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目的考察壳聚糖修饰的L-天门冬酰胺酶脂质体的血浆稳定性及药动学特性。方法血浆稳定性:于不同时间点,分别测定L-天门冬酰胺酶和壳聚糖修饰的L-天门冬酰胺酶脂质体在大鼠空白血浆中的活性。大鼠静脉注射L-天门冬酰胺酶和壳聚糖修饰的L-天门冬酰胺酶脂质体后,分别考察其药动学特性。采用DAS药动学软件计算药动学参数。结果在空白血浆中,壳聚糖修饰的L-天门冬酰胺酶脂质体的活性高于L-天门冬酰胺酶;壳聚糖修饰的L-天门冬酰胺酶脂质体的活性-时间曲线下面积(AUC_(0-48 h))约为L-天门冬酰胺酶的3.3倍,壳聚糖修饰的L-天门冬酰胺酶脂质体的平均滞留时间(MRT_(0-48 h))约为ASP的2.3倍。结论壳聚糖修饰的L-天门冬酰胺酶脂质体能提高L-天门冬酰胺酶的血浆稳定性及生物利用度。
Objective To investigate the plasma stability and pharmacokinetics of chitosan-modified L-asparaginase liposomes. Methods Plasma stability: At different time points, the activity of L-asparaginase and chitosan-modified L-asparaginase liposomes in blank plasma of rats were determined respectively. After intravenous injection of L-asparaginase and chitosan-modified L-asparaginase liposome, the pharmacokinetics of L-asparaginase liposome were investigated. Pharmacokinetic parameters were calculated using DAS pharmacokinetic software. Results The activity of chitosan-modified L-asparaginase liposome was higher than that of L-asparaginase in blank plasma; the activity-time curve of chitosan-modified L-asparaginase liposome The lower area (AUC 0 (0-48 h)) was approximately 3.3 times that of L-asparaginase, and the average retention time of chitosan-modified L-asparaginase liposomes (MRT 0-48 h) About 2.3 times as much as ASP. Conclusion Chitosan-modified L-asparaginase liposomes can improve the plasma stability and bioavailability of L-asparaginase.