TY - JOUR
T1 - MCM-41 as a useful vector for rutin topical formulations
T2 - Synthesis, characterization and testing
AU - Berlier, Gloria
AU - Gastaldi, Lucia
AU - Sapino, Simona
AU - Miletto, Ivana
AU - Bottinelli, Emanuela
AU - Chirio, Daniela
AU - Ugazio, Elena
N1 - Funding Information:
Compagnia di San Paolo and Università di Torino are gratefully acknowledged for funding Project ORTO114XNH through “Bando per il finanziamento di progetti di ricerca di Ateneo - anno 2011”. P. Iliade and P. Pretto are gratefully acknowledged for precious help.
PY - 2013
Y1 - 2013
N2 - Rutin, the glycoside of quercetin, could be used in topical preparations because of its antioxidant and radical scavenging properties, but its employ in cosmetic and pharmaceutical products is limited by poor physico-chemical stability. These issues were addressed by preparing, characterizing and testing rutin inclusion complexes with MCM-41 mesoporous silica. The effect of surface functionalization with aminopropyl groups (NH2-MCM-41) on the molecules properties was studied. The organic/inorganic interaction was confirmed by many techniques. In particular, the high inclusion of rutin in the pores of NH2-MCM-41 was assessed by XRD, TGA, gas-volumetric analysis (BET), while FTIR spectroscopy allowed to analyse with great detail the molecular interaction with the inorganic surface. Rutin was stabilized against UV degradation, mostly by its inclusion in NH2-MCM-41. Ex vivo studies showed a greater accumulation in porcine skin in the case of rutin complexed with NH2-MCM-41. Not only antioxidant properties of rutin were maintained after immobilization but, with aminopropyl silica, the metal-chelating activity increased noticeably. The immobilization of rutin in aminopropyl silica resulted in better performance in terms of activity and photostability, suggesting the importance of functionalization in stabilizing organic molecules within silica pores.
AB - Rutin, the glycoside of quercetin, could be used in topical preparations because of its antioxidant and radical scavenging properties, but its employ in cosmetic and pharmaceutical products is limited by poor physico-chemical stability. These issues were addressed by preparing, characterizing and testing rutin inclusion complexes with MCM-41 mesoporous silica. The effect of surface functionalization with aminopropyl groups (NH2-MCM-41) on the molecules properties was studied. The organic/inorganic interaction was confirmed by many techniques. In particular, the high inclusion of rutin in the pores of NH2-MCM-41 was assessed by XRD, TGA, gas-volumetric analysis (BET), while FTIR spectroscopy allowed to analyse with great detail the molecular interaction with the inorganic surface. Rutin was stabilized against UV degradation, mostly by its inclusion in NH2-MCM-41. Ex vivo studies showed a greater accumulation in porcine skin in the case of rutin complexed with NH2-MCM-41. Not only antioxidant properties of rutin were maintained after immobilization but, with aminopropyl silica, the metal-chelating activity increased noticeably. The immobilization of rutin in aminopropyl silica resulted in better performance in terms of activity and photostability, suggesting the importance of functionalization in stabilizing organic molecules within silica pores.
KW - Antiradical activity
KW - Flavonoids
KW - Mesoporous silica nanoparticles
KW - Photostability
KW - Skin permeation
UR - http://www.scopus.com/inward/record.url?scp=84885449132&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2013.09.018
DO - 10.1016/j.ijpharm.2013.09.018
M3 - Article
SN - 0378-5173
VL - 457
SP - 177
EP - 186
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1
ER -