[Influence of the stratum corneum and dermis of the skin on the percutaneous absorption of fluorouracil delivered through skin patch].
OBJECTIVE
To investigate the respective influence of skin layers, specifically the stratum corneum (SC) and the viable layer, and isopropyl myristate (IPM), an absorption enhancer, on the permeability (K(p)) of drug.


METHODS
Patches saturated with fluorouracil (5-FU), which was used as a test drug, were prepared. The Franz diffusion experiment via different rat skin layers was carried out, and high-performance liquid chromatography (HPLC) or gas chromatography (GC) was employed to determine the contents of 5-FU and IPM. K(p) of 5-FU in various conditions was calculated.


RESULTS
The K(p) of 5-FU via SC -stripped skin was 2.3 times that via intact skin, and in the presence of IPM, K(p) was 1.8 times that via intact skin and 2.4 times that via SC-stripped skin.


CONCLUSIONS
The permeability of 5-FU is enhanced after the SC is stripped, and IPM can overcome the barrier of SC in intact skin to facilitate 5-FU absorption, but can not enhance the K(p) of 5-FU via SC-stripped skin.
Li
Guo-feng
GF
Department of Pharmacy, Nanfang Hospital, First Military Medical University, Guangzhou 510515, China. lgfnf@fimmu.com
Chen
Jian-hai
JH
Kamiyama
Fumio
F
Yamamoto
Akira
A
Chen
Zhi-liang
ZL
D000279:Administration, Cutaneous; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002849:Chromatography, Gas; D002851:Chromatography, High Pressure Liquid; D020405:Dermis / Q000378:metabolism*; D005472:Fluorouracil / Q000008:administration & dosage / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D051381:Rats; D017208:Rats, Wistar; D012869:Skin Absorption
D000964:Antimetabolites, Antineoplastic; D005472:Fluorouracil