Ferulic acid-loaded nanocapsules: Evaluation of mucosal interaction, safety and antioxidant activity in human mononucleated cells

Toxicol In Vitro. 2022 Feb:78:105259. doi: 10.1016/j.tiv.2021.105259. Epub 2021 Oct 16.

Abstract

Ferulic acid (FA) is a phenolic compound that has antioxidant, anti-inflammatory and anticarcinogenic properties besides presenting cytoprotective activity. It has limited oral bioavailability what is a challenge to its therapeutic application. In this way, this investigation aimed to develop FA-loaded nanocapsule suspensions (NC-FA) prepared with ethylcellulose and evaluate their in vitro release profile, mucoadhesion and irritation potential; scavenging capacity, cytotoxicity, cytoprotection and genoprotection against hydrogen peroxide-induced damage in hMNC (human Mononucleated Cells) culture. The nanocapsules presented physicochemical characteristics compatible with colloidal systems (NC-FA: 112 ± 3 nm; NC-B (without FA): 107 ± 3 nm; PdI < 0.2; Span<2.0 and negative zeta potential). In addition, the nanoparticulate system promoted the FA controlled release, increasing the half-life twice through the in vitro dialysis method. NC-FA and NC-B were able to interact with mucin, which is an indicative of mucoadhesive properties and the association of FA with nanocapsules showed decreased irritation by HET-CAM method. Besides, the NC-FA did not present cytotoxicity in hMNC and improved the ATBS radical scavenging capacity. Besides, it prevented, treated and reversed oxidative conditions in a H2O2-induced model in hMNC. Thus, this nanocarrier formulation is promising to perform more preclinical investigations focusing on diseases involving oxidative mechanisms.

Keywords: Alternative methods. Cytotoxicity. Hydroxycinnamic acid. Polymeric nanoparticles. Scavenging capacity.

MeSH terms

  • Animals
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacokinetics
  • Antioxidants / pharmacology
  • Cells, Cultured
  • Cellulose / analogs & derivatives
  • Chick Embryo
  • Coumaric Acids / administration & dosage*
  • Coumaric Acids / pharmacokinetics
  • Coumaric Acids / pharmacology
  • Drug Delivery Systems / methods*
  • Humans
  • Hydrogen Peroxide / toxicity
  • Irritants
  • Lymphocytes
  • Mucins
  • Nanocapsules / adverse effects
  • Nanocapsules / chemistry*

Substances

  • Antioxidants
  • Coumaric Acids
  • Irritants
  • Mucins
  • Nanocapsules
  • ethyl cellulose
  • Cellulose
  • ferulic acid
  • Hydrogen Peroxide