Department of Pharmaceutics and Pharmaceutical Technology, College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates.
Research and Innovation Department, Lincoln University College, Petaling Jaya 47301, Selangor, Malaysia.
Curr Pharm Des. 2021;27(43):4356-4375. doi: 10.2174/1381612827666210830092539.
Breast cancer (BC) is one of the most aggressive and prevalent types of cancer, which is associated with a high rate of mortality and colossal potential of metastasis to other body organs. Conventionally, there are three commonly employed strategies for the treatment of BC including, surgery, radiations and chemotherapy; however, these modalities are associated with several deleterious effects and a high rate of relapse.
This review was aimed to critically discuss and conceptualize existing evidences related to the pharmaceutical significance and therapeutic feasibility of multi-functionalization of nanomedicines for early diagnosis and efficient treatment of BC.
Though the implication of nanotechnology-based modalities has revolutionised the outcomes of diagnosis and treatment of BC; however, the clinical translation of these nanomedicines is facing grandeur challenges. These challenges include recognition by the reticuloendothelial system (RES), short plasma half-life, non-specific accumulation in the non-cancerous cells, and expulsion of the drug(s) by the efflux pump. To circumvent these challenges, various adaptations such as PEGylation, conjugation of targeting ligand(s), and siteresponsive behaviour (i.e., pH-responsiveness, biochemical, or thermal-responsiveness) have been adapted. Similarly, multi-functionalization of nanomedicines has emerged as an exceptional strategy to improve the pharmacokinetic profile, specific targetability to the tumor microenvironment (active targeting) and efficient internalization, and to alleviate the expulsion of internalized drug contents by silencing-off efflux pump.
Critical analysis of the available evidences revealed that multi-functionalization of nanomedicines is a plausible and sustainable adaptation for early diagnosis and treatment of BC with better therapeutic outcomes.
乳腺癌（BC）是最具侵袭性和普遍性的癌症之一，其死亡率高，有巨大的向其他身体器官转移的潜力。传统上，有三种常用的 BC 治疗策略，包括手术、放疗和化疗；然而，这些方法与许多有害作用和高复发率有关。
本综述旨在批判性地讨论和概念化与多功能纳米药物在 BC 的早期诊断和有效治疗中的药物意义和治疗可行性相关的现有证据。
尽管基于纳米技术的方法的应用已经彻底改变了 BC 的诊断和治疗结果；然而，这些纳米药物的临床转化面临着巨大的挑战。这些挑战包括被网状内皮系统（RES）识别、血浆半衰期短、非特异性地在非癌细胞中积累，以及药物（s）被外排泵排出。为了规避这些挑战，已经采取了各种适应措施，如聚乙二醇化、靶向配体（s）的缀合和部位响应性（即 pH 响应性、生化或热响应性）。同样，纳米药物的多功能化已成为改善药代动力学特征、对肿瘤微环境的特异性靶向（主动靶向）和有效内化、以及通过沉默外排泵来减轻内化药物内容物的排出的一种可行且可持续的策略。
对现有证据的批判性分析表明，纳米药物的多功能化是一种可行且可持续的策略，可用于早期诊断和治疗 BC，以获得更好的治疗效果。
