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

Autor: Nadal JM; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil., Gomes MLS; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil., Borsato DM; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil., Almeida MA; Postgraduate Program in Chemistry, Department of Chemistry, Federal University of Paraná, Brazil., Barboza FM; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil., Zawadzki SF; Postgraduate Program in Chemistry, Department of Chemistry, Federal University of Paraná, Brazil., Kanunfre CC; Postgraduate Program in Biomedical Science, Department of General Biology, State University of Ponta Grossa, Brazil., Farago PV; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmaceutical Sciences, State University of Ponta Grossa, Brazil. Electronic address: pvfarago@gmail.com., Zanin SMW; Postgraduate Program in Pharmaceutical Sciences, Department of Pharmacy, Federal University of Paraná, Brazil.
Jazyk: angličtina
Zdroj: Materials science & engineering. C, Materials for biological applications [Mater Sci Eng C Mater Biol Appl] 2016 Jul 01; Vol. 64, pp. 318-328. Date of Electronic Publication: 2016 Mar 28.
DOI: 10.1016/j.msec.2016.03.086
Abstrakt: 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.
(Copyright © 2016 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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