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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Antitumor activity and pharmacokinetics of liposomes containing lipophilic gemcitabine prodrugs.
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Antitumor activity and pharmacokinetics of liposomes containing lipophilic gemcitabine prodrugs.

机译：含有亲脂性吉西他滨前药的脂质体的抗肿瘤活性和药代动力学。

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摘要

BACKGROUND: Gemcitabine is a deoxycytidine analogue that exhibits antitumoral activity against adenocarcinomas of the colon, lung and pancreas. After intravenous injection, gemcitabine is rapidly converted to the inactive metabolite 2'-deoxy-2',2'-difluorouridine by cytidine deaminase. MATERIALS AND METHODS: To improve the pharmacokinetic behavior and the antitumor activity of the drug, the gemcitabine prodrug, 4-(N)-stearoylgemcitabine (C18gem) was incorporated in liposomes and both the pharmacokinetic and the in vivo activity of this formulation intravenously or peritumorally administered in nude female CR1:Nu/Nu(CD-1)BR mice grafted with HT-29 and KB 396p cells were studied. RESULTS: The C18gem-liposomes showed both higher plasma half life and tumor regression than control and gemcitabine. CONCLUSION: The incorporation of C18gem-prodrug in liposomes increased the plasma half life of the drug resulting in increased accumulation in the tumor cells and a higher level of antitumoral efficacy. The results obtained with different tumors sensitive to gemcitabine support the efficacy of this proposed drug delivery system.
机译：背景：吉西他滨是一种脱氧胞苷类似物，对结肠，肺和胰腺腺癌具有抗肿瘤活性。静脉注射后，吉西他滨通过胞苷脱氨酶迅速转化为非活性代谢物2'-deoxy-2'，2'-difluorouridine。材料和方法：为了改善药物的药代动力学行为和抗肿瘤活性，将吉西他滨前药4-（N）-硬脂酰吉西他滨（C18gem）掺入脂质体中，并且该制剂的药代动力学和体内活性通过静脉内或经皮给药研究了在移植了HT-29和KB 396p细胞的雌性CR1：Nu / Nu（CD-1）BR裸鼠中施用的d。结果：C18gem-脂质体显示出比对照组和吉西他滨更高的血浆半衰期和肿瘤消退。结论：脂质体中掺入C18gem前药可延长药物的血浆半衰期，从而增加肿瘤细胞中的蓄积性并提高抗肿瘤功效。用对吉西他滨敏感的不同肿瘤获得的结果支持了该提议的药物递送系统的功效。

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