Abstract
The characteristics of in vitro permeation of flufenamic acid (FA) from lipid disperse systems composed of phosphatidylcholine (PC) and glycosylceramide (GC) were compared among rat abdominal skin, a silicon rubber membrane (Silastic®) and a stratum corneum (SC) sheet isolated from hamster cheek pouch. When a PC dispersion (PCD) containing 20 μmol PC/ml was applied, the permeation of FA through rat skin was enhanced approx. 2.2-fold compared with that from the lipid-free suspension (LFS). Further, a nearly 2-fold enhancement was observed when a GC-containing PCD (10% GC-PCD) was examined. A similar pattern of enhancement could be reproduced when cheek pouch SC was used instead of, rat skin, whereas it was not observed in Silastic®. The enhanced permeation in the skin could not be explained on the basis of the incremental increase in the apparent solubilities. A significant correlation was observed between skin permeation and epidermal tissue uptake of FA from LFS and PCDs, although the nearly 2-fold increase found in 10% GC-PCD might be due to mechanisms other than the increase in epidermal tissue uptake. The usefulness of an SC sheet isolated from hamster cheek pouch, a new model membrane without appendages, in studying the direct action of either permeation enhancers or dosage forms designed to enhance the percutaneous permeation of drugs on the SC is discussed.
| Original language | English |
|---|---|
| Pages (from-to) | 1-9 |
| Number of pages | 9 |
| Journal | International Journal of Pharmaceutics |
| Volume | 67 |
| Issue number | 1 |
| DOIs | |
| Publication status | Published - Jan 1 1991 |
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Keywords
- Flufenamic acid
- Hamster cheek pouch
- Isolated stratum corneum
- Lipid disperse system
- Percutaneous permeation
- Rat abdominal skin
- Silastic
ASJC Scopus subject areas
- Pharmaceutical Science
Cite this
Use of lipid disperse systems in transdermal drug delivery : Comparative study of flufenamic acid permeation among rat abdominal skin, silicon rubber membrane and stratum corneum sheet isolated from hamster cheek pouch. / Kurosaki, Yuji; Nagahara, Naoki; Tanizawa, Toshihiro; Nishimura, Hidekatsu; Nakayama, Taiji; Kimura, Toshikiro.
In: International Journal of Pharmaceutics, Vol. 67, No. 1, 01.01.1991, p. 1-9.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Use of lipid disperse systems in transdermal drug delivery
T2 - Comparative study of flufenamic acid permeation among rat abdominal skin, silicon rubber membrane and stratum corneum sheet isolated from hamster cheek pouch
AU - Kurosaki, Yuji
AU - Nagahara, Naoki
AU - Tanizawa, Toshihiro
AU - Nishimura, Hidekatsu
AU - Nakayama, Taiji
AU - Kimura, Toshikiro
PY - 1991/1/1
Y1 - 1991/1/1
N2 - The characteristics of in vitro permeation of flufenamic acid (FA) from lipid disperse systems composed of phosphatidylcholine (PC) and glycosylceramide (GC) were compared among rat abdominal skin, a silicon rubber membrane (Silastic®) and a stratum corneum (SC) sheet isolated from hamster cheek pouch. When a PC dispersion (PCD) containing 20 μmol PC/ml was applied, the permeation of FA through rat skin was enhanced approx. 2.2-fold compared with that from the lipid-free suspension (LFS). Further, a nearly 2-fold enhancement was observed when a GC-containing PCD (10% GC-PCD) was examined. A similar pattern of enhancement could be reproduced when cheek pouch SC was used instead of, rat skin, whereas it was not observed in Silastic®. The enhanced permeation in the skin could not be explained on the basis of the incremental increase in the apparent solubilities. A significant correlation was observed between skin permeation and epidermal tissue uptake of FA from LFS and PCDs, although the nearly 2-fold increase found in 10% GC-PCD might be due to mechanisms other than the increase in epidermal tissue uptake. The usefulness of an SC sheet isolated from hamster cheek pouch, a new model membrane without appendages, in studying the direct action of either permeation enhancers or dosage forms designed to enhance the percutaneous permeation of drugs on the SC is discussed.
AB - The characteristics of in vitro permeation of flufenamic acid (FA) from lipid disperse systems composed of phosphatidylcholine (PC) and glycosylceramide (GC) were compared among rat abdominal skin, a silicon rubber membrane (Silastic®) and a stratum corneum (SC) sheet isolated from hamster cheek pouch. When a PC dispersion (PCD) containing 20 μmol PC/ml was applied, the permeation of FA through rat skin was enhanced approx. 2.2-fold compared with that from the lipid-free suspension (LFS). Further, a nearly 2-fold enhancement was observed when a GC-containing PCD (10% GC-PCD) was examined. A similar pattern of enhancement could be reproduced when cheek pouch SC was used instead of, rat skin, whereas it was not observed in Silastic®. The enhanced permeation in the skin could not be explained on the basis of the incremental increase in the apparent solubilities. A significant correlation was observed between skin permeation and epidermal tissue uptake of FA from LFS and PCDs, although the nearly 2-fold increase found in 10% GC-PCD might be due to mechanisms other than the increase in epidermal tissue uptake. The usefulness of an SC sheet isolated from hamster cheek pouch, a new model membrane without appendages, in studying the direct action of either permeation enhancers or dosage forms designed to enhance the percutaneous permeation of drugs on the SC is discussed.
KW - Flufenamic acid
KW - Hamster cheek pouch
KW - Isolated stratum corneum
KW - Lipid disperse system
KW - Percutaneous permeation
KW - Rat abdominal skin
KW - Silastic
UR - http://www.scopus.com/inward/record.url?scp=0026068604&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0026068604&partnerID=8YFLogxK
U2 - 10.1016/0378-5173(91)90259-Q
DO - 10.1016/0378-5173(91)90259-Q
M3 - Article
VL - 67
SP - 1
EP - 9
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
SN - 0378-5173
IS - 1
ER -