Chitosan-olive oil microparticles for phenylethyl isothiocyanate delivery: Optimal formulation

Abstract

Phenylethyl isothiocyanate (PEITC), a chemopreventive compound, is highly reactive due to its considerably electrophilic nature. Furthermore, it is hydrophobic and has low stability, bioavailability and bioaccessibility. This restricts its use in biomedical and nutraceutical or food applications. Thus, the encapsulation of this agent has the function of overcoming these limitations, promoting its solubility in water, and stabilizing it, preserving its bioactivity. So, polymeric microparticles were developed using chitosan-olive oil-PEITC systems. For this, an optimisation process (factors: olive oil: chitosan ratio and PEITC: chitosan ratio) was implemented through a 3-level factorial experimental design. The responses were: the particle size, zeta-potential, polydisperse index, and entrapment efficiency. The optimal formulation was further characterised by FTIR and biocompatibility in Caco-2 cells. Optimal conditions were olive oil: chitosan and PEITC: chitosan ratios of 1.46 and 0.25, respectively. These microparticles had a size of 629 nm, a zeta-potential of 32.3 mV, a polydispersity index of 0.329, and entrapment efficiency of 98.49%. We found that the inclusion process affected the optical behaviour of the PEITC, as well as the microparticles themselves and their interaction with the medium. Furthermore, the microparticles did not show cytotoxicity within the therapeutic values of PEITC. Thus, PEITC was microencapsulated with characteristics suitable for potential biomedical, nutraceutical and food applications.

Formulation of a dual drug-loaded nanoparticulate co-delivery hydrogel system and its validation in rheumatoid arthritis animal model

“…The principal absorption peaks related to drugs (PEITC and MTX) showed an isothiocyanate (-N=C=S) peak of PEITC at 2105.69 cm −1 (Coscueta et al., 2021 ) and MTX at 3343.53 cm −1 confirming the presence of the -OH group, and 1645.09 cm −1 corresponding to the –C=C group (Jang et al., 2019 ). A comparison of the FTIR spectra of Free PEITC with DD NP HG FTIR showed a distinctive peak at 2092.83 cm −1 , corresponding to the –N=C=S group, and a peak at 1644.36 cm −1 for the –C=C group.…”

Phenylethyl Isothiocyanate: A Bioactive Agent for Gastrointestinal Health

“…However, PEITC and ITCs micro/nanoencapsulation has been poorly studied [ 63 ]. Till now, cyclodextrin and chitosan microparticles were reported to be plausible carriers for isothiocyanates [ 64 , 65 ]. Besides, PEITC was already stabilized with vegetable oils that protect non-polar isothiocyanates from decomposition or volatilization [ 56 ].…”

Biopolymer from Water Kefir as a Potential Clean-Label Ingredient for Health Applications: Evaluation of New Properties

“…Caco-2 cell line is commonly used to assess the intrinsic cytotoxicity of new materials, drugs, or drug delivery systems [119][120][121]. The results obtained for the in vitro cytotoxicity analysis of the EPSwk are in Figure 6.…”