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具有增强制剂稳定性的光响应性聚合物胶束纳米颗粒

Light-Responsive Polymeric Micellar Nanoparticles with Enhanced Formulation Stability.

作者信息

Kim Kyoung Nan, Oh Keun Sang, Shim Jiwook, Schlaepfer Isabel R, Karam Sana D, Lee Jung-Jae

机构信息

Department of Chemistry, University of Colorado Denver, Denver, CO 80204, USA.

TGel Bio, Co, LTD, Seoul 06185, Korea.

出版信息

Polymers (Basel). 2021 Jan 26;13(3):377. doi: 10.3390/polym13030377.

Abstract

Light-sensitive polymeric micelles have recently emerged as promising drug delivery systems for spatiotemporally controlled release of payload at target sites. Here, we developed diazonaphthoquinone (DNQ)-conjugated micellar nanoparticles that showed a change in polarity of the micellar core from hydrophobic to hydrophilic under UV light, releasing the encapsulated anti-cancer drug, doxetaxel (DTX). The micelles exhibited a low critical micelle concentration and high stability in the presence of bovine serum albumin (BSA) solution due to the hydrophobic and π-π stacking interactions in the micellar core. Cell studies showed enhanced cytotoxicity of DTX-loaded micellar nanoparticles upon irradiation. The enhanced stability would increase the circulation time of the micellar nanoparticles in blood, and enhance the therapeutic effectiveness for cancer therapy.

摘要

光敏聚合物胶束最近已成为一种很有前景的药物递送系统,可在靶位点实现药物时空可控释放。在此,我们开发了重氮萘醌(DNQ)共轭胶束纳米颗粒,其在紫外光照射下胶束核心的极性从疏水性变为亲水性,从而释放出包裹的抗癌药物多西他赛(DTX)。由于胶束核心中的疏水和π-π堆积相互作用,这些胶束在牛血清白蛋白(BSA)溶液存在下表现出低临界胶束浓度和高稳定性。细胞研究表明,照射后负载DTX的胶束纳米颗粒的细胞毒性增强。增强的稳定性将增加胶束纳米颗粒在血液中的循环时间,并提高癌症治疗的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2da9/7866127/5d0d7796fbee/polymers-13-00377-g001.jpg

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