脂质体棕榈酰-L-天冬酰胺酶：特性与生物活性
Liposomal palmitoyl-L-asparaginase: characterization and biological activity.
作者信息
Jorge J C, Perez-Soler R, Morais J G, Cruz M E
机构信息
Departamento de Biotecnologia/INETI, Estrada das Palmeiras, Portugal.
出版信息
Cancer Chemother Pharmacol. 1994;34(3):230-4. doi: 10.1007/BF00685082.
A new derivative of L-asparaginase, palmitoyl-L-asparaginase (palmitoyl-L-ASNase), has been incorporated in liposomes. For this purpose we modified the dehydration-rehydration method and optimized the liposomal composition. The pharmacokinetics, toxicity, and in vivo antitumor activity against P1534 lymphoma of different liposomal palmitoyl-L-ASNase formulations were studied. Liposomal encapsulation of palmitoyl-L-ASNase as compared with free palmitoyl-L-ASNase resulted in a prolongation of the blood half-life (from 2.88 h to longer than 23.7 h), abrogation of acute toxicity, and preservation of in vivo antitumor activity.
一种新的L-天冬酰胺酶衍生物，棕榈酰-L-天冬酰胺酶（palmitoyl-L-ASNase），已被包封于脂质体中。为此，我们改进了脱水再水化方法并优化了脂质体组成。研究了不同脂质体棕榈酰-L-天冬酰胺酶制剂对P1534淋巴瘤的药代动力学、毒性及体内抗肿瘤活性。与游离棕榈酰-L-天冬酰胺酶相比，脂质体包封的棕榈酰-L-天冬酰胺酶使血液半衰期延长（从2.88小时延长至超过23.7小时），消除了急性毒性，并保留了体内抗肿瘤活性。
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