具有增强制剂稳定性的光响应性聚合物胶束纳米颗粒

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

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

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

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

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.

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。