title: TNF-α blocker effect of naringenin-loaded sericin microparticles that are potentially useful in the treatment of psoriasis.
abstract: This study aims to evaluate the effect of combined use of the racemic flavanone Naringenin (NRG) and the protein sericin as TNF-α blockers. Sericin (SMs) and (R/S) NRG-loaded Sericin (SNRGMs) microparticles were prepared by spray-drying, characterized in terms of morphology and particle size distribution, and encapsulation efficiency was determined. Concerning morphology and particle size distribution of microparticles, results indicated that they were not affected by the presence of NRG. The encapsulation efficiency was almost quantitative (93%), thus proving that sericin can be advantageously loaded with (R/S) NRG. Biological evaluation of (R/S) NRG, SMs and SNRGMs was then performed in lipopolysaccharide (LPS)-stimulated human peripheral blood mononuclear cells (hPBMC). SNRGMs resulted cytotoxic at the higher dose used (200 μg/mL) and the effect was greater than (R/S) NRG alone. Moreover, even if sericin alone was not effective in suppressing LPS-induced serum TNF-α levels, SNRGMs loaded with 9.3% of (R/S) NRG were significantly more potent than (R/S) NRG alone. In summary, this study provides the proof of concept that sericin-based microspheres loaded with TNF-α-blockers could contribute to the down regulation of the cytokine and represents the starting point for the development of new topical formulations for the treatment of middle-stage psoriasis.
authors.affiliation: Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Cell Delivery System Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy. theodora.chlapanidas@unipv.it.
authors.forename: Theodora
authors.initials: T
authors.lastname: Chlapanidas
authors.affiliation: Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Cell Delivery System Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy. sara.perteghella@unipv.it.
authors.forename: Sara
authors.initials: S
authors.lastname: Perteghella
authors.affiliation: Italfarmaco Research Center, Via dei Lavoratori 54, 20092 Cinisello Balsamo, Italy. f.leoni@italfarmaco.com.
authors.forename: Flavio
authors.initials: F
authors.lastname: Leoni
authors.affiliation: Innovhub, Stazioni Sperimentali per l'Industria, Divisione Seta, Via Giuseppe Colombo 83, 20133 Milan, Italy. silvio.farago@mi.camcom.it.
authors.forename: Silvio
authors.initials: S
authors.lastname: Faragò
authors.affiliation: Struttura Semplice Tissue Therapy, Niguarda Hospital, Piazza dell'Ospedale Maggiore 3, 20162 Milan, Italy. mario.marazzi@ospedaleniguarda.it.
authors.forename: Mario
authors.initials: M
authors.lastname: Marazzi
authors.affiliation: Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Medicinal Chemistry Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy. daniela.rossi@unipv.it.
authors.forename: Daniela
authors.initials: D
authors.lastname: Rossi
authors.affiliation: Department of Earth and Environmental Sciences, University of Pavia, Via S. Epifanio 14, 27100 Pavia, Italy. emanuela.martino@unipv.it.
authors.forename: Emanuela
authors.initials: E
authors.lastname: Martino
authors.affiliation: Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Medicinal Chemistry Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy. raffaella.gaggeri@unipv.it.
authors.forename: Raffaella
authors.initials: R
authors.lastname: Gaggeri
authors.affiliation: Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Medicinal Chemistry Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy. simona.collina@unipv.it.
authors.forename: Simona
authors.initials: S
authors.lastname: Collina
mesh_terms: D002478:Cells, Cultured; D002626:Chemistry, Pharmaceutical; D016207:Cytokines / Q000378:metabolism; D015536:Down-Regulation / Q000187:drug effects; D044950:Flavanones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D008070:Lipopolysaccharides / Q000633:toxicity; D008863:Microspheres; D010316:Particle Size; D011565:Psoriasis / Q000188:drug therapy*; D047030:Sericins / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D016207:Cytokines; D044950:Flavanones; D008070:Lipopolysaccharides; D047030:Sericins; D014409:Tumor Necrosis Factor-alpha; C005273:naringenin
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