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载紫杉醇的 Pluronic 纳米粒经壳聚糖/肝素复合修饰后靶向能力增强。

Enhancement of the targeting capabilities of the Paclitaxel-loaded pluronic nanoparticles with a glycol chitosan/heparin composite.

机构信息

College of Pharmacy, Korea University , Jochiwon, Yeongi, Chungnam 339-700, Republic of Korea.

出版信息

Mol Pharm. 2012 Feb 6;9(2):230-6. doi: 10.1021/mp200278s. Epub 2011 Dec 23.

DOI:10.1021/mp200278s
PMID:22149139
Abstract

An enhancement of tumor-targeting capability was demonstrated with paclitaxel (PTX)-loaded Pluronic nanoparticles (NPs) with immobilized glycol chitosan and heparin. The PTX-loaded Pluronic NPs were prepared as described in our previous report by means of a temperature-induced phase transition in a mixture of Pluronic F-68 and liquid polyethylene glycol (PEG; molecular weight: 400) containing PTX. The liquid PEG is used as the solubilizer of PTX, and Pluronic F-68 is the polymer that encapsulates the PTX. The glycol chitosan and heparin were immobilized on the surface of the Pluronic NPs in an aqueous medium, and a powdery form of the glycol chitosan/heparin immobilized Pluronic NPs (composite NPs) was obtained by freeze-drying. Field emission scanning electron microscopy and a particle size analyzer were used to observe the morphology and size distribution of the prepared NPs. To apply the composite NPs as a delivery system for the model anticancer drug PTX, the release pattern and pharmacokinetic parameters were observed, and the tumor growth was monitored by injecting the composite NPs into the tail veins of tumor-bearing mice. An enhancement of tumor-targeting capability of NPs was verified by using noninvasive live animal imaging technology to observe the time-dependent excretion profile, the in vivo biodistribution, circulation time, and the tumor-targeting capability of composite NPs.

摘要

载紫杉醇(PTX)的 Pluronic 纳米粒(NPs)通过固定化的壳聚糖乙二醇和肝素增强了肿瘤靶向能力。PTX 负载的 Pluronic NPs 是按照我们之前的报道方法制备的,即在含有 PTX 的 Pluronic F-68 和液态聚乙二醇(PEG;分子量:400)混合物中通过温度诱导的相转变。液态 PEG 用作 PTX 的增溶剂,Pluronic F-68 是包裹 PTX 的聚合物。壳聚糖乙二醇和肝素在水介质中固定在 Pluronic NPs 的表面,通过冷冻干燥得到壳聚糖乙二醇/肝素固定化 Pluronic NPs(复合 NPs)的粉末形式。场发射扫描电子显微镜和粒径分析仪用于观察制备的 NPs 的形态和粒径分布。为了将复合 NPs 用作模型抗癌药物 PTX 的递送系统,观察了释放模式和药代动力学参数,并通过向荷瘤小鼠尾静脉注射复合 NPs 来监测肿瘤生长。通过使用非侵入性活体动物成像技术观察复合 NPs 的时间依赖性排泄曲线、体内分布、循环时间和肿瘤靶向能力,验证了 NPs 的肿瘤靶向能力增强。

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