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5-氟尿嘧啶负载微球在实验性大鼠胶质瘤上的释放动力学

Release kinetics of 5-fluorouracil-loaded microspheres on an experimental rat glioma.

作者信息

Roullin Valérie-Gaelle, Lemaire Laurent, Venier-Julienne Marie-Claire, Faisant Nathalie, Franconi Florence, Benoit Jean-Pierre

机构信息

INSERM ERIT-M 0104, 10 rue A. Boquel, F-49100 Angers, France.

出版信息

Anticancer Res. 2003 Jan-Feb;23(1A):21-5.

Abstract

BACKGROUND

Biodegradable loaded systems are promising devices for controlled and sustained release of anticancer drugs to brain tumours. We investigated the influence of drug-release profiles of 5-fluorouracil-loaded microspheres designed for the treatment of malignant gliomas.

MATERIALS AND METHODS

2.5 mg 5-FU delivered by either fast. (1 formulation) or slow-(2 formulations) 5-FU release microspheres (MS) were tested in C6-glioma rat brains. Tumor response was assessed by T2-weighted MRI.

RESULTS

All treated animals, whatever the release profile considered, displayed a comparable 50% increase in life span versus controls. Delays in C6-glioma development appeared to correspond to the in vitro release periods of MS. In terms of curative prospect, complete remission was only observed in 11% of 5-FU-treated animals (4 out of 38).

CONCLUSION

Formulation was unambiguously implicated in the response observed after local delivery of 5-FU to glioma.

摘要

背景

可生物降解的负载系统是用于向脑肿瘤控制和持续释放抗癌药物的有前景的装置。我们研究了设计用于治疗恶性胶质瘤的载5-氟尿嘧啶微球的药物释放曲线的影响。

材料与方法

通过快速(1种制剂)或缓慢(2种制剂)释放5-氟尿嘧啶的微球(MS)递送2.5mg 5-氟尿嘧啶,在C6胶质瘤大鼠脑中进行测试。通过T2加权MRI评估肿瘤反应。

结果

无论考虑何种释放曲线,所有接受治疗的动物与对照组相比,寿命均有相当的50%的增加。C6胶质瘤发展的延迟似乎与MS的体外释放期相对应。就治愈前景而言,仅在11%的5-氟尿嘧啶治疗动物(38只中的4只)中观察到完全缓解。

结论

制剂无疑与向胶质瘤局部递送5-氟尿嘧啶后观察到的反应有关。

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