Spray-dried Eudragit® L100 microparticles containing ferulic acid: Formulation, in vitro cytoprotection and in vivo anti-platelet effect

Nadal, Jéssica Mendes; Gomes, Mona Lisa Simionatto; Borsato, Débora Maria; Almeida, Martinha Antunes; Barboza, Fernanda Malaquias; Zawadzki, Sônia Faria; Kanunfre, Carla Cristine; Farago, Paulo Vítor; Zanin, Sandra Maria Warumby

doi:10.1016/j.msec.2016.03.086

Cited by 22 publications

(15 citation statements)

References 44 publications

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“…PGA-co-PDL/Eudragit MPs loaded IND (1:1.5 wt/wt ratio) showed complete disappearance of PGA-co-PDL characteristic peaks ( Fig.1; Trace D) which was attributed to the efficient coating of Eudragit L-100-55 around PGA-co-PDL particles. Similar behaviour was also observed by (Nadal et al, 2016) who used Eudragit L100 to coat MPs containing ferulic acid using spray drying method.…”

Section: Pga-co-pdl Microparticle/eudragit Characterisationsupporting

confidence: 81%

Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

Tawfeek

Abdellatif

Dennison

et al. 2017

International Journal of Pharmaceutics

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The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying. The produced coated microparticles (PGA-co-PDL-IND/Eudragit) were formulated into optimised FTD using a single station press. The loading, in vitro release, permeability and transport of IND from PGA-co-PDL-IND/Eudragit microparticles was studied in Caco-2 cell lines. IND was efficiently encapsulated (570.15±4.2μg/mg) within the PGA-co-PDL microparticles. In vitro release of PGA-co-PDL-IND/Eudragit microparticles (1:1.5) showed significantly (p<0.05, ANOVA/Tukey) lower release of IND 13.70±1.6 and 56.46±3.8% compared with 1:1 (89.61±2.5, 80.13±2.6%) and 1:0.5 (39.46±0.9 & 43.38±3.12) after 3 and 43h at pH 5.5 and 6.8, respectively. The permeability and transport studies indicated IND released from PGA-co-PDL-IND/Eudragit microparticles had a lower permeability coefficient of 13.95±0.68×10cm/s compared to free IND 23.06±3.56×10cm/s. These results indicate the possibility of targeting anti-inflammatory drugs to the colon using FDTs containing microparticles coated with Eudragit.

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Section: Pga-co-pdl Microparticle/eudragit Characterisationsupporting

confidence: 81%

Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

Tawfeek

Abdellatif

Dennison

et al. 2017

International Journal of Pharmaceutics

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“…H 2 O 2 is well known to act as a potent inducer of reactive oxygen species (ROS) and it is capable of inducing cell injury both in vitro and in vivo. H 2 O 2 is particularly known to induce oxidative damage, leading to lipid peroxidation, ROS generation, depletion in reduced glutathione, and reduction in antioxidant enzyme activity (catalase, superoxide dismutase, and glutathione peroxidase) preceding cell death [26]. Thus, the cytoprotective effect of grape pomace is a great finding in order to suggest the cosmetic use of this raw material due to its high potential in preventing damages caused in dermal cells such as fibroblasts and preventing skin aging.…”

Section: Discussionmentioning

confidence: 99%

“…Twenty-four hours later, the medium was replaced by the MTT solution (0.05 mg•mL −1 ) and cells were incubated for 3 h. The MTT solution was removed, and 100 uL of DMSO was added for the solubilization of formazan crystals. Cytotoxicity was assessed by the microplate reader (Thermo Scientific Multiskan ® FC, Thermo Fisher Scientific, Vantaa, Finland) at 590 nm [26]. The optical density (OD) values were converted to % of cell viability as:…”

Section: Mtt Cytotoxicity Assaymentioning

confidence: 99%

“…Cytoprotection Assay Fibroblast cells were plated in a 96-well plate (1 × 10 3 cells/well). The media was removed 24 h after seeding (except for the negative control group) and the cells were exposed to an acute dose (600 µM) of peroxide (H 2 O 2 ) in phosphate buffered saline (PBS) (hydrogen peroxide concentration that promoted a 50% reduction of cell viability) [26]. After this treatment, the solution with the oxidizing agent was removed, and cell viability was then determined by the MTT method.…”

Section: Mtt Cytotoxicity Assaymentioning

confidence: 99%

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Cytoprotection of Antioxidant Biocompounds from Grape Pomace: Further Exfoliant Phytoactive Ingredients for Cosmetic Products

et al. 2018

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The goal of this study was to investigate the efficacy and the safety of grape pomace (Vitis labrusca L.) obtained from the winemaking process as an antioxidant raw material for cosmetic formulations. Grape pomace was dried and submitted to extraction with solvents. The extracts were filtered and freeze-dried. The extraction carried out with 75% acetone-water showed a better yield (1.9 g·g−1). High performance liquid chromatography (HPLC) analysis confirmed the presence of ellagic acid as an active biocompound in the extracts. The Total phenolic content of freeze-dried extracts reached 69.83 ± 1.02 mg for 75% acetone-water system. Antioxidant activity determined by the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) method revealed there was no statistical difference between the extract (EC50 6.9 ± 0.21) and butylated hydroxytoluene (BHT) (EC50 7.6 ± 0.71). Results of cytotoxicity showed that extracts from grape pomace were safe, even at the highest concentration tested (200 mg·mL−1) against the 3T3 cell line. Scanning Electron Microscopy (SEM) analysis revealed that there were no morphological cell changes of cells treated. Cytoprotection of cells towards the oxidation promoted by the peroxide solution was observed in the lowest concentration tested (0.73 mg·mL−1). Grape pomace from the winemaking process revealed a significant antioxidant activity attributed to its biocompounds. The safety and efficacy of extracts of grape pomace as raw material for cosmetic formulations was proposed through cell culture assays.

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“…In nature, FA is usually found as component of plant cell walls offering linkage with lignin; in arabinoxylans, FA is esterified to the C-5 of αlarabinofuranose; in pectins, it is esterified to the C-2 of α1➔5-linked arabinofuranose or to the C-6 of β1➔4-linked galactopyranose, while in xyloglucans, it is found attached to the C-4 of α-D-xylopyranose 2,3 . FA exhibits a wide range of therapeutic effects against various diseases such as cancer, diabetes, and cardiovascular and neurodegenerative disorders 4 . A wide spectrum of beneficial activities for human health has been proposed for this phenolic compound, at least in part because of its strong antioxidant activity.…”

Section: Introductionmentioning

confidence: 99%

A Simple and High-yield Synthesis of Hexadecyl Ferulate and Its In Vitro Antioxidant Potential

Nadal

Pedroso

Minozzo

et al. 2018

Braz. arch. biol. technol.

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Ferulic acid (FA) is a phenolic compound with well-known antioxidant potential that can be used as a promising anti-inflammatory and anti-cancer molecule. Furthermore, it has been reported to have neuroprotective activity. One of the main problems, which limit its clinical use, is its low bioavailability when administered orally. This limitation can be circumvented by changes in their structure and/or for preparing lipid-based formulations. The aim of this study was to synthesize a derivative of FA, the hexadecyl ferulate (HF). This compound would be more susceptible to pass through blood-brain barrier (BBB) due to its lipophilic character. The HF was obtained by Steglich esterification and yielded 76.77 ± 1.35%. Its structural characterization was performed by spectroscopic methods of Fourier-transformed infrared spectroscopy (FTIR) and nuclear magnetic resonance (NMR). FTIR spectrum of HF presented two typical bands of ester group, a C=O ester stretching band at 1725 cm-1 and a CO stretching band at 1159 cm-1. The 1 H and 13 C spectral data confirmed the chemical structure of HF. Regarding the 13 C NMR spectrum, HF showed a chemical shift at δ 167.39 ppm which corresponded to the carbonyl carbon of the ester group. Concerning the in vitro antioxidant potential, HF had equivalent or improved scavenger activity than FA leading to IC50 values of 0.083 ± 0.009 nmol.mL-1 and 0.027 ± 0.002 nmol.mL-1 in DPPH radical scavenging and ABTS radical cation decolorization assays, respectively. Further studies are required in order to investigate the antioxidant effect of HF in biological media.

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Spray-dried Eudragit® L100 microparticles containing ferulic acid: Formulation, in vitro cytoprotection and in vivo anti-platelet effect

Cited by 22 publications

References 44 publications

Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

Cytoprotection of Antioxidant Biocompounds from Grape Pomace: Further Exfoliant Phytoactive Ingredients for Cosmetic Products

A Simple and High-yield Synthesis of Hexadecyl Ferulate and Its In Vitro Antioxidant Potential

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