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.

Highlights

  • Polymeric micelles have emerged as promising drug delivery systems for cancer treatment because amphiphilic block copolymers enable micelles to improve drug solubility, control drug release, prolong circulation time in body and avoid the elimination of reticuloendothelial system (RES) [1,2,3,4,5,6,7,8]

  • In many light-responsive polymeric micelle systems, UV light triggers a change in polarity or a transition from hydrophobicity to hydrophilicity in domains bearing photochromic azobenzene, spiropyran, and 2-diazo-1,2-naphthoquinone (DNQ) [27,28,29,30,31,32,33], which leads to drug release [34,35,36,37,38]

  • Conventional micelle systems have limited drug loading capacity (LC) and relatively high critical micelle concentrations (CMC), which impair particle stability resulting in decreased blood circulation time and release of drugs before the micelles accumulate in the tumor sites

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Summary

Introduction

Polymeric micelles have emerged as promising drug delivery systems for cancer treatment because amphiphilic block copolymers enable micelles to improve drug solubility, control drug release, prolong circulation time in body and avoid the elimination of reticuloendothelial system (RES) [1,2,3,4,5,6,7,8]. Stimulus-responsive polymeric micelles activated by pH, temperatures, redox, ultrasound, and light have been explored to provide spatial or temporal control of release of anti-cancer drugs to tumors [13,14,15,16,17,18]. Conventional micelle systems have limited drug loading capacity (LC) and relatively high critical micelle concentrations (CMC), which impair particle stability resulting in decreased blood circulation time and release of drugs before the micelles accumulate in the tumor sites.

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