title: Solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced oral bioavailability of poorly water-soluble tacrolimus: physicochemical characterisation and pharmacokinetics.
abstract: To develop a novel self-nanoemulsifying drug delivery system (solid SNEDDS) with better oral bioavailability of tacrolimus, the solid SNEDDS was obtained by spray-drying the solutions containing the liquid SNEDDS and colloidal silica. Its reconstitution properties were determined and correlated to solid state characterisation of the powder. Moreover, the dissolution and pharmacokinetics in rats was done in comparison to the commercial product. Among the liquid SNEDDS formulations tested, the liquid SNEDDS comprised of Capryol PGMC, Transcutol HP and Labrasol (10:15:75, v/v/v) presented the highest dissolution rate. In the solid SNEDDS, this liquid SNEDDS was absorbed in the pores and attached onto the surface of the colloidal silica. Drug was present in the amorphous state in it. The solid SNEDDS with 5% w/v tacrolimus produced the nanoemulsions and improved the oral bioavailability of tacrolimus in rats. Therefore, this solid SNEDDS would be a potential candidate for enhancing the oral bioavailability of tacrolimus.
authors.affiliation: College of Pharmacy, Yeungnam University , Gyongsan , South Korea .
authors.forename: Youn Gee
authors.initials: YG
authors.lastname: Seo
authors.forename: Dong Wuk
authors.initials: DW
authors.lastname: Kim
authors.forename: Abid Mehmood
authors.initials: AM
authors.lastname: Yousaf
authors.forename: Jong Hyuck
authors.initials: JH
authors.lastname: Park
authors.forename: Pahn-Shick
authors.initials: PS
authors.lastname: Chang
authors.forename: Hyung Hee
authors.initials: HH
authors.lastname: Baek
authors.forename: Soo-Jeong
authors.initials: SJ
authors.lastname: Lim
authors.forename: Jong Oh
authors.initials: JO
authors.lastname: Kim
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Han-Gon
authors.initials: HG
authors.lastname: Choi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics; D004655:Emulsions; D051381:Rats; D012995:Solubility; D016559:Tacrolimus / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D016559:Tacrolimus
keywords: Bioavailability; colloidal silica; self-nanoemulsifying drug delivery system; solid carrier; tacrolimus