As a first-line anticancer drug, paclitaxel has shortcomings, such as poor solubility and lack of tumour cell selectivity, which limit its further applications in clinical practice. Therefore, the authors aimed to utilise the characteristics of prodrug and nanotechnology to prepare a reactive oxygen species (ROS) and GSH dual-responsive targeted tumour prodrug nanoparticle Man-PEG-SS-PLGA/ProPTX to improve the clinical application status of paclitaxel limitation. The characterisation of Man-PEG-SS-PLGA/ProPTX was carried out through preparation. The cytotoxicity of nanoparticles on tumour cells and the effect on apoptosis of tumour cells were investigated by cytotoxicity assay and flow cytometry analysis. The ROS responsiveness of nanoparticles was investigated by detecting the ROS level of tumour cells. The tumour cell selectivity of the nanoparticles was further investigated by receptor affinity assay and cell uptake assay. The particle size of Man-PEG-SS-PLGA/ProPTX was (132.90 ± 1.81) nm, the dispersion coefficient Polymer dispersity index was 0.13 ± 0.03, and the Zeta potential was (-8.65 ± 0.50) mV. The encapsulation rate was 95.46 ± 2.31% and the drug load was 13.65 ± 2.31%. The nanoparticles could significantly inhibit the proliferation and promote apoptosis of MCF-7, HepG2, and MDA-MB-231 tumour cells. It has good ROS response characteristics and targeting. The targeted uptake mechanism is energy-dependent and endocytosis is mediated by non-clathrin, non-caveolin, lipid raft/caveolin, and cyclooxygenase (COX)/caveolin with a certain concentration dependence and time dependence. Man-PEG-SS-PLGA/ProPTX is a tumour microenvironment-responsive nanoparticle that can actively target tumour cells. It restricts the release of PTX in normal tissues, enhances its selectivity to tumour cells, and has significant antitumour activity, which is expected to solve the current limitations of PTX use.

中文翻译：

---

一种谷胱甘肽/活性氧双响应、CD206靶向的紫杉醇前药纳米粒，提高抗肿瘤效果。

紫杉醇作为一线抗癌药物，存在溶解度差、缺乏肿瘤细胞选择性等缺点，限制了其在临床的进一步应用。因此，作者旨在利用前药和纳米技术的特点，制备活性氧（ROS）和GSH双重响应的靶向肿瘤前药纳米颗粒Man-PEG-SS-PLGA/ProPTX，以改善紫杉醇局限性的临床应用状况。通过制备对Man-PEG-SS-PLGA/ProPTX进行了表征。通过细胞毒性实验和流式细胞术分析纳米颗粒对肿瘤细胞的细胞毒性以及对肿瘤细胞凋亡的影响。通过检测肿瘤细胞的ROS水平来研究纳米粒子的ROS响应性。通过受体亲和力测定和细胞摄取测定进一步研究了纳米颗粒的肿瘤细胞选择性。Man-PEG-SS-PLGA/ProPTX的粒径为（132.90±1.81）nm，分散系数聚合物分散指数为0.13±0.03，Zeta电位为（-8.65±0.50）mV。包封率为95.46±2.31%，载药量为13.65±2.31%。纳米颗粒可显着抑制MCF-7、HepG2和MDA-MB-231肿瘤细胞的增殖并促进其凋亡。具有良好的ROS响应特性和靶向性。靶向摄取机制是能量依赖性的，内吞作用由非网格蛋白、非小窝蛋白、脂筏/小窝蛋白、环加氧酶（COX）/小窝蛋白介导，具有一定的浓度依赖性和时间依赖性。Man-PEG-SS-PLGA/ProPTX是一种肿瘤微环境响应型纳米颗粒，可以主动靶向肿瘤细胞。它限制PTX在正常组织中的释放，增强其对肿瘤细胞的选择性，具有显着的抗肿瘤活性，有望解决目前PTX使用的局限性。