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Pharmaceutical Research

, Volume 14, Issue 8, pp 1073–1078 | Cite as

Spreading and Retention of Vaginal Formulations in Post-Menopausal Women as Assessed by Gamma Scintigraphy

  • J. Brown
  • G. Hooper
  • C. J. Kenyon
  • S. Haines
  • J. Burt
  • J. M. Humphries
  • S. P. Newman
  • S. S. Davis
  • R. A. Sparrow
  • I. R. Wilding
Article

Abstract

Purpose. 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.

vaginal delivery gamma scintigraphy bioadhesion pessary post-menopausal women 

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REFERENCES

  1. 1.
    J. L. Richardson and L. Illum. Adv. Drug Del. Rev. 8:341–366 (1992)Google Scholar
  2. 2.
    C. J. Elias and L. Heise. Population Council Working Papers 6:1–105 (1993)Google Scholar
  3. 3.
    J. R. Robinson and W. J. Bologna. J. Cont. Rel. 28:87–94 (1994)Google Scholar
  4. 4.
    J. L. Richardson, J. Whetstone, A. N. Fisher, P. Watts, N. F. Farraj, M. Hinchcliffe, L. Benedetti and L. Illum. J. Cont. Rel 42:133–142 (1996)Google Scholar
  5. 5.
    A. Joglekar, C. T. Rhodes and M. Danish. Drug Dev. Ind. Pharm. 17:2103–2113 (1991)Google Scholar
  6. 6.
    G. Meseuguer, R. Gurny and P. Buri. J. Drug Target. 2:269–288 (1994)Google Scholar
  7. 7.
    S. P. Newman, K. P. Steed, J. G. Hardy, I. R. Wilding, G. Hooper and R. A. Sparrow. J. Pharm. Pharmacol. 46:657–660 (1994)Google Scholar
  8. 8.
    I. R. Wilding, C. J. Kenyon, G. Hooper, S. Marshall, J. S. McCracken, S. Chauhan, H. J. Staab and J. Armbrecht. Aliment. Pharmacol. Therapeut. 9:161–166 (1995)Google Scholar
  9. 9.
    I. R. Wilding, A. J. Coupe and S. S. Davis. Adv. Drug Del. Rev. 7:87–117 (1991)Google Scholar
  10. 10.
    S. P. Newman. Critical Reviews in Therapeutic Drug Carrier Systems 10:65–109 (1993)Google Scholar
  11. 11.
    J. L. Richardson, P. A. Ramires, M. R. Miglietta, M. Rochira, L. Bacelle, L. Callegaro and L. Benedetti. Int. J. Pharm. 115:9–15 (1995)Google Scholar
  12. 12.
    P. Britton, P. Flanagan, W. P. Hart and D. Linkin. United States Patent No. 5,458,884 Google Scholar
  13. 13.
    P. Putteman, M. K. J. François and E. C. L. Snoeck. PCT Patent No. WO 95/31178 Google Scholar
  14. 14.
    W. J. Henderson, T. C. Hamilton, M. S. Baylis, C. G. Pierrepoint and K. Griffeths. Environ. Res. 40:247–250 (1986)Google Scholar
  15. 15.
    A. P. Wehner and R. E. Weller. Food Chem. Toxicol. 24:329–338 (1986)Google Scholar

Copyright information

© Plenum Publishing Corporation 1997

Authors and Affiliations

  • J. Brown
    • 1
  • G. Hooper
    • 1
  • C. J. Kenyon
    • 1
  • S. Haines
    • 1
  • J. Burt
    • 1
  • J. M. Humphries
    • 1
  • S. P. Newman
    • 1
  • S. S. Davis
    • 2
  • R. A. Sparrow
    • 3
  • I. R. Wilding
    • 1
  1. 1.Pharmaceutical Profiles LimitedNottinghamU.K
  2. 2.Department of Pharmaceutical SciencesNottingham UniversityU.K
  3. 3.Department of Human MorphologyQueen's Medical CentreNottinghamU.K

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