L-Cysteine Modified Chitosan Nanoparticles and Carbon-Based Nanostructures for the Intranasal Delivery of Galantamine

Stavroula G. Nanaki*, Konstantinos Spyrou, Pelagia Veneti, Niki Karouta, Dimitrios Gournis, Turki N. Baroud, Panagiotis Barmpalexis, Dimitrios N. Bikiaris*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

3 Scopus citations

Abstract

The present study evaluates the use of thiolized chitosan conjugates (CS) in combination with two fundamental carbon nanoforms (carbon dots (CDs) and Hierarchical Porous Carbons (HPC)) for the preparation of intranasally (IN) administrated galantamine (GAL) nanoparticles (NPs). Initially, the modification of CS with L-cysteine (Cys) was performed, and the successful formation of a Cys-CS conjugates was verified via 1H-NMR, FTIR, and pXRD. The new Cys-CS conjugate showed a significant solubility enhancement in neutral and alkaline pH, improving CS’s utility as a matrix-carrier for IN drug administration. In a further step, drug-loaded NPs were prepared via solid-oil–water double emulsification, and thoroughly analyzed by SEM, DLS, FTIR and pXRD. The results showed the formation of spherical NPs with a smooth surface, while the drug was amorphously dispersed within most of the prepared NPs, with the exemption of those systems contianing the CDs. Finally, in vitro dissolution release studies revealed that the prepared NPs could prolong GAL’s release for up to 12 days. In sum, regarding the most promising system, the results of the present study clearly suggest that the preparation of NPs using both Cys-CS and CDs results in a more thermodynamically stable drug dispersion, while a zero-order release profile was achieved, which is essential to attain a stable in vivo pharmacokinetic behavior.

Original languageEnglish
Article number4004
JournalPolymers
Volume14
Issue number19
DOIs
StatePublished - Oct 2022

Bibliographical note

Publisher Copyright:
© 2022 by the authors.

Keywords

  • L-cysteine
  • carbon dots
  • drug delivery
  • galantamine
  • modified chitosan
  • nanoparticles
  • porous carbon nanostructures

ASJC Scopus subject areas

  • General Chemistry
  • Polymers and Plastics

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