title: A semisynthetic Quillaja saponin as a drug delivery agent for aminoglycoside antibiotics.
abstract: OBJECTIVE
  The purpose of this study was to investigate the utility of a purified, semisynthetic saponin, DS-1, prepared by deacylation of a naturally occurring saponin from the bark of the Quillaja saponaria Molina tree, as a permeation enhancer for mucosal delivery of the aminoglycosides, gentamicin and tobramycin.
  
  
  METHODS
  Gentamicin or tobramycin formulations, with and without DS-1, were administered to rats nasally, ocularly, and rectally. Serum aminoglycoside levels following mucosal application were compared with those administered intramuscularly. Gentamicin formulations, with and without DS-1, were administered intranasally to mice 60 minutes after a lethal bacterial challenge. To ascertain nasal irritation potential, DS-1 nosedrops were administered to rats twice daily for 7 days in the right nostril only. Comparison of the left (internal control) and right nostril was made with a control group that received only buffer.
  
  
  RESULTS
  Significant transport across mucous membranes was only observed in formulations containing DS-1. This effect on drug delivery was transient. Administration of an intranasal gentamicin/DS-1 formulation reversed the lethal bacterial challenge in mice, demonstrating that biological activity was retained after absorption. Nasal irritation was not observed in groups receiving DS-1 nosedrops, which were identical to control groups.
  
  
  CONCLUSIONS
  DS-1 has potential as a transmucosal delivery agent for the aminoglycoside antibiotics.
authors.affiliation: Cambridge Biotech Corporation, Worcester, Massachusetts 01605-2376, USA.
authors.forename: J
authors.initials: J
authors.lastname: Recchia
authors.forename: M H
authors.initials: MH
authors.lastname: Lurantos
authors.forename: J A
authors.initials: JA
authors.lastname: Amsden
authors.forename: J
authors.initials: J
authors.lastname: Storey
authors.forename: C R
authors.initials: CR
authors.lastname: Kensil
mesh_terms: D000617:Aminoglycosides / Q000493:pharmacokinetics*; D000818:Animals; D016503:Drug Delivery Systems; D005839:Gentamicins / Q000097:blood; D051381:Rats; D017207:Rats, Sprague-Dawley; D012503:Saponins / Q000378:metabolism*; D014031:Tobramycin / Q000097:blood
chemical_list: D000617:Aminoglycosides; D005839:Gentamicins; D012503:Saponins; D014031:Tobramycin