[基于整合素导向肽的磷脂纳米颗粒靶向递送系统的阿霉素细胞积累效率的研究]。

Q3 Biochemistry, Genetics and Molecular Biology
L V Kostryukova, Yu A Tereshkina, E G Tikhonova, M A Sanzhakov, D V Bobrova, Yu Yu Khudoklinova
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引用次数: 0

摘要

含有靶向系统的化疗药物是提高胶质母细胞瘤治疗有效性的有希望的途径。肿瘤细胞表面表达增加的特异性蛋白被认为是可能的靶点。整合素αvβ3就是细胞表面的一类蛋白质。它能有效结合环状Arg-Gly-Asp (cRGD)肽。在本研究中,研究了cRGD肽修饰的阿霉素(Dox)磷脂组成。该合成物的粒径为43.76±2.09 nm, ζ电位为4.33±0.54 mV。Dox几乎完全融入纳米颗粒(99.7±0.58%)。在酸性介质中(pH 5.0,约为35±3.2%)药物释放增加。与自由形式相比,使用磷脂纳米颗粒与目标载体的组合物,Dox的总积累和内化是1.4倍。在不表达αvβ3整合素的HeLa细胞系中,没有观察到这种效应。这些结果表明,利用环状RGD肽将Dox传递到胶质母细胞瘤细胞的前景,以及进一步研究整个组合物整体作用机制的可行性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Study of the efficiency of cellular accumulation of doxorubicin supplied with a targeted delivery system based on phospholipid nanoparticles with integrin-directed peptide].

Chemotherapeutic agents containing targeted systems are a promising pathway to increase the effectiveness of glioblastoma treatment. Specific proteins characterized by increased expression on the surface of tumor cells are considered as possible targets. Integrin αvβ3 is one of such proteins on the cell surface. It effectively binds the cyclic Arg-Gly-Asp (cRGD) peptide. In this study, the cRGD peptide-modified doxorubicin (Dox) phospholipid composition was investigated. The particle size of this composition was 43.76±2.09 nm, the ζ-potential was 4.33±0.54 mV. Dox was almost completely incorporated into the nanoparticles (99.7±0.58%). The drug release increased in an acidic medium (at pH 5.0 of about 35±3.2%). The total accumulation and internalization of Dox used the composition of phospholipid nanoparticles with the targeted vector was 1.4-fold higher as compared to the free form. In the HeLa cell line (not expressing αvβ3 integrin) this effect was not observed. These results suggest the prospects of using the cyclic RGD peptide in the delivery of Dox to glioblastoma cells and the feasibility of further investigation of the mechanism of action of the entire composition as a whole.

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来源期刊
Biomeditsinskaya khimiya
Biomeditsinskaya khimiya Biochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (all)
CiteScore
1.30
自引率
0.00%
发文量
49
期刊介绍: The aim of the Russian-language journal "Biomeditsinskaya Khimiya" (Biomedical Chemistry) is to introduce the latest results obtained by scientists from Russia and other Republics of the Former Soviet Union. The Journal will cover all major areas of Biomedical chemistry, including neurochemistry, clinical chemistry, molecular biology of pathological processes, gene therapy, development of new drugs and their biochemical pharmacology, introduction and advertisement of new (biochemical) methods into experimental and clinical medicine etc. The Journal also publish review articles. All issues of journal usually contain invited reviews. Papers written in Russian contain abstract (in English).
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