Microfluidic-assisted synthesis of multifunctional iodinated contrast agent polymeric nanoplatforms

Enrica Chiesa, Antonietta Greco, Rossella Dorati, Bice Conti, Giovanna Bruni, Dimitrios Lamprou*, Ida Genta*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Contrast InducedNephropathy is the most severe side-effect arising after non-ionic iodinatedcontrast agents (CAs) intravenous administration. The use of antioxidants (i.e.,N-Acetylcysteine; NAC) is one of the attempted prevention approaches. Herein,we describe the microfluidic-assisted synthesis of iodinated polymericnanoparticles (NPs) as new multifunctional blood pool CA. The aim of thisresearch is to co-encapsulate Iohexol (IOX; iodinated CA) and NAC (preventiveagent) into poly-D,L-lactide-co-glycolide (PLGA) and PEGylated-PLGA (PLGA-PEG)NPs to exploit CA diagnostic proprieties and NAC preventing antioxidantactivity. A microfluidic-assisted nanoprecipitation protocol has been set-up forPLGA and PLGA-PEG NPs, evaluating the effect of formulation and microfluidicparameters by analysing the size, PDI and IOX and NAC encapsulation efficiency.The optimized NPs (PLGA-PEG, L:G 50:50, 5% PEG, Mw 90 kDa) formulated with a  size of 67±2.8 nm with PDI<0.2, sphericalshape, and an IOX and NAC encapsulation efficiency of 38% and 20%,respectively. The IOX and NAC encapsulation was confirmed by FTIR and DSC. Invitro release study showed an IOX retention into the polymeric matrix andNAC sustained release up to 24-48h stating microfluidics aspowerful tool for the formulation of multifunctional nanoplatforms. Finally, the protective effect ofNPs and NAC were preliminary assessed on human kidney cells. 

Original languageEnglish
Article number120447
JournalInternational Journal of Pharmaceutics
Volume599
Early online date05 Mar 2021
DOIs
Publication statusPublished - 15 Apr 2021

Keywords

  • contrast-induced nephropathy
  • multifunctional contrast agent
  • iohexol
  • N-acetylcysteine
  • Microfluidics
  • PLGA
  • Nanoparticles

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