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两亲性聚唾液酸衍生物:合成、表征及体外细胞毒性

Amphiphilic polysialic acid derivatives: synthesis, characterization, and in-vitro cytotoxicity.

作者信息

Deepagan V G, Thambi Thavasyappan, Ko Hyewon, Kang Young Mo, Park Jae Hyung

机构信息

Department of Polymer Science and Engineering, College of Engineering, Sungkyunkwan University, Suwon 440-746, Republic of Korea.

出版信息

J Nanosci Nanotechnol. 2013 Nov;13(11):7312-8. doi: 10.1166/jnn.2013.8089.

DOI:10.1166/jnn.2013.8089
PMID:24245249
Abstract

Polysialic acid (PSA), a natural hydrophilic polysaccharide, is a potential alternative to poly(ethylene glycol) as the hydrophilic constituent of the polymeric amphiphiles for biomedical applications. In this study, amphiphilic block copolymers were prepared based on PSA as the hydrophilic block and polycaprolactone (PCL) as the hydrophobic block. The block copolymers formed micelles with spherical shapes in an aqueous environment. The average sizes of the nanoparticles were in the range of 270-390 nm, depending on the block length of PCL. The zeta potential values of the micelles were approximately -20 mV due to the negatively charged carboxylic acids of PSA. The nanoparticles showed good stability for five days in a physiological solution (pH 7.4), and had low critical micelle concentration values (1.68-8.54 microg/ml). The in-vitro cytotoxicity tests confirmed that the PSA-PCL micelles had little cytotoxicity. All these results suggest that the PSA-PCL block copolymers can form nano-sized micelles with high stability and low toxicity, implying their high potential for biomedical application.

摘要

聚唾液酸(PSA)是一种天然的亲水性多糖,作为聚合物两亲物的亲水性成分,它是聚乙二醇在生物医学应用中的潜在替代品。在本研究中,基于PSA作为亲水嵌段和聚己内酯(PCL)作为疏水嵌段制备了两亲性嵌段共聚物。该嵌段共聚物在水性环境中形成了球形胶束。纳米颗粒的平均尺寸在270 - 390 nm范围内,这取决于PCL的嵌段长度。由于PSA带负电荷的羧酸,胶束的zeta电位值约为 - 20 mV。纳米颗粒在生理溶液(pH 7.4)中五天内表现出良好的稳定性,并且具有较低的临界胶束浓度值(1.68 - 8.54 μg/ml)。体外细胞毒性测试证实PSA - PCL胶束几乎没有细胞毒性。所有这些结果表明,PSA - PCL嵌段共聚物可以形成具有高稳定性和低毒性的纳米级胶束,这意味着它们在生物医学应用中具有很高的潜力。

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