Background/Objectives: Effective and targeted delivery of doxorubicin (DOX) remains a significant challenge due to its dose-limiting cardiotoxicity and systemic side effects. Liposomal formulations like Doxil®have improved tumor targeting and reduced toxicity, but issues such as limited stability, poor release control, and insufficient site-specific delivery persist. As a result, there is a growing interest in advanced drug delivery systems, particularly polymeric nanocarriers, which offer biocompatibility, tunable properties, and ease of fabrication. Methods: This review is organized into two key sections. The first section provides a comprehensive overview of DOX, including its mechanism of action, clinical challenges, and the limitations of current chemotherapy approaches. The second section highlights recent advances in polymeric nanocarriers for DOX delivery, focusing on polymeric micelles as well as other promising systems like hydrogels, dendrimers, polymersomes, and polymer–drug conjugates. Results: Initial discussions explore current strategies enhancing DOX’s clinical translation, including methods to address cardiotoxicity and multidrug resistance. The latter part presents recent studies that report improved drug loading efficiency in polymeric nanocarriers through techniques such as core/shell modifications, enhanced hydrophobic interactions, and polymer–drug conjugation. Conclusions: Despite notable progress in polymeric nanocarrier-based DOX delivery, challenges like limited circulation time, immunogenicity, and manufacturing scalability continue to hinder clinical application. Continued innovation in this field is crucial for the development of safe, effective, and clinically translatable polymeric nanocarriers for cancer therapy.
背景/目的：阿霉素（DOX）因其剂量限制性心脏毒性和全身性副作用，其有效且靶向的递送仍面临重大挑战。以Doxil®为代表的脂质体制剂虽改善了肿瘤靶向性并降低了毒性，但仍存在稳定性有限、释放控制不佳及位点特异性递送不足等问题。因此，先进药物递送系统，特别是具有生物相容性、性能可调且易于制备的聚合物纳米载体，正受到日益广泛的关注。方法：本综述分为两个主要部分。第一部分全面概述了DOX的作用机制、临床挑战及当前化疗方法的局限性；第二部分重点介绍了用于DOX递送的聚合物纳米载体的最新进展，聚焦于聚合物胶束以及水凝胶、树状大分子、聚合物囊泡和聚合物-药物偶联物等其他有前景的系统。结果：前期讨论探讨了当前促进DOX临床转化的策略，包括应对心脏毒性和多药耐药性的方法；后续部分展示了通过核/壳修饰、增强疏水相互作用及聚合物-药物偶联等技术提高聚合物纳米载体载药效率的最新研究成果。结论：尽管基于聚合物纳米载体的DOX递送研究已取得显著进展，但循环时间有限、免疫原性和规模化生产等挑战仍阻碍其临床应用。该领域的持续创新对于开发安全有效、可临床转化的癌症治疗用聚合物纳米载体至关重要。
Advances in Doxorubicin Chemotherapy: Emerging Polymeric Nanocarriers for Drug Loading and Delivery
肿瘤(癌症)患者之家