Gupta Pranav, Jani Khushboo A, Yang Dong-Hua, Sadoqi Mostafa, Squillante Emilio, Chen Zhe-Sheng
a Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences , St. John's University , Queens , New York , USA.
b Department of Physics, St. John's College of Liberal Arts and Sciences , St. John's University , Queens , New York , USA.
Expert Opin Drug Metab Toxicol. 2016;12(3):281-9. doi: 10.1517/17425255.2016.1145655. Epub 2016 Feb 15.
Drug resistance is the major obstacle impeding the efficacy of chemotherapeutic agents. Although numerous drug delivery techniques have been developed to combat drug resistance, their limitations of non-specific targeting and inconsistent bioavailability has led to the search of novel delivering strategies, such as nanoparticles.
Nanoparticles for anti-cancer drug delivery are microscopic preparations encapsulating a chemotherapeutic and a chemosensitizer into a rationally designed drug delivery vehicle. Nano-strategies directed against multi-drug resistance (MDR) can be categorized into those inhibiting the drug efflux pumps, those effective against the cellular factors of drug resistance, and the combinational based strategies. Here, we review the most recent literature to reposition nanoparticles as chemotherapeutics and inhibitors of MDR.
Novelty in anti-cancer drug delivery has led to the formulation of chemotherapeutics and MDR inhibitors as nano-preparations, which are multi-functional and have better tumor cell-targeting effects. Their characteristics of size and surface attachments make them readily diffusible through the tumor vasculature and increase their retention time as well. With a better understanding of the molecular mechanisms of drug resistance, more potent and multi-targeted nano-preparations can be formulated in the near future.
耐药性是阻碍化疗药物疗效的主要障碍。尽管已经开发了多种药物递送技术来对抗耐药性,但它们非特异性靶向和生物利用度不一致的局限性促使人们寻找新的递送策略,如纳米颗粒。
用于抗癌药物递送的纳米颗粒是将化疗药物和化学增敏剂封装到合理设计的药物递送载体中的微观制剂。针对多药耐药(MDR)的纳米策略可分为抑制药物外排泵的策略、对抗耐药细胞因子的策略以及基于组合的策略。在此,我们回顾最新文献,将纳米颗粒重新定位为化疗药物和MDR抑制剂。
抗癌药物递送的新进展导致将化疗药物和MDR抑制剂制成纳米制剂,这些制剂具有多功能且对肿瘤细胞具有更好的靶向作用。它们的尺寸和表面附着物特性使其易于通过肿瘤脉管系统扩散,并延长其滞留时间。随着对耐药分子机制的更好理解,在不久的将来可以制备出更有效和多靶点的纳米制剂。