Distribution of salicylic acid in human stratum corneum following topical application in vivo: a comparison of six different formulations.
Distribution of salicylic acid in human stratum corneum from treatment of six different formulations was assessed by quantitation of drug content in sequentially tape-stripped stratum corneum after a single 2-h dose was applied unoccluded to skin on the ventral forearm of four female subjects. The profile and total amounts of stratum corneum removed in 20 tape-strips varied among different types of formulations. With or without normalization by the total stratum corneum weights removed, the extent of drug delivery to the stratum corneum decreased in the following order: SA (5%) > > SAC (10%), Duofilm (16.7%) > TSSS (2%) > SAO (10%), Salic (2.5%), the percentage in parentheses indicating the salicylic acid concentration in each formulation. The greatest topical bioavailability was observed for the alcoholic solution containing glycerol (SA). The 10% collodion formulation (SAC) was found to deliver an amount of salicylic acid into the stratum corneum 2-fold greater than 10% ointment formulation (SAO). Use of absorption ointment (TSSS) also increased the uptake of salicylic acid into the stratum corneum in comparison with formulations based on simple ointment (SAO) and oil in water (o/w) cream (Salic). The partitioning of salicylic acid from collodion formulations (SAC and Duofilm) appeared to be concentration-independent. The results of this study indicate that topical bioavailability of salicylic acid in the stratum corneum varies substantially among different formulations.
Tsai
J
J
Institute of Clinical Pharmacy, National Cheng Kung University, 1 University Road, Tainan, Taiwan, ROC. jctsai@mail.ncku.edu.tw
Chuang
S
S
Hsu
M
M
Sheu
H
H
D000269:Adhesives; D000279:Administration, Cutaneous; D000328:Adult; D004305:Dose-Response Relationship, Drug; D004817:Epidermis / Q000737:chemistry / Q000378:metabolism*; D005260:Female; D006801:Humans; D007641:Keratolytic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010592:Pharmaceutic Aids / Q000008:administration & dosage; D020156:Salicylic Acid / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics*
D000269:Adhesives; D007641:Keratolytic Agents; D010592:Pharmaceutic Aids; D020156:Salicylic Acid