5‐Fluoroorotate: a new liposome‐dependent cytotoxic agent

FEBS Letters

Papahadjopoulos, Demetrios¹  Lopez, Ninfa G.²  Stem, Walter H.²  Heath, Timothy D.² 

[1] Depts of Pharmacology, University of California, San Francisco, CA 94143, and Veterans Administration Medical Center, San Francisco, CA 94121, USA;Depts of Ophthalmology, University of California, San Francisco, CA 94143, and Veterans Administration Medical Center, San Francisco, CA 94121, USA

关键词: Fluoropyrimidine Liposome Targeting Endocytosis Lysosomotropism Drug carrier;   

DOI  :  10.1016/0014-5793(85)81217-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The potency of 5-fluoroorotate for inhibition of L929 or CV1-P cell growth is increased by encapsulation in negatively charged liposomes. The optimal liposome composition is dipalmitoylphosphatidylglycerol: cholesterol, 67:33. Unextruded large unilamellar liposomes are the optimal size for delivery. This compound is the second transport-negative drug which we have found to exhibit liposome-dependent delivery.

【 授权许可】

Unknown