Publication

In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats

VOLLMER, U., MULLER, BW., MESENS, J., WILFFERT, B. & Peters, T., 1-Sep-1993, In : International Journal of Pharmaceutics. 99, 1, p. 51-58 8 p.

Research output: Contribution to journalArticleAcademicpeer-review

APA

VOLLMER, U., MULLER, BW., MESENS, J., WILFFERT, B., & Peters, T. (1993). In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats. International Journal of Pharmaceutics, 99(1), 51-58.

Author

VOLLMER, U ; MULLER, BW ; MESENS, J ; WILFFERT, B ; Peters, Thies. / In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats. In: International Journal of Pharmaceutics. 1993 ; Vol. 99, No. 1. pp. 51-58.

Harvard

VOLLMER, U, MULLER, BW, MESENS, J, WILFFERT, B & Peters, T 1993, 'In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats', International Journal of Pharmaceutics, vol. 99, no. 1, pp. 51-58.

Standard

In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats. / VOLLMER, U; MULLER, BW; MESENS, J; WILFFERT, B; Peters, Thies.

In: International Journal of Pharmaceutics, Vol. 99, No. 1, 01.09.1993, p. 51-58.

Research output: Contribution to journalArticleAcademicpeer-review

Vancouver

VOLLMER U, MULLER BW, MESENS J, WILFFERT B, Peters T. In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats. International Journal of Pharmaceutics. 1993 Sep 1;99(1):51-58.


BibTeX

@article{8c3feee7d7d4414baee317ba24b1bf43,
title = "In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats",
abstract = "The aim of the study was to evaluate whether 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) can be used as transdermal absorption enhancer for liarozole. Therefore, we used an in vivo model where transdermal drug absorption in rats can be studied under physiological conditions by cannulating the peripheral skin vein draining the area of the skin which is used for drug application, and collecting the blood (Vollmer et al., 1992a). We compared liarozole, applied as a 1{\%} aqueous solution, in different formulations. We varied the pH, the concentration of HPbetaCD and tested another cyclodextrin derivative (2,6-dimethyl-beta-cyclodextrin, DIMEB). In addition, we compared the absorption with a formulation of 40{\%} propylene glycol/10{\%} oleic acid (PG/OA) and after stripping the stratum corneum. HPbetaCD was a moderate enhancer at a concentration of 20{\%} (4.9{\%} HPbetaCD was ineffective) and increased the flux of liarozole at pH 4 from 0.138-0.151 (control) to 0.421-0.487 nmol per h (i.e., 3-fold) after a lag time of 84-104 min (95{\%} limits of confidence), whereas the same formulation at pH 7 did not reach steady state during 4.5 h. The absorption of liarozole in 20{\%} aqueous solution of DIMEB was slightly decreased (by a factor of 0.6), in PG/OA it increased by a factor 1.7 and the flux after stripping the stratum corneum reached 91.4-101.4 nmol/h with a lag time of 10-16 min. Therefore, a 20{\%} aqueous solution of HPbetaCD appears to be a suitable transdermal absorption enhancer for liarozole.",
keywords = "CYCLODEXTRIN, LIAROZOLE, PENETRATION ENHANCEMENT, PERCUTANEOUS ABSORPTION, IN-VIVO ABSORPTION, RAT SKIN, BARRIER",
author = "U VOLLMER and BW MULLER and J MESENS and B WILFFERT and Thies Peters",
year = "1993",
month = "9",
day = "1",
language = "English",
volume = "99",
pages = "51--58",
journal = "International Journal of Pharmaceutics",
issn = "0378-5173",
publisher = "Elsevier Bedrijfsinformatie b.v.",
number = "1",

}

RIS

TY - JOUR

T1 - In-vivo skin pharmacokinetics of liarozole - percutaneous-absorption studies with different formulations of cyclodextrin derivatives in rats

AU - VOLLMER, U

AU - MULLER, BW

AU - MESENS, J

AU - WILFFERT, B

AU - Peters, Thies

PY - 1993/9/1

Y1 - 1993/9/1

N2 - The aim of the study was to evaluate whether 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) can be used as transdermal absorption enhancer for liarozole. Therefore, we used an in vivo model where transdermal drug absorption in rats can be studied under physiological conditions by cannulating the peripheral skin vein draining the area of the skin which is used for drug application, and collecting the blood (Vollmer et al., 1992a). We compared liarozole, applied as a 1% aqueous solution, in different formulations. We varied the pH, the concentration of HPbetaCD and tested another cyclodextrin derivative (2,6-dimethyl-beta-cyclodextrin, DIMEB). In addition, we compared the absorption with a formulation of 40% propylene glycol/10% oleic acid (PG/OA) and after stripping the stratum corneum. HPbetaCD was a moderate enhancer at a concentration of 20% (4.9% HPbetaCD was ineffective) and increased the flux of liarozole at pH 4 from 0.138-0.151 (control) to 0.421-0.487 nmol per h (i.e., 3-fold) after a lag time of 84-104 min (95% limits of confidence), whereas the same formulation at pH 7 did not reach steady state during 4.5 h. The absorption of liarozole in 20% aqueous solution of DIMEB was slightly decreased (by a factor of 0.6), in PG/OA it increased by a factor 1.7 and the flux after stripping the stratum corneum reached 91.4-101.4 nmol/h with a lag time of 10-16 min. Therefore, a 20% aqueous solution of HPbetaCD appears to be a suitable transdermal absorption enhancer for liarozole.

AB - The aim of the study was to evaluate whether 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) can be used as transdermal absorption enhancer for liarozole. Therefore, we used an in vivo model where transdermal drug absorption in rats can be studied under physiological conditions by cannulating the peripheral skin vein draining the area of the skin which is used for drug application, and collecting the blood (Vollmer et al., 1992a). We compared liarozole, applied as a 1% aqueous solution, in different formulations. We varied the pH, the concentration of HPbetaCD and tested another cyclodextrin derivative (2,6-dimethyl-beta-cyclodextrin, DIMEB). In addition, we compared the absorption with a formulation of 40% propylene glycol/10% oleic acid (PG/OA) and after stripping the stratum corneum. HPbetaCD was a moderate enhancer at a concentration of 20% (4.9% HPbetaCD was ineffective) and increased the flux of liarozole at pH 4 from 0.138-0.151 (control) to 0.421-0.487 nmol per h (i.e., 3-fold) after a lag time of 84-104 min (95% limits of confidence), whereas the same formulation at pH 7 did not reach steady state during 4.5 h. The absorption of liarozole in 20% aqueous solution of DIMEB was slightly decreased (by a factor of 0.6), in PG/OA it increased by a factor 1.7 and the flux after stripping the stratum corneum reached 91.4-101.4 nmol/h with a lag time of 10-16 min. Therefore, a 20% aqueous solution of HPbetaCD appears to be a suitable transdermal absorption enhancer for liarozole.

KW - CYCLODEXTRIN

KW - LIAROZOLE

KW - PENETRATION ENHANCEMENT

KW - PERCUTANEOUS ABSORPTION

KW - IN-VIVO ABSORPTION

KW - RAT SKIN

KW - BARRIER

M3 - Article

VL - 99

SP - 51

EP - 58

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1

ER -

ID: 13858550