dihydroartemisinin (DHA)/10-hydroxycamptothecin (HCPT) polymer conjugate nanoparticle (RCGDDH-NPs) based on Ganoderma lucidum polysaccharide (GLP), which features dual pH and redox responsiveness. The three drugs loaded in RCGDDH-NPs can be released in a programmed manner: rutin is released in the acidic microenvironment of tumor tissues, while DHA and HCPT are released in the redox environment of tumor cells. Interestingly, GLP as the carrier itself possesses anticancer activity, which can further enhance the overall anticancer efficacy. The as-prepared RCGDDH-NPs have a mean size of approximately 98 nm. In vitro release studies show that the drug release from the nanoparticles under the conditions of pH 5.2 and 10 mM reduced glutathione (GSH) is 2.5-fold and 2.7-fold higher than that under normal physiological states, respectively. Additionally, rutin released from the nanoparticles under slightly acidic conditions can significantly inhibit matrix metalloproteinase-9 (MMP-9). Furthermore, in vitro and in vivo experiments demonstrate that the as-prepared RCGDDH-NPs can effectively kill tumor cells, suppress tumor growth, and induce minimal systemic side effects. This dataset mainly records the preparation, Fourier-transform infrared spectroscopy (FTIR) characterization, nuclear magnetic resonance (NMR) analysis, drug release kinetics, stimuli-responsive release, cytotoxicity assays, and mouse animal experiments of the GLP-rutin-dihydroartemisinin conjugate and related systems.

搜集汇总

背景与挑战

背景概述

该数据集聚焦于一种新型的pH和氧化还原双智能响应灵芝多糖-药物偶联物递送系统（RCGDDH-NPs），用于抗癌药物的精确控制释放。数据集记录了该系统的制备、药物释放动力学、智能响应特性以及体外和体内实验，展示了其在高效杀死肿瘤细胞、抑制肿瘤生长并降低副作用方面的潜力。