Impact of surfactant treatment of paclitaxel nanocrystals on biodistribution and tumor accumulation in tumor-bearing mice
Impact of surfactant treatment of paclitaxel nanocrystals on biodistribution and tumor accumulation in tumor-bearing mice
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DOI：
10.1016/j.jconrel.2016.07.015
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发表时间：
2016-09-10
影响因子：
10.8
通讯作者：
Li, Tonglei
中科院分区：
文献类型：
--
作者：
Gao, Wei;Chen, Yan;Li, Tonglei
我们先前在肿瘤小鼠模型中测试了紫杉醇纳米晶体（PTX-NC），并了解到纳米晶体制剂可以实现与常规Taxol（R）制剂相似且上级的抗癌功效，但副作用显著降低。纳米晶体没有涂覆任何表面活性剂，大部分注射剂量被肝脏吸收（>40%），而血液循环中存在极少量并迅速消除。这项工作的目的是用基于PEG的聚合物处理PTX-NC的表面，并检查表面涂层对生物分布、药代动力学和肿瘤保留的影响。在荷瘤小鼠中的测试显示，用Pluronic（R）F68（PEG-PPG-PEG嵌段聚合物）处理的PTX-NC显著增强了药物的血液循环和在肿瘤组织中的积累。然而，到达肿瘤的绝对量相对于剂量仍然是最小的。(C)2016爱思唯尔B. V.保留所有权利。
We have previously tested paclitaxel nanocrystals (PTX-NCs) in tumor murine models and learned that the nano-crystal formulation could achieve similar and superior anticancer efficacy to the conventional Taxol (R) formulation, but with significantly reduced side-effects. The nanocrystals were not coated with any surfactants and a majority of the injected dose was taken up by the liver (>40%), while a minimal amount was present in the blood circulation and quickly eliminated. The aim of this work was to treat the surface of PTX-NCs with PEG-based polymers and examine the impact by surface coating on biodistribution, pharmacokinetics, and tumor retention. Testing in tumor-bearing mice showed that PTX-NCs treated with Pluronic (R) F68 (PEG-PPG-PEG block polymer) significantly enhanced blood circulation of the drug and accumulation in tumor tissue. The absolute amount reaching the tumor, however, was still minimal relative to the dose. (C) 2016 Elsevier B.V. All rights reserved.