title: Inhibition of Photodegradation of Highly Dispersed Folic Acid Nanoparticles by the Antioxidant Effect of Transglycosylated Rutin.
abstract: We developed highly dispersible and photostable nanoparticles of vitamin, folic acid (FA). FA was wet bead milled with milling and dispersing adjuvants and transglycosylated compounds such as α-glucosyl hesperidin (Hesperidin-G) and rutin (Rutin-G), which solubilized FA. The milled slurries of FA particles with transglycosylated compounds consisted of nanosized particles with a median diameter of <100 nm. The lyophilized formulations of these slurries retained their nanometer size after resuspension in water with no aggregation. The apparent solubility of FA in these formulations was 100-fold higher than that of untreated FA. The solubilizing effect of Rutin-G may affect the particle size reduction and dispersibility of FA. The photostability results showed that the strong antioxidant activity of Rutin-G substantially increased the photostability of FA solution. On the basis of these results, bead milling of FA with Rutin-G is a promising technique for developing highly dispersible, photostable nanoparticle FA formulations.
authors.affiliation: Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Kazunori
authors.initials: K
authors.lastname: Kadota
authors.affiliation: Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Kumi
authors.initials: K
authors.lastname: Semba
authors.affiliation: Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Ryosuke
authors.initials: R
authors.lastname: Shakudo
authors.affiliation: Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Sato
authors.affiliation: Department of Chemical Engineering and Materials Science, Doshisha University , 1-3 Miyakodani, Tatara, Kyotanabe, Kyoto 610-0321, Japan.
authors.forename: Yuto
authors.initials: Y
authors.lastname: Deki
authors.affiliation: Department of Chemical Engineering and Materials Science, Doshisha University , 1-3 Miyakodani, Tatara, Kyotanabe, Kyoto 610-0321, Japan.
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Shirakawa
authors.affiliation: Osaka University of Pharmaceutical Sciences , 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Tozuka
mesh_terms: D000975:Antioxidants / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005079:Excipients / Q000494:pharmacology; D005492:Folic Acid / Q000378:metabolism*; D005612:Freeze Drying; D005960:Glucosides / Q000378:metabolism*; D006569:Hesperidin / Q000031:analogs & derivatives* / Q000378:metabolism; D053758:Nanoparticles; D010782:Photolysis / Q000187:drug effects; D012431:Rutin; D012995:Solubility; D014867:Water
chemical_list: D000975:Antioxidants; D005079:Excipients; D005960:Glucosides; D014867:Water; C487382:glucosyl hesperidin; D012431:Rutin; D005492:Folic Acid; D006569:Hesperidin
keywords: antioxidant activity; bead milling; folic acid; transglycosylated rutin