Abstract

Drug carriers based on polyelectrolyte microcapsules remotely controlled with an external magnetic field are a promising drug delivery system. However, the influence of capsule parameters on microcapsules’ behavior in vivo is still ambiguous and requires additional study. Here, we discuss how the processes occurring in the blood flow influence the circulation time of magnetic polyelectrolyte microcapsules in mouse blood after injection into the blood circulatory system and their interaction with different blood components, such as WBCs and RBCs. The investigation of microcapsules ranging in diameter 1–5.5 m allowed us to reveal the dynamics of their filtration by vital organs, cytotoxicity, and hemotoxicity, which is dependent on their size, alongside the efficiency of their interaction with the magnetic field. Our results show that small capsules have a long circulation time and do not affect blood cells. In contrast, the injection of large 5.5 m microcapsules leads to fast filtration from the blood flow, induces the inhibition of macrophage cell line proliferation after 48 h, and causes an increase in hemolysis, depending on the carrier concentration. The obtained results reveal the possible directions of fine-tuning microcapsule parameters, maximizing capsule payload without the side effects for the blood flow or the blood cells.

Highlights

  • Modern systems for targeted drug delivery solve several pharmaceutical problems, protecting the substance from biological media, allowing for the delivery of poorly soluble substances, and ensuring a better distribution of the substance throughout the body and over time

  • The number of magnetite particles was varied using the method of introduction, either label-by-label (LbL) or freezing-induced loading (FIL) [19]

  • Application of the magnetic capsules suggests a systemic administration by injecting the microcapsule suspension into the blood flow, which is followed by targeting the affected area using an external source of magnetic field [4,25]

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Summary

Introduction

Modern systems for targeted drug delivery solve several pharmaceutical problems, protecting the substance from biological media, allowing for the delivery of poorly soluble substances, and ensuring a better distribution of the substance throughout the body and over time. The main advantage of using drug delivery systems is the reduction in the systemic side effects of drug administration through local delivery to the affected area [1] This approach becomes more complicated in the case of drug delivery to soft tissues and the internal parts of the body. In this case, the required drug distribution can be provided by the introduction of carriers into the bloodstream and localization in the affected area by external stimuli. To be attracted and held against the vessel wall, the carriers must be sufficiently sensitive to the magnetic field This requires the Pharmaceutics 2021, 13, 2147.

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