Anti-tumor Effect of All-Trans Retinoic Acid Loaded Polymeric Micelles in Solid Tumor Bearing Mice
Anti-tumor Effect of All-Trans Retinoic Acid Loaded Polymeric Micelles in Solid Tumor Bearing Mice
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DOI：
10.1007/s11095-007-9398-x
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发表时间：
2008-02
影响因子：
3.7
通讯作者：
Narin Chansri;S. Kawakami;M. Yokoyama;Tatsuhiro Yamamoto;Pensri Charoensit;M. Hashida
中科院分区：
文献类型：
--
作者：
Narin Chansri;S. Kawakami;M. Yokoyama;Tatsuhiro Yamamoto;Pensri Charoensit;M. Hashida
目的开发用于肠胃外给药的全反式视黄酸 (ATRA) 聚合物胶束。对CT26实体瘤小鼠静脉注射后评价ATRA聚合物胶束的分布特性和抗肿瘤活性。方法采用蒸发法制备聚乙二醇-聚天冬氨酸苄酯嵌段共聚物ATRA。通过测量小鼠注射后的放射性来测定血液和组织（包括肿瘤）中[3H]ATRA的水平。测定肿瘤体积和小鼠的存活率来评估抗癌活性。结果与游离ATRA相比，聚合物胶束递送ATRA可延长血液循环并增强ATRA在肿瘤组织中的积累。 ATRA聚合物胶束治疗后，小鼠肿瘤生长明显延迟，存活时间延长，这表明ATRA具有改善的抗癌活性。结论聚合物胶束是一种有前途且有效的ATRA载体，可以增强肿瘤递送，在实体瘤的治疗中具有广阔的应用前景。
PurposeAll-transretinoic acid (ATRA) polymeric micelles were developed for parenteral administration. The distribution characteristics and antitumor activities of ATRA polymeric micelles were evaluated after intravenous administration to mice bearing CT26 solid tumors.MethodsATRA incorporated in poly(ethylene glycol)-poly(benzyl aspartate) block copolymer was prepared by the evaporation method. The levels of [3H]ATRA in blood and tissue including tumor were determined by measuring the radioactivity after injection into mice. The tumor volume and the survival of the mice were determined to assess the anticancer activity.ResultsThe delivery of ATRA by polymeric micelles prolonged the blood circulation and enhanced the accumulation of ATRA in the tumor tissue compared with the administration of free ATRA. Tumor growth was significantly delayed and the survival time of mice was prolonged following the treatment by ATRA polymeric micelles demonstrating the improved anticancer activity of ATRA.ConclusionPolymeric micelles are a promising and effective carrier of ATRA in order to enhance tumor delivery and they have a promising potential application in the treatment of solid tumors.