We herein review various pharmacological and clinical aspects of pegylated liposomal doxorubicin (PLD), the first nanomedicine to be approved for cancer therapy, and discuss the gap between its potent antitumor activity in preclinical studies and its comparatively modest achievements in clinical studies and limited use in clinical practice. PLD is a complex formulation of doxorubicin based on pharmaceutical nanotechnology with unique pharmacokinetic and pharmacodynamic properties. Its long circulation time with stable retention of the payload and its accumulation in tumors with high vascular permeability both result in important advantages over conventional chemotherapy. The ability of PLD to buffer a number of undesirable side effects of doxorubicin, including a major risk reduction in cardiac toxicity, is now well-established and confers a major added value in a number of disease conditions. PLD is approved for the treatment of ovarian cancer, breast cancer, multiple myeloma, and Kaposi sarcoma. In addition, clinically significant antitumor activity of PLD has been reported in a number of other cancer types, including lymphomas and soft tissue sarcomas. In spite of this, PLD has not replaced conventional doxorubicin in common applications such as the adjuvant and neoadjuvant treatment of breast cancer, and its use in the clinic has not become as widespread as one may have predicted. Exploiting the unique pharmacology of PLD, analyzing its selective biodistribution and homing to tumors in cancer patients with proper theranostic tools, and harnessing its complex interaction with the immune system, will lead to a more selective and rational use of PLD that may have great impact on future clinical results and may help realize its largely untapped potential.

我们在本文中综述了聚乙二醇化脂质体阿霉素（PLD）（首个被批准用于癌症治疗的纳米药物）的各种药理和临床方面，并讨论了其在临床前研究中有效的抗肿瘤活性与其在临床研究中相对中等的成就以及在临床上的有限使用之间的差距。临床实践。PLD是基于药物纳米技术的阿霉素的复杂制剂，具有独特的药代动力学和药效学特性。与传统的化学疗法相比，其循环时间长，有效负载保持稳定以及在高血管通透性肿瘤中的蓄积均具有重要的优势。PLD缓冲阿霉素的许多不良副作用的能力，包括降低心脏毒性的主要风险，现在已经建立了良好的基础，并赋予了许多疾病条件主要的附加值。PLD被批准用于治疗卵巢癌，乳腺癌，多发性骨髓瘤和卡波西肉瘤。此外，在许多其他癌症类型中，包括淋巴瘤和软组织肉瘤中，也报告了PLD在临床上具有重要的抗肿瘤活性。尽管如此，PLD在诸如乳癌的辅助治疗和新辅助治疗等常见应用中并未替代传统的阿霉素，并且其在临床中的使用并未像人们所预期的那样广泛。利用PLD的独特药理学，通过适当的治疗学工具分析其选择性生物分布并归巢到癌症患者的肿瘤中，并利用其与免疫系统的复杂相互作用，