Chitosan/sulfobutylether-β-cyclodextrin based nanoparticles coated with thiolated hyaluronic acid for indomethacin ophthalmic delivery

Fabrizio Ricci, Giuseppe Francesco Racaniello, Angela Lopedota, Valentino Laquintana, Ilaria Arduino, Antonio Lopalco, Annalisa Cutrignelli, Massimo Franco, Hakon Hrafn Sigurdsson, Nunzio Denora*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

Indomethacin (IND) is topically administered for the treatment of the anterior segment diseases such as conjunctivitis, uveitis, and inflammation prevention for post-cataract surgery, as well as posterior segment diseases as macular edema. Currently IND is available as 0.1% w/v hydroxypropyl-β-cyclodextrin-based eye drop formulation and its bioavailability is limited by several drawbacks such as the nasolacrimal duct draining, the reflex blinking and the low volume of the conjunctival sac. In this study, chitosan (CS)/sulfobutylether-β-cyclodextrin (SBE-β-CD) based nanoparticles (NPs) with a mean diameter of 340 (±7) nm, a ζ-potential value of +18.3 (±0.5) mV and coated with thiolated low molecular weight hyaluronic acid were formulated to improve both the solubility and the residential time in the conjunctival sac of the loaded drug IND. The NPs were prepared through the ionotropic gelation technique, exploiting the interaction between the positively charged amino group of CS and the negatively charged sulfonic group of SBE-β-CD. The mucoadhesive properties of the NPs were evaluated on chicken trachea and esophagus tissues using a texture analyser. The irritability effects of NPs were disclaimed with Hecam test. The developed coated NPs showed increased residential time in the conjunctival sac, displayed no irritancy or toxicity for local administration, making them an optimal and innovative drug delivery system for the treatment of anterior segment inflammation diseases. On the other hand, the uncoated NPs displayed better permeating properties since they are smaller and could be further exploited for the treatment of posterior segment diseases.

Original languageEnglish
Article number121905
Pages (from-to)121905
JournalInternational Journal of Pharmaceutics
Volume622
DOIs
Publication statusPublished - 1 Jun 2022

Bibliographical note

Funding Information:
Authors would like to thank Primex ehf. (Iceland) to provide us with ChitoClear Chitosan and Siciliani SPA (Palo, (BA), Italy) for the bovine's eyes. The University of Bari “Aldo Moro” (Italy) is also gratefully acknowledged.

Publisher Copyright:
© 2022 Elsevier B.V.

Other keywords

  • Coating
  • Cyclodextrins
  • DDS
  • Indomethacin
  • Mucoadhesion
  • Nanoparticles
  • Ophthalmic
  • Thiolated hyaluronic acid
  • Hyaluronic Acid
  • Humans
  • Inflammation
  • Drug Carriers
  • beta-Cyclodextrins
  • Chitosan
  • Drug Delivery Systems/methods

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