title: Physicochemical characterization and in vivo evaluation of solid self-nanoemulsifying drug delivery system for oral administration of docetaxel.
abstract: To formulate a self-nanoemulsifying drug delivery system (SNEDDS) for the oral administration of docetaxel as an alternative to commercial docetaxel-loaded injectable products, it was prepared by spray-drying an aqueous solution containing liquid SNEDDS and colloidal silica. Its physicochemical properties and oral bioavailability were investigated compared to a clear docetaxel solution administered intravenously or orally to rats. In the docetaxel-loaded solid SNEDDS prepared with colloidal silica, the liquid SNEDDS composed of Capryol 90, Cremophore EL and Transcutol HP (45/35/20, volume ratio) was absorbed inside the pores of carriers, and docetaxel was present in a changed amorphous state. The solid SNEDDS with 3.3% (w/v) docetaxel produced nanoemulsions, and showed about 12.5% absolute bioavailability in rats. Thus, this solid SNEDDS may be a potential candidate for oral pharmaceutical product with improved oral bioavailability of docetaxel.
authors.affiliation: College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.
authors.forename: Qizhe
authors.initials: Q
authors.lastname: Quan
authors.forename: Dong-Wuk
authors.initials: DW
authors.lastname: Kim
authors.forename: Nirmal
authors.initials: N
authors.lastname: Marasini
authors.forename: Dae Hwan
authors.initials: DH
authors.lastname: Kim
authors.forename: Jin Ki
authors.initials: JK
authors.lastname: Kim
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; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D000077143:Docetaxel; D016503:Drug Delivery Systems; D004655:Emulsions; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D017207:Rats, Sprague-Dawley; D012822:Silicon Dioxide / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D043823:Taxoids / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004655:Emulsions; D043823:Taxoids; D000077143:Docetaxel; D012822:Silicon Dioxide