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脂质体蒽环类药物的临床药理学:聚焦于聚乙二醇化脂质体阿霉素。

Clinical pharmacology of liposomal anthracyclines: focus on pegylated liposomal Doxorubicin.

作者信息

Soloman Rebecca, Gabizon Alberto A

机构信息

Oncology Department, Shaare Zedek Medical Center, Jerusalem, Israel.

出版信息

Clin Lymphoma Myeloma. 2008 Feb;8(1):21-32. doi: 10.3816/clm.2008.n.001.

DOI:10.3816/clm.2008.n.001
PMID:18501085
Abstract

Pegylated liposomal doxorubicin (PLD) is a liposomal formulation with a distinct pharmacokinetic profile characterized by an extended circulation time and a reduced volume of distribution. Biodistribution animal studies indicate preferential accumulation of PLD into various implanted mouse-human tumors, with an enhancement of liposomal drug tumor levels compared with free drugs. The extended circulation time of pegylated liposomes and their ability to extravasate through the leaky vasculature of tumors results in the enhanced delivery of liposomal drug and/or radiotracers to the tumor site in patients with cancer. In malignant effusions, Kaposi sarcoma skin lesions, and a variety of solid tumors there is evidence of selective tumor uptake detected by various methods. Pegylated liposomal doxorubicin has been approved for clinical use in a variety of neoplastic conditions because of its antitumor efficacy and unique safety profile with an impressive reduction of cardiac toxicity in comparison with conventional doxorubicin.

摘要

聚乙二醇化脂质体阿霉素(PLD)是一种脂质体制剂,具有独特的药代动力学特征,其特点是循环时间延长和分布容积减小。生物分布动物研究表明,PLD在各种植入的人源化小鼠肿瘤中优先蓄积,与游离药物相比,脂质体药物在肿瘤中的水平有所提高。聚乙二醇化脂质体延长的循环时间及其通过肿瘤渗漏血管系统外渗的能力,导致脂质体药物和/或放射性示踪剂在癌症患者肿瘤部位的递送增强。在恶性胸腔积液、卡波西肉瘤皮肤病变和多种实体瘤中,有证据表明通过各种方法检测到肿瘤有选择性摄取。聚乙二醇化脂质体阿霉素因其抗肿瘤疗效和独特的安全性,与传统阿霉素相比显著降低了心脏毒性,已被批准用于多种肿瘤疾病的临床治疗。

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