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利用聚合物胶束的多功能方法来规避多药耐药肿瘤。

Multifunctional approaches utilizing polymeric micelles to circumvent multidrug resistant tumors.

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy & Allied Health Professions, South Dakota State University, Brookings, SD, 57007, USA.

Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), S.A.S. Nagar, Sector 67, Mohali, Punjab, 160062, India.

出版信息

Colloids Surf B Biointerfaces. 2019 Jan 1;173:581-590. doi: 10.1016/j.colsurfb.2018.10.022. Epub 2018 Oct 10.

Abstract

The concerns impeding the success of chemotherapy in cancer is descending efficacy of drugs due to the development of multiple drug resistance (MDR). The current efforts employed to overcome MDR have failed or are limited to only preliminary in-vitro investigations. Nanotechnology is at the forefront of the drug delivery research, playing pivotal role in chemotherapy and diagnosis, thereby providing innovative approaches for the management of the disease with minimal side effects. Recently, polymeric micelles (PMs) have witnessed significant developments in cancer therapy. PMs are self-assembled colloidal particles, with a hydrophilic head and a long hydrophobic tail, which enhance the solubility, permeability and bioavailability of drugs, due to the unique features of reaching higher concentration in the biological system, above critical micellar concentration. One of the effective approaches to improve the efficacy of chemotherapy and overcome drug resistance would be to employ multifunctional approach (combination of stimuli-responsive, utilization of drug resistance modulators and combination therapy) using PMs as drug delivery systems. Actively targeted, stimuli-sensitive and multifunctional approaches involve using single and/or combination of approaches (pH-responsive, temperature regulated, reduction-sensitive, ultrasound etc.) to combat drug resistant. The review will describe PMs, types of copolymers used in PMs, preparation and characterization of PMs. A comprehensive list of PMs tested in clinical trials is discussed. Lastly, this review covers stimuli-sensitive and multifunctional approaches to overcome MDR in cancer utilizing PMs.

摘要

阻碍癌症化疗成功的问题是由于多药耐药性(MDR)的发展,药物的疗效下降。目前克服 MDR 的努力要么失败,要么仅限于初步的体外研究。纳米技术处于药物输送研究的前沿,在化疗和诊断中发挥着关键作用,从而为最小化副作用的疾病管理提供了创新方法。最近,聚合物胶束(PMs)在癌症治疗方面取得了重大进展。PMs 是自组装胶体颗粒,具有亲水头部和长疏水尾部,由于在生物系统中达到更高浓度的独特特性,超过临界胶束浓度,从而提高了药物的溶解度、渗透性和生物利用度。提高化疗疗效和克服耐药性的有效方法之一是使用 PMs 作为药物输送系统,采用多功能方法(刺激响应组合、利用耐药调节剂和联合治疗)。主动靶向、刺激敏感和多功能方法涉及使用单一和/或组合方法(pH 响应、温度调节、还原敏感、超声等)来对抗耐药性。本综述将描述 PMs、PMs 中使用的共聚物类型、PMs 的制备和表征。讨论了在临床试验中测试的 PMs 的综合清单。最后,本综述涵盖了利用 PMs 克服癌症 MDR 的刺激敏感和多功能方法。

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