EGDMA- and TRIM-Based Microparticles Imprinted with 5-Fluorouracil for Prolonged Drug Delivery.

Michał Cegłowski,Aleksandra Lusina,Joanna Kurczewska,Tomasz Nazim,Piotr Ruszkowski

doi:10.3390/polym14051027

Michał Cegłowski, Aleksandra Lusina + Show 3 more

Open Access

https://doi.org/10.3390/polym14051027

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Abstract

Imprinted materials possess designed cavities capable of forming selective interactions with molecules used in the imprinting process. In this work, we report the synthesis of 5-fluorouracil (5-FU)-imprinted microparticles and their application in prolonged drug delivery. The materials were synthesized using either ethylene glycol dimethacrylate (EGDMA) or trimethylolpropane trimethacrylate (TRIM) cross-linkers. For both types of polymers, methacrylic acid was used as a functional monomer, whereas 2-hydroxyethyl methacrylate was applied to increase the final materials’ hydrophilicity. Adsorption isotherms and adsorption kinetics were investigated to characterize the interactions that occur between the materials and 5-FU. The microparticles synthesized using the TRIM cross-linker showed higher adsorption properties towards 5-FU than those with EGDMA. The release kinetics was highly dependent upon the cross-linker and pH of the release medium. The highest cumulative release was obtained for TRIM-based microparticles at pH 7.4. The IC50 values proved that 5-FU-loaded TRIM-based microparticles possess cytotoxic activity against HeLa cell lines similar to pure 5-FU, whereas their toxicity towards normal HDF cell lines was ca. three times lower than for 5-FU.

Highlights

Drug delivery systems (DDS) are sophisticated technologies that allow targeted delivery of particular pharmaceutical or controlled therapeutic agents’ release
The stretching and bending O-H vibrations of carboxyl groups originating from Methacrylic acid (MAA) can be observed at 3562 and 1389 cm−1, respectively
These bands overlap with O-H stretching, and bending vibrations originated from hydroxyl groups of hydroxyethyl methacrylate (HEMA)

Summary

Introduction

Drug delivery systems (DDS) are sophisticated technologies that allow targeted delivery of particular pharmaceutical or controlled therapeutic agents’ release. The design, synthesis, and production of new substances and materials that can be applied to prepare new DDS have become a major topic of many research groups. Their goal is to develop a DDS which would allow drug administration to a specific site with a known quantity and for a precise amount of time. It is, necessary to produce DDS that, as well as their metabolites, show no toxicity and are removed from the human body [1–3]

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