title: Spray-dried Eudragit® L100 microparticles containing ferulic acid: Formulation, in vitro cytoprotection and in vivo anti-platelet effect.
abstract: This paper aimed to obtain new spray-dried microparticles containing ferulic acid (FA) prepared by using a methacrylic polymer (Eudragit® L100). Microparticles were intended for oral use in order to provide a controlled release, and improved in vitro and in vivo biological effects. FA-loaded Eudragit® L100 microparticles were obtained by spray-drying. Physicochemical properties, in vitro cell-based effects, and in vivo platelet aggregation were investigated. FA-loaded Eudragit® L100 microparticles were successfully prepared by spray-drying. Formulations showed suitable encapsulation efficiency, i.e. close to 100%. Microparticles were of spherical and almost-spherical shape with a smooth surface and a mean diameter between 2 and 3μm. Fourier-transformed infrared spectra demonstrated no chemical bond between FA and polymer. X-ray diffraction and differential scanning calorimetry analyses indicated that microencapsulation led to drug amorphization. FA-loaded microparticles showed a slower dissolution rate than pure drug. The chosen formulation demonstrated higher in vitro cytoprotection, anti-inflammatory and immunomodulatory potential and also improved in vivo anti-platelet effect. These results support an experimental basis for the use of FA spray-dried microparticles as a feasible oral drug delivery carrier for the controlled release of FA and improved cytoprotective and anti-platelet effects.
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil.
authors.forename: Jessica Mendes
authors.initials: JM
authors.lastname: Nadal
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil.
authors.forename: Mona Lisa Simionatto
authors.initials: MLS
authors.lastname: Gomes
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Débora Maria
authors.initials: DM
authors.lastname: Borsato
authors.affiliation: Postgraduate Program in Chemistry, Department of Chemistry, Federal University of Paraná, Brazil.
authors.forename: Martinha Antunes
authors.initials: MA
authors.lastname: Almeida
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil.
authors.forename: Fernanda Malaquias
authors.initials: FM
authors.lastname: Barboza
authors.affiliation: Postgraduate Program in Chemistry, Department of Chemistry, Federal University of Paraná, Brazil.
authors.forename: Sônia Faria
authors.initials: SF
authors.lastname: Zawadzki
authors.affiliation: Postgraduate Program in Biomedical Science, Department of General Biology, State University of Ponta Grossa, Brazil.
authors.forename: Carla Cristine
authors.initials: CC
authors.lastname: Kanunfre
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil. Electronic address: pvfarago@gmail.com.
authors.forename: Paulo Vitor
authors.initials: PV
authors.lastname: Farago
authors.affiliation: Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil.
authors.forename: Sandra Maria Warumby
authors.initials: SMW
authors.lastname: Zanin
mesh_terms: D000179:Acrylates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D002460:Cell Line; D003373:Coumaric Acids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D019610:Cytoprotection / Q000187:drug effects*; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D010975:Platelet Aggregation Inhibitors; D011108:Polymers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000179:Acrylates; D003373:Coumaric Acids; D004337:Drug Carriers; C477020:Eudragit E100; D010975:Platelet Aggregation Inhibitors; D011108:Polymers; C004999:ferulic acid
keywords: Anti-inflammatory; Antioxidant; Methacrylic polymer; Phytoalexin; Platelet aggregation