Study of Targeting and Controlled Release Behavior of 5-Fluorouracil-loaded PLA Ultramicron on the Treatment of Human Gastric Tumor Xenograft

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Study of Targeting and Controlled Release Behavior of 5-Fluorouracil-loaded PLA Ultramicron on the Treatment of Human Gastric Tumor Xenograft

更新时间：2022-09-18

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- Study of Targeting and Controlled Release Behavior of 5-Fluorouracil-loaded PLA Ultramicron on the Treatment of Human Gastric Tumor Xenograft
- Polymer Bulletin Vol. 18, Issue 6, Pages: 90-94(2005)
- 作者机构：
  
  1.天津大学材料学院纳米生物技术研究所，天津　300072
  2.天津医科大学总医院，天津　300052
- 作者简介：
- 基金信息：
- DOI：10.14028/j.cnki.1003-3726.2005.06.015
  CLC：
- Published：2005-12，
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Chun-bao MA, Xiao-yan LIU, Jin CHANG, Tao WANG, Qing-yu ZHANG. Study of Targeting and Controlled Release Behavior of 5-Fluorouracil-loaded PLA Ultramicron on the Treatment of Human Gastric Tumor Xenograft. [J]. Polymer Bulletin 18(6):90-94(2005)
DOI：

Chun-bao MA, Xiao-yan LIU, Jin CHANG, Tao WANG, Qing-yu ZHANG. Study of Targeting and Controlled Release Behavior of 5-Fluorouracil-loaded PLA Ultramicron on the Treatment of Human Gastric Tumor Xenograft. [J]. Polymer Bulletin 18(6):90-94(2005) DOI： 10.14028/j.cnki.1003-3726.2005.06.015.

摘要

使用w/o/w 复乳法制备聚乳酸载5-氟尿嘧啶超微粒子，使用透射电镜、激光粒度仪和紫外分光光度计对超微粒子进行表征，并考察其体外释药性质。将

99m

Tc 标记的连有VEGF

121

单克隆抗体的超微粒子通过尾静脉注射到SCID 裸鼠体内，观察它对胃癌转移瘤的靶向效果和治疗效果。结果显示超微粒子成圆球形，平均粒径为195.2nm，多分散系数为0.148，靶向载药超微粒子的载药率为8.23%，包封率为24.71%。聚乳酸载5-FU超微粒子在PBS 缓冲溶液中具有较好的控释效果，累积释放量Q 与时间平方根

t

1/2

基本呈线性关系.尾静脉注射靶向超微粒子两小时以后可看到大部分超微粒子集中到肿瘤部位。在所有的实验组中，含5-FU 靶向载药超微粒子组的疗效最好，说明本靶向载药超微粒子具有抑制肿瘤的血管生成并在肿瘤组织释放化疗药物抑制肿瘤生长的双重作用。

Abstract

5-FU-loaded PLA ultramicron were prepared by a w/o/w emulsion evaporation method

and were characterized by transmission electron microscopy (TEM)

particle size analyzer and UV spectrometer.The release performances of 5-FU loaded PLA ultramicron in vitro were studied.The VEGF/5-FU loaded PLA ultramicron labeled technetium-

99

m were injected in nude mice by tail vein to observe targerting effect and therapeutic effect.TEM observation showed ultramicron were spherical

The mean diameter was 195.2nm

and the index of polydispersity was 0.148

the drug content was 8.23%

and the encapsulation efficiency was 24.71%.There was a linear relationship between the amount of accumulative release Q and time square root

t

1/2

.After targeted 5-FU loaded PLA ultramicron injection 2 hours

the majority of ultramicron centralized at tumor site.In all the treatment groups

5-FU/VEGF loaded PLA ultramicron group had best result.That demonstrated 5-FU/VEGF loaded PLA ultramicron had multiple function with inhibition of growth of blood vessel of tumor and controlled release drug in the tumor site.

关键词

靶向超微粒子控制释放抗VEGF 单克隆抗体5-氟尿嘧啶

Keywords

Targeted ultramicronControlled releaseVEGF monoclonal antibody5-Fluorouracil

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