脂质体包裹的脂溶性烷化剂治疗效率提高。
Increased therapeutic efficiency of a lipid-soluble alkylating agent incorporated in liposomes.
作者信息
Babbage J W, Berenbaum M C
出版信息
Br J Cancer. 1982 Jun;45(6):830-4. doi: 10.1038/bjc.1982.134.
Abstract
A highly hydrophobic alkylating agent, 1-N,N-bis(beta-bromoethyl) amino-3-methylnaphthalene, given as the free drug in oil, cured a substantial proportion of mice bearing the PC6 myeloma in the dose range 2-7 mg/kg. However, these doses were toxic, and the LD50 was 6-7 mg/kg. When incorporated in liposomes, similar curative effects were obtained at doses of 10-41 mg/kg without material toxicity, even at the highest dose. Liposome entrapment therefore greatly increases the therapeutic efficiency of this agent.
摘要
一种高度疏水的烷基化剂，1-N，N-双（β-溴乙基）氨基-3-甲基萘，以油剂形式的游离药物给药，在2-7mg/kg的剂量范围内治愈了相当比例的携带PC6骨髓瘤的小鼠。然而，这些剂量有毒，半数致死量为6-7mg/kg。当包裹于脂质体中时，在10-41mg/kg的剂量下可获得相似的治愈效果，且无明显毒性，即使是最高剂量。因此，脂质体包封极大地提高了该药物的治疗效率。
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