pH-responsive biocompatible fluorescent polymer nanoparticles based on phenylboronic acid for intracellular imaging and drug delivery

Abstract

To address current medical challenges, there is an urgent need to develop drug delivery systems with multiple functions, such as simultaneous stimuli-responsive drug release and real-time imaging. Biocompatible polymers have great potential for constructing smart multifunctional drug-delivery systems through grafting with other functional ligands. More importantly, novel biocompatible polymers with intrinsic fluorescence emission can work as theranostic nanomedicines for real-time imaging and drug delivery. Herein, we developed a highly fluorescent nanoparticle based on a phenylboronic acid-modified poly(lactic acid)-poly(ethyleneimine)(PLA-PEI) copolymer loaded with doxorubicin (Dox) for intracellular imaging and pH-responsive drug delivery. The nanoparticles exhibited superior fluorescence properties, such as fluorescence stability, no blinking and excitation-dependent fluorescence behavior. The Dox-loaded fluorescent nanoparticles showed pH-responsive drug release and were more effective in suppressing the proliferation of MCF-7 cells. In addition, the biocompatible fluorescent nanoparticles could be used as a tool for intracellular imaging and drug delivery, and the process of endosomal escape was traced by real-time imaging. These pH-responsive and biocompatible fluorescent polymer nanoparticles, based on phenylboronic acid, are promising tools for intracellular imaging and drug delivery.

Using hyaluronic acid-functionalized pH stimuli-responsive mesoporous silica nanoparticles for targeted delivery to CD44-overexpressing cancer cells

“…9 When these nanomaterials are developed as drug delivery systems, drawbacks are encountered such as drug leakage, 10 nonspecific targeting effects, 11 difficulties in monitoring cellular events after drug delivery, etc. 12 Therefore, the design and development of smart drug delivery systems with multiple functions, such as simultaneous stimuli-responsive drug release and targeting to tumor cell, are becoming increasingly urgent. Various stimuli, such as temperature, photoirradiation, enzymes, and pH levels have been applied as triggers to release encapsulated drugs.…”

Microfluidic Devices in Fabricating Nano or Micromaterials for Biomedical Applications

“…Studies on the cytotoxicity and permeability of the CDs on human embryonic kidney cells established that their adsorption on cells has no impact on cellular morphology . Apart from CDs, fluorescence polymers are another biocompatible candidate for cellular imaging . Fluorescent polyethylenimine nanoparticles about 10 nm in diameter, with significantly reduced cytotoxicity against MCF‐7 breast cancer cells and being devoid of extended conjugated structures, have been prepared in a VFD microfluidic platform (Figure c) .…”

Phenylboronic acid-decorated polymeric nanomaterials for advanced bio-application

“…The pH-sensitive interaction between PBA and diphenol is always used in the stimuli-responsive drug delivery systems [87][88][89]. Li et al developed a DOX-loaded fluorescent nanoparticle based on the installed boronic acid- [91].…”

“…Schematic illustration for the formulation of FBNPs-DOX nanoparticles and pH-responsive DOX release. Reproduced with permission from[89]. Copyright 2014, The Royal Society of Chemistry modified poly(lactic acid)-poly(ethyleneimine)(PLA-PEI) copolymers for intracellular imaging and pH-responsive drug delivery[89].…”