title: Evidence of oral translocation of anionic G6.5 dendrimers in mice.
abstract: Development of carrier systems to improve oral bioavailability and target drugs to specific sites continues to be an unmet need. The goal of this study was to evaluate the potential of anionic generation (G) 6.5 poly(amido amine) (PAMAM) dendrimers in oral drug delivery by assessing their in vivo oral translocation. G6.5-COOH dendrimers were characterized for their physiochemical characteristics and acute oral toxicity was assessed in CD-1 mice. The dendrimers were labeled with (125)I and their stability evaluated. Oral bioavailability was assessed in the same mouse model. Investigation of the radioactivity profile in plasma revealed presence of both large and small molecular weight compounds. Detailed area under the curve analysis suggests an effective 9.4% bioavailability of radiolabeled marker associated with G6.5-COOH. Results reported here suggest the potential of dendrimers in permeating gastrointestinal barriers in vivo.
authors.affiliation: Department of Bioengineering, University of Utah , Salt Lake City, Utah 84112, USA.
authors.forename: Giridhar
authors.initials: G
authors.lastname: Thiagarajan
authors.forename: Shraddha
authors.initials: S
authors.lastname: Sadekar
authors.forename: Khaled
authors.initials: K
authors.lastname: Greish
authors.forename: Abhijit
authors.initials: A
authors.lastname: Ray
authors.forename: Hamidreza
authors.initials: H
authors.lastname: Ghandehari
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D050091:Dendrimers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D007422:Intestines / Q000737:chemistry; D051379:Mice; D013270:Stomach / Q000737:chemistry
chemical_list: D050091:Dendrimers; D004337:Drug Carriers; C104700:PAMAM Starburst