New formulation of chemical peeling agent:: 30% salicylic acid in polyethylene glycol -: Absorption and distribution of 14C-salicylic acid in polyethylene glycol applied topically to skin of hairless mice

被引:16
作者
Ueda, S
Mitsugi, K
Ichige, K
Yoshida, K
Sakuma, T
Ninomiya, S
Sudou, T
机构
[1] Ueda Setsuko Clin, Higashi Ku, Fukuoka 8130044, Japan
[2] Daiichi Pure chem Co Ltd, ADME TOX Res Inst, Tokai, Ibaraki, Japan
关键词
dermal absorption; C-14-salicylic acid; polyethylene glycol; hairless mouse; microautoradiography; chemical peeling;
D O I
10.1016/S0923-1811(01)00168-2
中图分类号
R75 [皮肤病学与性病学];
学科分类号
100206 ;
摘要
Salicylic acid is used in chemical peeling procedures. However, they have caused many side effects, even salicylism. To achieve a salicylic acid peeling that would be safer for topical use, we recently developed a new formulation consisting of 30% salicylic acid in polyethylene glycol (PEG) vehicle. In an extension of our previous research, we studied the absorption of 30% salicylic acid labeled with C-14 in PEG vehicle applied topically to the intact and damaged skin of male hairless mice. An ointment containing 3 mg salicylic acid in 10 mg vehicle was applied to both groups. In animals with intact skin, 1 h after application the plasma concentration of radioactivity was 1665.1 ng eq/ml, significantly lower than the 21 437.6 ng eq/ml observed in mice with damaged skin. Microautoradiograms of intact skin showed that the level of radioactivity in the cornified cell layer was similar at 6 h after application. However, in damaged skin, the overall level of radioactivity showed a decrease by 3 h after application. In the carcasses remaining after the treated intact and damaged skin had been removed, 0.09 and 11.38% of the applied radioactivity remained, respectively. These findings confirm that 30% salicylic acid in PEG vehicle is little absorbed through the intact skin of hairless mice, and suggest that salicylism related to absorption through the skin of quantities of topically applied salicylic acid is not likely to occur in humans with intact skin during chemical peeling with this preparation. This new preparation of 30% salicylic acid in PEG vehicle is believed to be safe for application as a chemical peeling agent. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.
引用
收藏
页码:211 / 218
页数:8
相关论文
共 15 条
[1]   Variability in the pharmacokinetics and pharmacodynamics of low dose aspirin in healthy male volunteers [J].
Benedek, IH ;
Joshi, AS ;
Pieniaszek, HJ ;
King, SYP ;
Kornhauser, DM .
JOURNAL OF CLINICAL PHARMACOLOGY, 1995, 35 (12) :1181-1186
[2]  
CHAU K, 2001, ANALGESIC ANTIPYRETI, P696
[3]   The safety and efficacy of salicylic acid chemical peels in darker racial-ethnic groups [J].
Grimes, PE .
DERMATOLOGIC SURGERY, 1999, 25 (01) :18-22
[4]   Histologic changes in the skin of hairless mice following peeling with salicylic acid [J].
Imayama, S ;
Ueda, S ;
Isoda, M .
ARCHIVES OF DERMATOLOGY, 2000, 136 (11) :1390-1395
[5]  
Isoda M, 2001, J DERMATOL SCI, V27, pS60
[6]   Salicylic acid peels for the treatment of photoaging [J].
Kligman, D ;
Kligman, AM .
DERMATOLOGIC SURGERY, 1998, 24 (03) :325-328
[7]  
KLIGMAN D, 1997, COSMETIC DERMATOL, V10, P44
[8]   LIPIDS ARE COVALENTLY ATTACHED TO RIGID CORNEOCYTE PROTEIN ENVELOPES EXISTING PREDOMINANTLY AS BETA-SHEETS - A SOLID-STATE NUCLEAR-MAGNETIC-RESONANCE STUDY [J].
LAZO, ND ;
MEINE, JG ;
DOWNING, DT .
JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1995, 105 (02) :296-300
[9]  
NOGAMI H, 1958, Chem Pharm Bull (Tokyo), V6, P249
[10]   THE EFFECT OF VARIOUS OINTMENT BASES ON THE PERCUTANEOUS ABSORPTION OF SALICYLATES .1. EFFECT OF TYPE OF OINTMENT BASE [J].
STOLAR, ME ;
ROSSI, GV ;
BARR, M .
JOURNAL OF THE AMERICAN PHARMACEUTICAL ASSOCIATION, 1960, 49 (03) :144-147