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.
Similar content being viewed by others
REFERENCES
J. L. Richardson and L. Illum. Adv. Drug Del. Rev. 8:341–366 (1992)
C. J. Elias and L. Heise. Population Council Working Papers 6:1–105 (1993)
J. R. Robinson and W. J. Bologna. J. Cont. Rel. 28:87–94 (1994)
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)
A. Joglekar, C. T. Rhodes and M. Danish. Drug Dev. Ind. Pharm. 17:2103–2113 (1991)
G. Meseuguer, R. Gurny and P. Buri. J. Drug Target. 2:269–288 (1994)
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)
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)
I. R. Wilding, A. J. Coupe and S. S. Davis. Adv. Drug Del. Rev. 7:87–117 (1991)
S. P. Newman. Critical Reviews in Therapeutic Drug Carrier Systems 10:65–109 (1993)
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)
P. Britton, P. Flanagan, W. P. Hart and D. Linkin. United States Patent No. 5,458,884
P. Putteman, M. K. J. François and E. C. L. Snoeck. PCT Patent No. WO 95/31178
W. J. Henderson, T. C. Hamilton, M. S. Baylis, C. G. Pierrepoint and K. Griffeths. Environ. Res. 40:247–250 (1986)
A. P. Wehner and R. E. Weller. Food Chem. Toxicol. 24:329–338 (1986)
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Brown, J., Hooper, G., Kenyon, C.J. et al. Spreading and Retention of Vaginal Formulations in Post-Menopausal Women as Assessed by Gamma Scintigraphy. Pharm Res 14, 1073–1078 (1997). https://doi.org/10.1023/A:1012113714552
Issue Date:
DOI: https://doi.org/10.1023/A:1012113714552