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

Author(s)

Rampelotto, Camila Reck ^[1] ; Pereira, Viviane Goncalves ^[2] ; Silveira, Larissa da Silva ^[3] ; Rossato, Aline ^[3] ; Machado, Alencar Kolinski ^[3] ; Sagrillo, Michele Rorato ^[3] ; Gundel, Andre ^[4] ; Burger, Marilise Escobar ^[5] ; Schaffazick, Scheila Rezende ^[2] ; da Silva, Cristiane de Bona ^{[1, 2]}

Affiliation

^[1] Univ Fed Santa Maria, Ctr Ciencias Saude, Programa Posgrad Ciencias Farmaceut, Santa Maria, RS - Brazil

^[2] Univ Fed Santa Maria, Ctr Ciencias Saude, Dept Farm Ind, Santa Maria, RS - Brazil

^[3] Univ Franciscana, Programa Posgrad Nanociencias, Santa Maria, RS - Brazil

^[4] Univ Fed Pampa, Bage, RS - Brazil

^[5] Univ Fed Santa Maria UFSM, Programa Posgrad Farmacol, Santa Maria, RS - Brazil

• Document type: Journal article
• Source: TOXICOLOGY IN VITRO; v. 78, FEB 2022.
• Web of Science Citations: 0

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. (AU)

• FAPESP's process: 14/50928-2 - INCT 2014: Pharmaceutical Nanotechnology: a transdisciplinary approach
• Grantee: Maria Vitória Lopes Badra Bentley
• Support Opportunities: Research Projects - Thematic Grants