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可显影碘化油-氟尿嘧啶聚乳酸微球的研制
王新霞1,张丽2,周闺臣3,张国庆1,鲁莹3,钟延强3*,钟延强3*
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(1.第二军医大学东方肝胆外科医院药材科,上海 200438;2.解放军71352部队医院药房,安阳 455000;3.第二军医大学药学院药剂学教研室,上海 200433)
摘要:
目的制备用于肝动脉栓塞的可显影碘化油-氟尿嘧啶(iodized oil-5-fluorouracil,iodized oil-5-Fu)聚乳酸(polylactide acid, PLA)微球。方法选择具有良好生物相容性及生物可降解性的聚乳酸为载体,加入阳性造影剂碘化油,采用复乳法制备可显影碘化油-氟尿嘧啶聚乳酸微球。以外观、粒径、载药量、包封率为考察指标,采用正交设计确定可显影碘化油-氟尿嘧啶聚乳酸微球的制备工艺。结果显微镜下微球球形圆整,粒径分布均匀,扫描电镜下微球表面有孔,平均粒径约100 μm;载药量(10.78%±0.14%),包封率(63.34%±0.545%),微球显影效果好。结论以可生物降解的PLA材料可制备显影效果好的氟尿嘧啶微球,并且微球具有一定的缓释作用。
关键词:  氟尿嘧啶  聚乳酸  碘化油  微球体  复乳法
DOI:10.3724/SP.J.1008.2010.01100
投稿时间:2010-03-12修订日期:2010-09-13
基金项目:
Preparation of visualized iodized oil-5-fluorouracil loaded polylactic acid microspheres
WANG Xin-xia1, ZHANG Li2, ZHOU Gui-chen3, ZHANG Guo-qing1, LU Ying3, ZHONG Yan-qiang3*,ZHONG Yan-qiang3*
(1. Department of Pharmacy, Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai 200438, China;2. Department of Pharmacy, Hospital of No. 71325 Troop, Anyang 455000, Henan, China;3. Department of Pharmacy, School of Pharmacy, Second Military Medical University, Shanghai 200433, China)
Abstract:
ObjectiveTo prepare visualized iodized oil-5-fluorouracil loaded polylactic acid(PLA) micropheres for hepatic artery embolism treatment.MethodsBiocompatible and biodegradable material PLA was used as vector and iodized oil was used as positive contrast agent to prepare 5-fluorouracil loaded microspheres using double emulsion method. The preparation technology of the microspheres was developed through optimization of appearance, size distribution, drug loading, and encapsulation efficiency by orthogonal-designing method.ResultsThe prepared PLA microspheres were round in shape and had a homogenous diameter distribution. Scanning electron microscope (SEM) showed a pored surface, with an average diameter of 100 μm. The encapsulation efficiency and drug content of microspheres were (63.34%±0.54%) and (10.78%±0.14%), respectively.ConclusionWe have successfully prepared the visualized iodized oil-5-fluorouracil PLA microspheres, which can release 5-fluorouracil in a controlled manner.
Key words:  fluorouracil  polylactic acid  iodized oil  microspheres  double emulsion method