TNF-α Blocker Effect of Naringenin-Loaded Sericin Microparticles that Are Potentially Useful in the Treatment of Psoriasis

International Journal of Molecular Sciences

Theodora Chlapanidas⁴  Sara Perteghella⁴  Flavio Leoni⁵  Silvio Faragò⁶  Mario Marazzi³  Daniela Rossi¹  Emanuela Martino²  Raffaella Gaggeri¹ 

[1] Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Medicinal Chemistry Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy; E-Mails:;Department of Earth and Environmental Sciences, University of Pavia, Via S. Epifanio 14, 27100 Pavia, Italy; E-Mail:;Struttura Semplice Tissue Therapy, Niguarda Hospital, Piazza dell’Ospedale Maggiore 3, 20162 Milan, Italy; E-Mail:;Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section (MCPTS), Cell Delivery System Laboratory, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy; E-Mails:;Italfarmaco Research Center, Via dei Lavoratori 54, 20092 Cinisello Balsamo, Italy; E-Mail:;Innovhub, Stazioni Sperimentali per l’Industria, Divisione Seta, Via Giuseppe Colombo 83, 20133 Milan, Italy; E-Mail:

关键词: flavanones;    Naringenin;    sericin;    microparticles;    psoriasis;    anti-inflammatory activity;    TNF-α;   

DOI  :  10.3390/ijms150813624

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.