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脂质体包裹的1-β-D-阿拉伯呋喃糖基胞嘧啶对小鼠中枢神经系统白血病的治疗

Therapy of central nervous system leukemia in mice by liposome-entrapped 1-beta-D-arabinofuranosylcytosine.

作者信息

Hong F, Mayhew E

机构信息

Department of Experimental Pathology, Roswell Park Memorial Institute, Buffalo, New York 14263.

出版信息

Cancer Res. 1989 Sep 15;49(18):5097-102.

PMID:2766280
Abstract

Studies were undertaken to determine the therapeutic effects of liposome-encapsulated 1-beta-D-arabinofuranosylcytosine (lip-ara-C) against intracranial L1210 leukemia. The effects of administration route, drug dosage, liposome type, and tumor load on therapeutic efficacy were also studied. One hundred % mice were cured after a single intracranial 40 mg/kg dose of lip-ara-C, dependent on tumor load. Intracranial lip-ara-C was more effective than i.v. lip-ara-C. A single i.v. dose of lip-ara-C was therapeutically superior to 5-day i.v. infusion of the free drug. Intracranial or i.v. lip-ara-C at therapeutic doses resulted in less systemic toxicity than i.v. infusion of free ara-C, suggesting possible use of lip-ara-C as an adjunct to treatment of central nervous system leukemia.

摘要

开展了多项研究以确定脂质体包裹的1-β-D-阿拉伯呋喃糖基胞嘧啶(脂质体阿糖胞苷)对颅内L1210白血病的治疗效果。还研究了给药途径、药物剂量、脂质体类型和肿瘤负荷对治疗效果的影响。根据肿瘤负荷,单次颅内给予40mg/kg剂量的脂质体阿糖胞苷后,100%的小鼠被治愈。颅内给予脂质体阿糖胞苷比静脉注射脂质体阿糖胞苷更有效。单次静脉注射脂质体阿糖胞苷在治疗上优于游离药物的5天静脉输注。治疗剂量的颅内或静脉注射脂质体阿糖胞苷比静脉输注游离阿糖胞苷产生的全身毒性更小,这表明脂质体阿糖胞苷可能用作中枢神经系统白血病治疗的辅助药物。

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