Percutaneous Absorption of Hydrocortisone-4-C* in Two Human Subjects*

Malkinson, Frederick D.; Ferguson, Edward H.

doi:10.1038/jid.1955.131

Cited by 106 publications

(16 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The poor efficiency of topical formulations due to the unwanted drug crystallisation may be related to the drug reservoir formation in the skin [37]. The potential to create a drug reservoir in the skin was previously observed by other researchers but the mechanism of drug reservoir formation remains unknown [14,38,39]. The present study indicates that drug crystallisation in the skin may contribute to the formation of drug reservoir in the skin.…”

Section: Discussionmentioning

confidence: 57%

The application of ATR-FTIR spectroscopy and multivariate data analysis to study drug crystallisation in the stratum corneum

Goh

Craig

Hadgraft

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

View full text Add to dashboard Cite

Drug permeation through the intercellular lipids, which pack around and between corneocytes, may be enhanced by increasing the thermodynamic activity of the active in a formulation. However, this may also result in unwanted drug crystallisation on and in the skin. In this work, we explore the combination of ATR-FTIR spectroscopy and multivariate data analysis to study drug crystallisation in the skin.Ex vivo permeation studies of saturated solutions of diclofenac sodium (DF Na) in two vehicles, propylene glycol (PG) and dimethyl sulphoxide (DMSO), were carried out in porcine ear skin. Tape stripping and ATR-FTIR spectroscopy were conducted simultaneously to collect spectral data as a function of skin depth. Multivariate data analysis was applied to visualise and categorise the spectral data in the region of interest (1700 -1500 cm -1 ) containing the carboxylate (COO -) asymmetric stretching vibrations of DF Na. 3Spectral data showed the redshifts of the COO -asymmetric stretching vibrations for DF Na in the solution compared with solid drug. Similar shifts were evident following application of saturated solutions of DF Na to porcine skin samples. Multivariate data analysis categorised the spectral data based on the spectral differences and drug crystallisation was found to be confined to the upper layers of the skin.This proof-of-concept study highlights the utility of ATR-FTIR spectroscopy in combination with multivariate data analysis as a simple and rapid approach in the investigation of drug deposition in the skin. The approach described here will be extended to the study of other actives for topical application to the skin. GRAPHICAL ABSTRACT KEY WORDSStratum corneum; Crystallisation; ATR-FTIR; Multivariate data analysis, Porcine skin 4

show abstract

Section: Discussionmentioning

confidence: 57%

The application of ATR-FTIR spectroscopy and multivariate data analysis to study drug crystallisation in the stratum corneum

Goh

Craig

Hadgraft

et al. 2017

European Journal of Pharmaceutics and Biopharmaceutics

View full text Add to dashboard Cite

show abstract

“…Malkinson and Ferguson [4] first suggested this concept but as Vickers [1] points out their data could be explained by a slow diffusion process through the stratum corneum. Potential sites for this depot were suggested to be keratin spaces, follicular openings and surface folds [5].…”

Section: Historical Perspective On the Stratum Corneum Reservoir For mentioning

confidence: 99%

Factors Affecting the Formation of a Skin Reservoir for Topically Applied Solutes

Roberts

Cross

Anissimov³

2003

Skin Pharmacol Physiol

View full text Add to dashboard Cite

The reservoir function of the skin is an important determinant of the duration of action of a topical solute. The reservoir can exist in the stratum corneum, in the viable avascular tissue (viable epidermis and supracapillary dermis) and in the dermis. A steroid reservoir in the stratum corneum has been demonstrated by the reactivation of a vasoconstrictor effect by occlusion or application of a placebo cream to the skin some time after the original topical application of steroid. Other solutes have also been reported to show a reservoir effect in the skin after topical application. A simple compartmental model is used to understand why reactivation of vasoconstriction some time after a topical steroid application shows dependency on time, topical solute concentration and the product used to cause reactivation. The model is also used to show which solutes are likely to show a reservoir effect and could be potentially affected by desquamation, especially when the turnover of the skin is abnormally rapid. A similar form of the model can be used to understand the promotion of reservoir function in the viable tissue and in the dermis in terms of effective removal by blood perfusing the tissues.

show abstract

“…The presence of endogenous estrogens in the skin and differences in estrogen binding affinities in different regions of the integument were first demonstrated in murine skin by titrated estradiol in autoradiographic studies (with estrogenrelated radioactivity found to be localized in the epidermis, dermal fibroblasts, and the hair follicle) (13,14). In 1978, an "ER protein" was detected in murine skin, and titrated estradiol was found to bind specifically to the cytosol of cells from mouse back skin (15).…”

Section: Introductionmentioning

confidence: 99%

The Hair Follicle as an Estrogen Target and Source

et al. 2006

View full text Add to dashboard Cite

For many decades, androgens have dominated endocrine research in hair growth control. Androgen metabolism and the androgen receptor currently are the key targets for systemic, pharmacological hair growth control in clinical medicine. However, it has long been known that estrogens also profoundly alter hair follicle growth and cycling by binding to locally expressed high-affinity estrogen receptors (ERs). Besides altering the transcription of genes with estrogen-responsive elements, 17␤-estradiol (E2) also modifies androgen metabolism within distinct subunits of the pilosebaceous unit (i.e., hair follicle and sebaceous gland). The latter displays prominent aromatase activity, the key enzyme for androgen conversion to E2, and is both an estrogen source and target.Here, we chart the recent renaissance of estrogen research in hair research; explain why the hair follicle offers an ideal, clinically relevant test system for studying the role of sex steroids, their receptors, and interactions in neuroectodermal-mesodermal interaction systems in general; and illustrate how it can be exploited to identify novel functions and signaling cross talks of ER-mediated signaling. Emphasizing the long-underestimated complexity and species-, gender-, and site-dependence of E2-induced biological effects on the hair follicle, we explore targets for pharmacological intervention in clinically relevant hair cycle manipulation, ranging from androgenetic alopecia and hirsutism via telogen effluvium to chemotherapy-induced alopecia. While defining major open questions, unsolved clinical challenges, and particularly promising research avenues in this area, we argue that the time has come to pay estrogen-mediated signaling the full attention it deserves in future endocrinological therapy of common hair growth disorders. (Endocrine Reviews 27: 677-706, 2006)

show abstract

Percutaneous Absorption of Hydrocortisone-4-C* in Two Human Subjects*

Cited by 106 publications

References 7 publications

The application of ATR-FTIR spectroscopy and multivariate data analysis to study drug crystallisation in the stratum corneum

The application of ATR-FTIR spectroscopy and multivariate data analysis to study drug crystallisation in the stratum corneum

Factors Affecting the Formation of a Skin Reservoir for Topically Applied Solutes

The Hair Follicle as an Estrogen Target and Source

Contact Info

Product

Resources

About