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荧光(罗丹明)、叶酸修饰和阿霉素负载、PEG 化纳米粒子的合成。

Fluorescent (rhodamine), folate decorated and doxorubicin charged, PEGylated nanoparticles synthesis.

机构信息

Department of Materials and Production Engineering, University of Naples Federico II, 80125, Naples, Italy.

出版信息

J Mater Sci Mater Med. 2012 Jul;23(7):1697-704. doi: 10.1007/s10856-012-4634-2. Epub 2012 Apr 7.

DOI:10.1007/s10856-012-4634-2
PMID:22484837
Abstract

PEGylated silica nanoparticles, giving very stable aqueous sols, were successfully functionalised with rhodamine, one of the more stable fluorophore; they were also decorated with the targeting agent folic acid (FA) and charged with the well known drug doxorubicin. Rhodamine functionalization required a modification of the synthesis route of the nanoparticles (NP). Functionalization with FA required activation with 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride. Folate decorated NP were easily charged with doxorubicin. The experimental results proved the successfulness of the functionalization. The bond to the NP does not reduce the therapeutic efficacy of the drug. The calculated encapsulation efficiency (32 %) was only a little lower than the value (47 %) reported for the very popular PEGylated PLGA NP.

摘要

聚乙二醇化硅纳米颗粒,可形成非常稳定的水溶胶,成功地用荧光素进行了功能化,荧光素是一种更稳定的荧光团之一;它们还被靶向剂叶酸(FA)修饰,并负载了著名的药物阿霉素。荧光素的功能化需要对纳米颗粒(NP)的合成路线进行修改。FA 的功能化需要用 1-乙基-3-(3-二甲基氨基丙基)碳二亚胺盐酸盐进行激活。叶酸修饰的 NP 很容易负载阿霉素。实验结果证明了功能化的成功。与 NP 的键合不会降低药物的治疗效果。计算出的包封效率(32%)仅略低于非常流行的聚乙二醇化 PLGA NP 的报告值(47%)。

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