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 language | English (US) |
|---|---|
| Pages (from-to) | 839-850 |
| Number of pages | 12 |
| Journal | Journal of Biomedical Materials Research |
| Volume | 16 |
| Issue number | 6 |
| DOIs | |
| State | Published - Nov 1982 |
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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, D. 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 journal › Article
}
TY - JOUR
T1 - In vitro retinoid binding and release from a collagen sponge material in a simulated intravaginal environment
AU - Dorr, Robert T
AU - Surwit, E. A.
AU - Droegemueller, W.
AU - Alberts, D. S.
AU - Meyskens, F. L.
AU - Chvapil, M.
PY - 1982/11
Y1 - 1982/11
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0020213978&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0020213978&partnerID=8YFLogxK
U2 - 10.1002/jbm.820160609
DO - 10.1002/jbm.820160609
M3 - Article
C2 - 6960000
AN - SCOPUS:0020213978
VL - 16
SP - 839
EP - 850
JO - Journal of Biomedical Materials Research - Part A
JF - Journal of Biomedical Materials Research - Part A
SN - 0021-9304
IS - 6
ER -