Penetration of Topical Corticosteroids Through Human Epidermis

Abstract

The penetration of hydrocortisone, hydrocortisone 17‐butyrate 21‐propionate, betamethasone, betamethasone 17‐valerate, and clobetasol 17‐propionate through separated human epidermis was compared. The amount of each topical corticosteroid which was released on the skin and penetrated to saline was greater in ethanol solution than propylene glycol solution. The addition of water to the ethanol increased the release of some corticosteroids. The lipid solubility of each corticosteroid correlated well with skin penetration; however, the polarity of each corticosteroid was inversely proportional to skin penetration. The results of the blanching phenomenon caused by the application of these corticosteroids and of their skin penetration suggested to us that the local pharmacological activity of each topical corticosteroid, rather than their skin penetration, related well to their clinical effectiveness.

Microdermabrasion as a Novel Tool to Enhance Drug Delivery via the Skin: An Animal Study

“…Because the SC is a lipophilic barrier in the skin, the lipophilic clobetasol easily partitions into the SC, after which it passes across the skin. Previous studies also indicated that the SC/vehicle partition coefficient plays an important role in the amount of corticosteroids such as clobetasol and betamethasone released from the vehicle to the skin 17,18 . The ablation and homogenization of the SC layers may reduce the inherent barrier properties of the SC and thus increase the skin delivery of drugs; however, the partitioning of lipophilic permeants into the SC may be reduced because of the limited area of the SC after microdermabrasion exposure 3 .…”

“…In vitro skin delivery using porcine skin and in vivo topical application employing nude mouse as the animal model were both used to examine the effect of microdermabrasion. The vacuum pressures used in this study (15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25) were much lower than those used for therapeutic purposes.…”

Drug Delivery to Local Subcutaneous Structures Following Topical Administration

“…The time course of disposition to the back muscle in the two species is shown in Fig. It is also true that radial movement within the skin as assessed by visual detection of a pharmacological response is not limited to vasodilation, but has also been witnessed with the opposite effect produced by corticosteroids (6). It is apparent that significant levels of escin are present in the deeper local tissue over prolonged periods of time.…”

16β-methyl-17α,21-diesterified glucocorticoids as partial agonists of glucocorticoid in rat endotoxin-induced inflammation

“…There are several possible explanations for these contrasting results. There may be differences in the inflammatory site, as in the rat ear edema model, glucocorticoids were applied to the ear and they may not easily enter into the systemic circulation through the skin [15]. After application of 16b-methyl17a,21-diesterified glucocorticoids, they and their metabolites may stay in the skin at higher concentrations and for longer periods than those of non-esterified glucocorticoids, and thus may show potent topical anti-inflammatory activity even though 16b-methyl-17a,21-diesterified glucocorticoids have only weak activity.…”