title: Spreading and retention of vaginal formulations in post-menopausal women as assessed by gamma scintigraphy.
abstract: OBJECTIVE
  In this paper we report on the first scintigraphic evaluation of vaginal dosage forms in post-menopausal women. To date, almost nothing is known about the in vivo performance of pharmaceutical formulations in the human vagina, which is a major deficiency in the rational design of drug delivery systems for both existing and new indications.
  
  
  METHODS
  The vaginal spreading and clearance of a radiolabelled pessary formulation and Replens (polycarbophil) gel, was assessed in six healthy, post-menopausal female volunteers over a six hour period using the technique of gamma scintigraphy.
  
  
  RESULTS
  In five out of the six subjects studied, clearance of the two formulations exhibited very little intra-subject variation. However, there was considerable inter-subject variability in clearance; in Subject 5 circa 80% of the products were retained whilst in Subject 2 less than 2% was present at the end of the six hour imaging period. Importantly, there was no evidence to suggest that either of the formulations dispersed material beyond the cervix, into the uterus, in any of the subjects studied.
  
  
  CONCLUSIONS
  The lack of significant retention of these products in most of the volunteers has obvious implications for the delivery of therapeutic agents. This study shows that gamma scintigraphy is an invaluable technique with which to assess novel formulations aimed at optimising retention in the vagina for topical or systemic drug delivery.
authors.affiliation: Pharmaceutical Profiles Limited, Nottingham, U.K.
authors.forename: J
authors.initials: J
authors.lastname: Brown
authors.forename: G
authors.initials: G
authors.lastname: Hooper
authors.forename: C J
authors.initials: CJ
authors.lastname: Kenyon
authors.forename: S
authors.initials: S
authors.lastname: Haines
authors.forename: J
authors.initials: J
authors.lastname: Burt
authors.forename: J M
authors.initials: JM
authors.lastname: Humphries
authors.forename: S P
authors.initials: SP
authors.lastname: Newman
authors.forename: S S
authors.initials: SS
authors.lastname: Davis
authors.forename: R A
authors.initials: RA
authors.lastname: Sparrow
authors.forename: I R
authors.initials: IR
authors.lastname: Wilding
mesh_terms: D000282:Administration, Intravaginal; D000328:Adult; D018592:Cross-Over Studies; D005260:Female; D006801:Humans; D008055:Lipids; D008153:Lubrication; D008875:Middle Aged; D010570:Pessaries; D017698:Postmenopause; D011877:Radionuclide Imaging; D014621:Vagina / Q000000981:diagnostic imaging / Q000378:metabolism*; D014622:Vaginal Creams, Foams, and Jellies / Q000008:administration & dosage / Q000493:pharmacokinetics*
chemical_list: D008055:Lipids; C085472:Replens; D014622:Vaginal Creams, Foams, and Jellies