Microencapsulated Multifunctionalized Graphene Oxide Equipped with Chloroquine for Efficient and Sustained siRNA Delivery

Biomed Res Int. 2022 Apr 6:2022:5866361. doi: 10.1155/2022/5866361. eCollection 2022.

Abstract

A multifunctionalized graphene oxide (GO)-based carrier with conjugation of aminated-polyethylene glycol (PEG-diamine), octaarginine (R8), and folic acid (FA), which also contains chloroquine (CQ), a lysosomotropic agent, is introduced. The cellular uptake mechanisms and intracellular targeting of FA-functionalized nanocarriers are examined. The localized releases of CQ and siRNA intracellular delivery are evaluated. Microencapsulation of the nanocarrier complexed with genes in layer-by-layer coating of alginate microbeads is also investigated. The covalently coconjugated FA with PEG and R8 provides a stable formulation with increased cellular uptake compared to FA-free carrier. The CQ-equipped nanocarrier shows a 95% release of CQ at lysosomal pH. The localized release of the drug inside the lysosomes is verified which accelerates the cargo discharge into cytoplasm.

MeSH terms

  • Chloroquine* / pharmacology
  • Drug Carriers
  • Folic Acid
  • Graphite*
  • Polyethylene Glycols
  • RNA, Small Interfering / genetics

Substances

  • Drug Carriers
  • RNA, Small Interfering
  • graphene oxide
  • Polyethylene Glycols
  • Graphite
  • Chloroquine
  • Folic Acid