Development and characterization of a copolymeric micelle containing soluble and insoluble model drugs

PLoS One. 2023 May 25;18(5):e0286251. doi: 10.1371/journal.pone.0286251. eCollection 2023.

Abstract

Objectives: Micelles are nano-sized particles with a core-shell structure that are made by natural or synthetic polymers or copolymers. The aim of this study was to develop and characterize a copolymeric micelle using two polymers loaded with hydrophilic and lipophilic drugs.

Methods: Poly(ethylene glycol) and poly(ε-caprolactone) (PEG-PCL) were used to form a copolymeric micelle which was further loaded with either moxifloxacin or clarithromycin as hydrophilic and lipophilic drug samples, respectively. Characterization tests were done including fourier transform-infrared (FT-IR) spectroscopy, proton nuclear magnetic resonance (1H NMR) spectroscopy, encapsulation efficiency, particle size, zeta potential, polydispersity index, transmission electron microscopy, and in-vitro release test.

Results: The construction of the copolymer was confirmed by the results of FT-IR and 1H NMR spectroscopy tests. The encapsulation efficiency test exhibited that loading was about 50% for twelve formulations. Particle size, zeta potential, polydispersity index, and transmission electron microscopy confirmed the formation of monodispersed, uniform, and nano-sized micelles with a few negative charges. The kinetic model of release was fitted to the Higuchi model.

Conclusions: Polymeric micelles consisting of PEG-PCL copolymer were loaded with adequate concentrations of hydrophilic (moxifloxacin) and lipophilic (clarithromycin) model drugs, with a mean particle size under 300 nm. Therefore, copolymeric micelles can be used as a suitable drug delivery system for mucous membranes and skin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Clarithromycin*
  • Drug Carriers / chemistry
  • Micelles*
  • Moxifloxacin
  • Particle Size
  • Polyesters / chemistry
  • Polyethylene Glycols / chemistry
  • Polymers / chemistry
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Micelles
  • Clarithromycin
  • Moxifloxacin
  • Polymers
  • Polyethylene Glycols
  • Polyesters
  • Drug Carriers

Grants and funding

This work was financially supported by the Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences and Health Care Services, Yazd, Iran (grant #7369 awarded to F.M.). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.