Biocompatible PEO-b-PCL Nanosized Micelles as Drug Carriers: Structure and Drug-Polymer Interactions

Nanomaterials (Basel). 2020 Sep 18;10(9):1872. doi: 10.3390/nano10091872.

Abstract

We report on the preparation of drug nanocarriers by encapsulating losartan potassium (LSR) into amphiphilic block copolymer micelles, utilizing the biocompatible/biodegradable poly(ethylene oxide)-b-poly(ε-caprolactone) (PEO-b-PCL) diblock copolymer. The PEO-b-PCL micelles and LSR-loaded PEO-b-PCL nanocarriers were prepared by organic solvent evaporation method (OSEM). Light scattering and nuclear magnetic resonance (NMR) provide information on micelle structure and polymer-drug interactions. According to dynamic light scattering (DLS) analysis, the PEO-b-PCL micelles and LSR-loaded PEO-b-PCL nanocarriers formed nanostructures in the range of 17-26 nm in aqueous milieu. Attenuated total reflection Fourier transform infrared (ATR-FTIR) and ultraviolet-visible (UV-Vis) measurements confirmed the presence of LSR in the polymeric drug solutions. NMR results proved the successful encapsulation of LSR into the PEO-b-PCL micelles by analyzing the drug-micelles intermolecular interactions. Specifically, 2D-NOESY experiments clearly evidenced the intermolecular interactions between the biphenyl ring and butyl chain of LSR structure with the methylene signals of PCL. Additionally, NMR studies as a function of temperature demonstrated an unexpected, enhanced proton mobility of the PEO-b-PCL micellar core in D2O solutions, probably caused by the melting of the PCL hydrophobic core.

Keywords: amphiphilic block copolymers; drug delivery systems; drug encapsulation; drug–polymer intermolecular interactions; organic solvent evaporation method; polymeric nanocarriers.