Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin

Glen Xiong, Danyi Quan, Howard I. Maibach

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

The influence of the penetration enhancers, laurocapram (Azone®), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: laurocapram > nerolidol, 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2% laurocapram and a 2-fold enhancement resulted with 2% nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10% 1,8-cineole. The highest enhancement factor was 5.6 with 5% laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.

Original languageEnglish (US)
Pages (from-to)289-296
Number of pages8
JournalJournal of Controlled Release
Volume42
Issue number3
DOIs
StatePublished - Dec 1996

Fingerprint

Skin Absorption
Low Molecular Weight Heparin
Skin
Cornea
Cellophane
Dermis
Epidermis
laurocapram
In Vitro Techniques
eucalyptol
Pharmaceutical Preparations
nerolidol

Keywords

  • 1,8-Cineole
  • Laurocapram
  • Low molecular weight heparin
  • Nerolidol
  • Penetration enhancer
  • Percutaneous absorption

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin. / Xiong, Glen; Quan, Danyi; Maibach, Howard I.

In: Journal of Controlled Release, Vol. 42, No. 3, 12.1996, p. 289-296.

Research output: Contribution to journalArticle

@article{a0c59c393ab14498928372e60d3fc701,
title = "Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin",
abstract = "The influence of the penetration enhancers, laurocapram (Azone{\circledR}), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: laurocapram > nerolidol, 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2{\%} laurocapram and a 2-fold enhancement resulted with 2{\%} nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10{\%} 1,8-cineole. The highest enhancement factor was 5.6 with 5{\%} laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.",
keywords = "1,8-Cineole, Laurocapram, Low molecular weight heparin, Nerolidol, Penetration enhancer, Percutaneous absorption",
author = "Glen Xiong and Danyi Quan and Maibach, {Howard I.}",
year = "1996",
month = "12",
doi = "10.1016/0168-3659(96)01465-4",
language = "English (US)",
volume = "42",
pages = "289--296",
journal = "Journal of Controlled Release",
issn = "0168-3659",
publisher = "Elsevier",
number = "3",

}

TY - JOUR

T1 - Effects of penetration enhancers on in vitro percutaneous absorption of low molecular weight heparin through human skin

AU - Xiong, Glen

AU - Quan, Danyi

AU - Maibach, Howard I.

PY - 1996/12

Y1 - 1996/12

N2 - The influence of the penetration enhancers, laurocapram (Azone®), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: laurocapram > nerolidol, 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2% laurocapram and a 2-fold enhancement resulted with 2% nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10% 1,8-cineole. The highest enhancement factor was 5.6 with 5% laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.

AB - The influence of the penetration enhancers, laurocapram (Azone®), 1,8-cineole, and nerolidol on the in vitro percutaneous absorption of low molecular weight heparin (LMWH) through human skin was investigated. The enhancing effectiveness of the enhancers decreased in the order: laurocapram > nerolidol, 1,8-cineole. Compared to the control formulation (without enhancers), a 4.4-fold enhancement was observed with 2% laurocapram and a 2-fold enhancement resulted with 2% nerolidol. There were no significant promoting effects at low concentrations of 1,8-cineole; however, a 3.5-fold increase in LMWH flux resulted with 10% 1,8-cineole. The highest enhancement factor was 5.6 with 5% laurocapram. Cellophane tape-stripping of the stratum corneum did not affect drug flux compared to the control (full-thickness skin). Thus the epidermis and dermis, as well as the stratum corneum, may constitute major rate determining barriers for LMWH permeation across human skin.

KW - 1,8-Cineole

KW - Laurocapram

KW - Low molecular weight heparin

KW - Nerolidol

KW - Penetration enhancer

KW - Percutaneous absorption

UR - http://www.scopus.com/inward/record.url?scp=0030560813&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0030560813&partnerID=8YFLogxK

U2 - 10.1016/0168-3659(96)01465-4

DO - 10.1016/0168-3659(96)01465-4

M3 - Article

AN - SCOPUS:0030560813

VL - 42

SP - 289

EP - 296

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

IS - 3

ER -