A novel ligand-modified nanocomposite microparticles improved efficiency of quercetin and paclitaxel delivery in the non-small cell lung cancer.

IF 6.5 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Xiaoming Cui, Fang Zhang, Yanyan Zhao, Pan Li, Ting Wang, Zhilu Xu, Jingjing Zhang, Weifen Zhang
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引用次数: 4

Abstract

Chemotherapy is the first choice for the treatment of cancer but it is still limited by insufficient kill efficiency and drug resistance. These problems urgently need to be overcome in a way that minimizes damage to the body. In this study, we designed the nanocomposite microparticles (NMPs) modified by cetuximab (Cet) and loaded anti-tumor agents- quercetin (QUE) and paclitaxel (PTX)- for eliciting specific drugs homing and enhancing the killing efficiency of chemotherapy drugs (P/Q@CNMPs). Physicochemical characteristics results presented that P/Q@CNMPs have a suitable aerodynamic diameter and uniform morphology that could meet the requirements of particles deposition in the lung. And it also had the characteristics of sustained-release and pH-responsive which could release the agents in the right place and has a continuous effect. In vitro and in vivo analysis results presented that P/Q@CNMPs have the accuracy targeting ability and killing effect on non-small cell lung cancer (NSCLC) which express positive epidermal growth factor receptor (EGFR) on the membrane. Furthermore, this system also has low toxicity and good biocompatibility. These results demonstrated that P/Q@CNMPs could be a potential intelligent targeting strategy used for chemo-resistant NSCLC therapies.

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一种新型配体修饰的纳米复合微粒提高了槲皮素和紫杉醇在非小细胞肺癌中的递送效率。
化疗是治疗癌症的首选,但仍受杀伤效率不足和耐药的限制。这些问题迫切需要以一种尽量减少对身体损害的方式加以克服。在本研究中,我们设计了西妥昔单抗(Cet)和负载抗肿瘤药物槲皮素(QUE)和紫杉醇(PTX)修饰的纳米复合微粒(NMPs),以诱导特异性药物归巢,提高化疗药物的杀伤效率(P/Q@CNMPs)。理化特性结果表明,P/Q@CNMPs具有合适的气动直径和均匀的形态,能够满足颗粒在肺内沉积的要求。同时具有缓释和ph响应的特点,能在适当的位置释放药物,并具有持续的效果。体外和体内分析结果表明,P/Q@CNMPs对膜上表达表皮生长因子受体(EGFR)阳性的非小细胞肺癌(NSCLC)具有准确的靶向能力和杀伤作用。此外,该系统还具有低毒性和良好的生物相容性。这些结果表明,P/Q@CNMPs可能是用于化疗耐药NSCLC治疗的潜在智能靶向策略。
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来源期刊
Drug Delivery
Drug Delivery 医学-药学
CiteScore
11.80
自引率
5.00%
发文量
250
审稿时长
3.3 months
期刊介绍: Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.
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