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 language | English (US) |
|---|---|
| Pages (from-to) | 289-296 |
| Number of pages | 8 |
| Journal | Journal of Controlled Release |
| Volume | 42 |
| Issue number | 3 |
| DOIs | |
| State | Published - Dec 1996 |
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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 journal › Article
}
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 -