Abstract

The engineering of delivery systems for drugs and contrasting labels ensuring the simultaneous imaging and treatment of malignant tumors is an important hurdle in developing new tools for cancer therapy and diagnosis. Polyelectrolyte microcapsules (MCs), formed by nanosized interpolymer complexes, represent a promising platform for the designing of multipurpose agents, functionalized with various components, including high- and low-molecular-weight substances, metal nanoparticles, and organic fluorescent dyes. Here, we have developed size-homogenous MCs with different structures (core/shell and shell types) and microbeads containing doxorubicin (DOX) as a model anticancer drug, and fluorescent semiconductor nanocrystals (quantum dots, QDs) as fluorescent nanolabels. In this study, we suggest approaches to the encapsulation of DOX at different stages of the MC synthesis and describe the optimal conditions for the optical encoding of MCs with water-soluble QDs. The results of primary characterization of the designed microcarriers, including particle analysis, the efficacy of DOX and QDs encapsulation, and the drug release kinetics are reported. The polyelectrolyte MCs developed here ensure a modified (prolonged) release of DOX, under conditions close to normal and tumor tissues; they possess a bright fluorescence that paves the way to their exploitation for the delivery of antitumor drugs and fluorescence imaging.

Highlights

  • Finding efficient systems for the targeted delivery of drugs and contrast agents to tumor growth areas and the stimulus-sensitive release of both drugs and agents is essential; it is at the forefront of the development of theranostic agents for the combined diagnosis and treatment of tumors [1,2]

  • Polyelectrolyte microcapsules (MCs) are versatile polymer microcontainers formed from the interpolymer complexes of oppositely charged polyelectrolytes [3]

  • This study was aimed at designing polyelectrolyte MCs and developing approaches to their functionalization with QDs that are water-solubilized using polyethylene glycol (PEG) derivatives, as well as using DOX as a model antitumor agent that contains hydrophilic moieties

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Summary

Introduction

Finding efficient systems for the targeted delivery of drugs and contrast agents to tumor growth areas and the stimulus-sensitive release of both drugs and agents is essential; it is at the forefront of the development of theranostic agents for the combined diagnosis and treatment of tumors [1,2].Polyelectrolyte microcapsules (MCs) are versatile polymer microcontainers formed from the interpolymer complexes of oppositely charged polyelectrolytes [3]. The main advantage of polyelectrolyte MCs as drug-delivery systems is their capacity for the controlled, stimulus-sensitive release of their functional components in response to a specific trigger, including physical (ultrasound, magnetic field, laser pulse, or optical radiation), chemical (the pH and ionic strength of the microenvironment or solvent polarity), and biochemical (receptors or target cells) triggers [4,5,6,7,8,9,10]. Nano- and microsized calcium carbonate (CaCO3 ) particles of the vaterite type (microbeads (MBs)) are widely used as a substrate for the formation of the polyelectrolyte shell [9,10,12,13,14,15] These particles are Nanomaterials 2021, 11, 3055.

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