Multifunctional Polymer Nanoparticles for Dual Drug Release and Cancer Cell Targeting.

Yu-Han Wen,Chun-Liang Lo,Tsung-Ying Lee,Yi-Ting Chiang,Ping-Chuan Fu

doi:10.3390/polym9060213

Yu-Han Wen, Chun-Liang Lo + Show 3 more

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https://doi.org/10.3390/polym9060213

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Journal: Polymers	Publication Date: Jun 9, 2017
Citations: 10	License type: CC BY 4.0

Affiliation: National Yang Ming Chiao Tung University

Abstract

Multifunctional polymer nanoparticles have been developed for cancer treatment because they could be easily designed to target cancer cells and to enhance therapeutic efficacy according to cancer hallmarks. In this study, we synthesized a pH-sensitive polymer, poly(methacrylic acid-co-histidine/doxorubicin/biotin) (HBD) in which doxorubicin (DOX) was conjugated by a hydrazone bond to encapsulate an immunotherapy drug, imiquimod (IMQ), to form dual cancer-targeting and dual drug-loaded nanoparticles. At low pH, polymeric nanoparticles could disrupt and simultaneously release DOX and IMQ. Our experimental results show that the nanoparticles exhibited pH-dependent drug release behavior and had an ability to target cancer cells via biotin and protonated histidine.

Highlights

IntroductionNanoparticle-based drug delivery systems have been used for cancer therapy for several decades
Nanoparticle-based drug delivery systems have been used for cancer therapy for several decades.Among these nanocarriers, polymeric nanoparticles showed more stable and easy preparation by various manufacturing methods [1]
Methacrylic Acid N-hydroxysuccinimide Ester (MAA–NHS) monomers and Biotin–NHS molecules were first synthesized via Steglich esterification

Summary

Introduction

Nanoparticle-based drug delivery systems have been used for cancer therapy for several decades. Among these nanocarriers, polymeric nanoparticles showed more stable and easy preparation by various manufacturing methods [1]. Polymeric nanoparticles with good design could evade recognition by the reticuloendothelial system (RES) and prolong the circulation time in blood vessels [2], resulting in increasing tumor-targeting probability by enhanced permeability and retention (EPR) effects [2]. Polymeric nanoparticles conjugated with targeting ligands (such as biotin [3], folate [4], transferring [5], and glucose [6]) enhanced tumor accumulation, and improved cancer internalization.

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