In vitro retinoid binding and release from a collagen sponge material in a simulated intravaginal environment

Robert T Dorr, E. A. Surwit, W. Droegemueller, David S Alberts, F. L. Meyskens, M. Chvapil

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Abstract

Four in vitro preparations were constructed to simulate the intravaginal release of two retinoids, all-trans-retinoic acid (t-RA) and 13-cis-retinoic acid (c-RA), from a 0.7% collagen sponge diaphragm insert. Four t-RA concentrations, 0.019, 0.05, 0.1, and 0.15% in methanol were added to the sponge. The release into an artificial vaginal fluid was monitored serially over 72 h by serial analysis for t-RA and c-RA using high-pressure liquid chromatography. In each preparation, retinoid release was immediate and noncontinuous. At 37°C, the retinoids were stable for at least 48 h. Trans-retinoic acid was the predominant retinoid recovered. Only trace amounts of the cis-isomer were released. Peak t-RA levels were 20 μM after 0.01%, 60-80 μM after 0.05%, 100-200 μM after 0.1%, and 320 μM after 0.15%. When the vaginal fluid bath was changed after 5 h, no further significant retinoid release occurred. There was significant loss of up to 70% of the applied t-RA into the collagen sponge. The retinoid binding was concentration dependent (higher binding with higher concentrations) and was maximal only after 24 h of co-incubation. The discontinuous release of t-RA and the high degree of binding to collagen would seem to preclude use of the diaphragm insert as a vaginal drug delivery system, at least for retinoids.

Original languageEnglish (US)
Pages (from-to)839-850
Number of pages12
JournalJournal of Biomedical Materials Research
Volume16
Issue number6
DOIs
StatePublished - Nov 1982

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Retinoids
Tretinoin
Collagen
Acids
Isotretinoin
Diaphragms
High pressure liquid chromatography
Fluids
Isomers
Methanol

ASJC Scopus subject areas

  • Biomedical Engineering
  • Biomaterials

Cite this

In vitro retinoid binding and release from a collagen sponge material in a simulated intravaginal environment. / Dorr, Robert T; Surwit, E. A.; Droegemueller, W.; Alberts, David S; Meyskens, F. L.; Chvapil, M.

In: Journal of Biomedical Materials Research, Vol. 16, No. 6, 11.1982, p. 839-850.

Research output: Contribution to journalArticle

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abstract = "Four in vitro preparations were constructed to simulate the intravaginal release of two retinoids, all-trans-retinoic acid (t-RA) and 13-cis-retinoic acid (c-RA), from a 0.7{\%} collagen sponge diaphragm insert. Four t-RA concentrations, 0.019, 0.05, 0.1, and 0.15{\%} in methanol were added to the sponge. The release into an artificial vaginal fluid was monitored serially over 72 h by serial analysis for t-RA and c-RA using high-pressure liquid chromatography. In each preparation, retinoid release was immediate and noncontinuous. At 37°C, the retinoids were stable for at least 48 h. Trans-retinoic acid was the predominant retinoid recovered. Only trace amounts of the cis-isomer were released. Peak t-RA levels were 20 μM after 0.01{\%}, 60-80 μM after 0.05{\%}, 100-200 μM after 0.1{\%}, and 320 μM after 0.15{\%}. When the vaginal fluid bath was changed after 5 h, no further significant retinoid release occurred. There was significant loss of up to 70{\%} of the applied t-RA into the collagen sponge. The retinoid binding was concentration dependent (higher binding with higher concentrations) and was maximal only after 24 h of co-incubation. The discontinuous release of t-RA and the high degree of binding to collagen would seem to preclude use of the diaphragm insert as a vaginal drug delivery system, at least for retinoids.",
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