Abstract

Bowl-shaped biodegradable polymersomes, or stomatocytes, have much potential as drug delivery systems, due to their intriguing properties, such as controllable size, programmable morphology, and versatile cargo encapsulation capability. In this contribution, we developed well-defined therapeutically active stomatocytes with aggregation-induced emission (AIE) features by self-assembly of biodegradable amphiphilic block copolymers, comprising poly(ethylene glycol) (PEG) and AIEgenic poly(trimethylene carbonate) (PTMC) moieties. The presence of the AIEgens endowed the as-prepared stomatocytes with intrinsic fluorescence, which was employed for imaging of cellular uptake of the particles. It simultaneously enabled the photo-mediated generation of reactive oxygen species (ROS) for photodynamic therapy. The potential of the therapeutic stomatocytes as cargo carriers was demonstrated by loading enzymes (catalase and glucose oxidase) in the nanocavity, followed by a cross-linking reaction to achieve stable encapsulation. This provided the particles with a robust motile function, which further strengthened their therapeutic effect. With these unique features, enzyme-loaded AIEgenic stomatocytes are an attractive platform to be exploited in the field of nanomedicine.

Highlights

  • Supramolecular polymeric nano-architectures, such as polymersomes and micelles, have attracted considerable interest for a wide range of applications, including the field of nanomedicine, due to their tunable morphology and well-defined functionality [1,2,3]

  • The TMC monomers were equipped with a reactive pentafluorophenyl ester substituent, which could be conveniently substituted with the AIEgenic moieties (PEG44 -P(AIE)14 )

  • The bowl-shaped aggregation-induced emission (AIE) stomatocyte morphology was attained by controlling the dialysis conditions

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Summary

Introduction

Supramolecular polymeric nano-architectures, such as polymersomes and micelles, have attracted considerable interest for a wide range of applications, including the field of nanomedicine, due to their tunable morphology and well-defined functionality [1,2,3]. Besides the hydrophilic lumen and hydrophobic membrane that all types of polymersomes contain, and that allows the respective encapsulation of hydrophilic and hydrophobic cargoes, they have an additional nanocavity, which is in direct contact with the outside environment. This cavity has, in previous reports, been loaded with a large variety of cargoes, such as inorganic functional nanoparticles (i.e., Pt and MnO2 ) [4,5,6], bio-organic catalysts (i.e., enzyme molecules) [7,8], therapeutic payloads (i.e., chemotherapeutic drugs and photosensitizers) [9], and fluorescent dyes [10]. The AIEgenic moieties attain their fluorescence in the aggregated state, and show higher resistance against

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