Studies on the in-vitro percutaneous penetration of indomethacin from gel systems in hairless mice

C. H. Liu, H. O. Ho, M. C. Hsieh, T. D. Sokoloski, M. T. Sheu

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

The influence of co-solvents on the in-vitro percutaneous penetration of indomethacin from gel systems was studied using a simplex lattice experimental design. Gel formulations were prepared by gelling the vehicle mixture of water, either alcohol or isopropanol and either propylene glycol or PEG 400 with 1% w/w Carbomer 940. Hairless mouse skin was employed as the barrier in a Franz-type diffusion cell. The penetration rates at steady state for seven formulations were fitted to a polynomial equation based on this simple lattice method and a three-dimensional plot was constructed. The formulation having the maximal penetration rate was determined to be the vehicle with a solvent ratio of water:alcohol:propylene glycol equal to 15:33:52, and which possessed a solubility parameter of 15 and a drug solubility of around 10 mg mL-1. When the solubility parameter of the vehicle was > 15, the drug solubility increased. However, the penetration rate decreased with an increasing solubility parameter. For those vehicles with a solubility parameter <15, both the drug solubility and the penetration rate decreased with a decrease in the solubility parameter. There was shown to be an approximately 20-fold increase in the relative enhancement factor when using both alcohol and isopropanol, but only a threefold increase for both propylene glycol and PEG 400, when compared with water.

Original languageEnglish
Pages (from-to)365-372
Number of pages8
JournalJournal of Pharmacy and Pharmacology
Volume47
Issue number5
Publication statusPublished - 1995

Fingerprint

Hairless Mouse
Indomethacin
Solubility
Gels
Propylene Glycol
2-Propanol
carbopol 940
Water
Alcohols
Pharmaceutical Preparations
In Vitro Techniques
Research Design
Skin

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

Cite this

Studies on the in-vitro percutaneous penetration of indomethacin from gel systems in hairless mice. / Liu, C. H.; Ho, H. O.; Hsieh, M. C.; Sokoloski, T. D.; Sheu, M. T.

In: Journal of Pharmacy and Pharmacology, Vol. 47, No. 5, 1995, p. 365-372.

Research output: Contribution to journalArticle

@article{e26eecfe60e34cec88ca622e6351b963,
title = "Studies on the in-vitro percutaneous penetration of indomethacin from gel systems in hairless mice",
abstract = "The influence of co-solvents on the in-vitro percutaneous penetration of indomethacin from gel systems was studied using a simplex lattice experimental design. Gel formulations were prepared by gelling the vehicle mixture of water, either alcohol or isopropanol and either propylene glycol or PEG 400 with 1{\%} w/w Carbomer 940. Hairless mouse skin was employed as the barrier in a Franz-type diffusion cell. The penetration rates at steady state for seven formulations were fitted to a polynomial equation based on this simple lattice method and a three-dimensional plot was constructed. The formulation having the maximal penetration rate was determined to be the vehicle with a solvent ratio of water:alcohol:propylene glycol equal to 15:33:52, and which possessed a solubility parameter of 15 and a drug solubility of around 10 mg mL-1. When the solubility parameter of the vehicle was > 15, the drug solubility increased. However, the penetration rate decreased with an increasing solubility parameter. For those vehicles with a solubility parameter <15, both the drug solubility and the penetration rate decreased with a decrease in the solubility parameter. There was shown to be an approximately 20-fold increase in the relative enhancement factor when using both alcohol and isopropanol, but only a threefold increase for both propylene glycol and PEG 400, when compared with water.",
author = "Liu, {C. H.} and Ho, {H. O.} and Hsieh, {M. C.} and Sokoloski, {T. D.} and Sheu, {M. T.}",
year = "1995",
language = "English",
volume = "47",
pages = "365--372",
journal = "Journal of Pharmacy and Pharmacology",
issn = "0022-3573",
publisher = "Pharmaceutical Press",
number = "5",

}

TY - JOUR

T1 - Studies on the in-vitro percutaneous penetration of indomethacin from gel systems in hairless mice

AU - Liu, C. H.

AU - Ho, H. O.

AU - Hsieh, M. C.

AU - Sokoloski, T. D.

AU - Sheu, M. T.

PY - 1995

Y1 - 1995

N2 - The influence of co-solvents on the in-vitro percutaneous penetration of indomethacin from gel systems was studied using a simplex lattice experimental design. Gel formulations were prepared by gelling the vehicle mixture of water, either alcohol or isopropanol and either propylene glycol or PEG 400 with 1% w/w Carbomer 940. Hairless mouse skin was employed as the barrier in a Franz-type diffusion cell. The penetration rates at steady state for seven formulations were fitted to a polynomial equation based on this simple lattice method and a three-dimensional plot was constructed. The formulation having the maximal penetration rate was determined to be the vehicle with a solvent ratio of water:alcohol:propylene glycol equal to 15:33:52, and which possessed a solubility parameter of 15 and a drug solubility of around 10 mg mL-1. When the solubility parameter of the vehicle was > 15, the drug solubility increased. However, the penetration rate decreased with an increasing solubility parameter. For those vehicles with a solubility parameter <15, both the drug solubility and the penetration rate decreased with a decrease in the solubility parameter. There was shown to be an approximately 20-fold increase in the relative enhancement factor when using both alcohol and isopropanol, but only a threefold increase for both propylene glycol and PEG 400, when compared with water.

AB - The influence of co-solvents on the in-vitro percutaneous penetration of indomethacin from gel systems was studied using a simplex lattice experimental design. Gel formulations were prepared by gelling the vehicle mixture of water, either alcohol or isopropanol and either propylene glycol or PEG 400 with 1% w/w Carbomer 940. Hairless mouse skin was employed as the barrier in a Franz-type diffusion cell. The penetration rates at steady state for seven formulations were fitted to a polynomial equation based on this simple lattice method and a three-dimensional plot was constructed. The formulation having the maximal penetration rate was determined to be the vehicle with a solvent ratio of water:alcohol:propylene glycol equal to 15:33:52, and which possessed a solubility parameter of 15 and a drug solubility of around 10 mg mL-1. When the solubility parameter of the vehicle was > 15, the drug solubility increased. However, the penetration rate decreased with an increasing solubility parameter. For those vehicles with a solubility parameter <15, both the drug solubility and the penetration rate decreased with a decrease in the solubility parameter. There was shown to be an approximately 20-fold increase in the relative enhancement factor when using both alcohol and isopropanol, but only a threefold increase for both propylene glycol and PEG 400, when compared with water.

UR - http://www.scopus.com/inward/record.url?scp=0029069992&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029069992&partnerID=8YFLogxK

M3 - Article

C2 - 7494184

AN - SCOPUS:0029069992

VL - 47

SP - 365

EP - 372

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

IS - 5

ER -