Abstract:
:Talarozole is a new highly potent and selective azole derivative which inhibits cytochrome-P450-dependent all-trans-retinoic acid catabolism. It is in clinical development for the treatment of psoriasis and acne. However, no local pharmacokinetic data on the diffusion behaviour of talarozole in the skin itself are available. As topical application might be an interesting alternative to oral therapy because of the reduced systemic side effects, the aim of this study was to assess the transdermal behaviour of topically applied talarozole, including its within-skin distribution. Franz diffusion cell experiments with talarozole dissolved in different pharmaceutically relevant solvents (i.e. propylene glycol, oleolyl macrogol glyceride, isopropyl myristate, diethylene glycol monoethylether, ethanol, caprylic/capric triglyceride and caprylocaproyl macrogol glyceride) were performed to assess the transdermal behaviour of talarozole. Talarozole slightly diffused into the skin only when dissolved in propylene glycol, isopropyl myristate or ethanol. Although only 0.1% of the dose applied was found in the skin itself after 12-24 h, this was sufficient to achieve local concentrations well above the half-maximal inhibitory concentration value for talarozole. The distribution of talarozole within the skin was investigated: 80% was located in the epidermis, while the remaining 20% was found in the dermis. The epidermal concentration of talarozole achieved after a single topical application was sufficiently high to enable the potential induction of local retinoid-like effects.
journal_name
Skin Pharmacol Physioljournal_title
Skin pharmacology and physiologyauthors
Baert B,De Spiegeleer Bdoi
10.1159/000323012subject
Has Abstractpub_date
2011-01-01 00:00:00pages
151-9issue
3eissn
1660-5527issn
1660-5535pii
000323012journal_volume
24pub_type
杂志文章abstract:BACKGROUND/AIMS:Wound healing is a complex regeneration process involving the degradation and reassembly of connective tissues and skin layers. Previous studies have shown that pH plays a significant role in both the direct and indirect regulation of cellular processes in the wound, which, in turn, affect the wound heal...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000447016
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND AND AIM:Since the pharmacological effects of diclofenac (DF) are short-lived because of its short half-life, prolongation of the pharmacological effect in a topical formulation is needed for more appropriate clinical use. For the enhancement of dermal accumulation and prolongation of the pharmacological effe...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000501734
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND/AIMS:Advanced glycation end products, which are linked to both aging and hyperglycemia, cause marked functional and structural alterations in human skin. Though it is well known that the metabolism of glucose is closely associated with that of fatty acid (FA), sharing the same energy-yielding reaction pathwa...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000448121
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Sesquiterpenes in Curcuma aeruginosa Roxb. inhibit steroid 5α-reductase and dihydrotestosterone production, and reverse androgenic alopecia. This study sought to show that a high sesquiterpene C. aeruginosa extract (CA-ext) retards axillary hair growth in women. METHODS:Thirty women (age 20-52 years) were r...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章,随机对照试验
doi:10.1159/000486136
更新日期:2018-01-01 00:00:00
abstract::Brian Barry published over 300 research articles across topics ranging from colloid science, vasoconstriction and the importance of thermodynamics in dermal drug delivery to exploring the structure and organisation of the stratum corneum barrier lipids and numerous strategies for improving topical and transdermal drug...
journal_title:Skin pharmacology and physiology
pub_type: 传,历史文章,杂志文章
doi:10.1159/000351946
更新日期:2013-01-01 00:00:00
abstract:BACKGROUND/AIM:The skin, as the outermost organ, protects against exogenous hazards (outside-in barrier) and prevents the loss of essential parts of the body (inside-out barrier). The epidermal barrier exerts several functions with specific morphological elements. Regional differences in skin functions are well known. ...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000330721
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:About 50% of the sun's radiation arriving on earth is visible light (VIS). For a long time, its effects on human health have not been fully investigated. But recently, the influence of VIS has gained more attention, especially regarding skin physiology. Studies showed various effects, many of them harmful, c...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000501131
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:The Cosmetics Europe ADME Task Force is developing in vitro and in silico tools for predicting skin and systemic concentrations after topical application of cosmetic ingredients. There are conflicting reports as to whether the freezing process affects the penetration of chemicals; therefore, we evaluated whe...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000475472
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND:Research has revealed new insights into the pathogenesis of psoriasis, leading to new therapeutic options. So far the order of changes in the pathogenesis of psoriasis is unclear. The responses to cutaneous leukotriene B4 (LTB4) application have been studied in the past as an in vivo model for inflammation. ...
journal_title:Skin pharmacology and physiology
pub_type: 临床试验,杂志文章
doi:10.1159/000354119
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:The vitamin D endocrine system, besides multiple other functions, regulates aging in many tissues, including the skin. It protects the skin against the hazardous effects of many skin age-inducing agents, including ultraviolet radiation. Thus, in the present study we aimed to investigate the relationship betw...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000443839
更新日期:2016-01-01 00:00:00
abstract::In the present study, we evaluated the protective action of cream preparations containing seven different types of marigold and rosemary extracts in vivo in healthy volunteers with experimentally induced irritant contact dermatitis (ICD). Marigold and rosemary extracts in base cream DAC (Deutscher Arzneimittel-Codex =...
journal_title:Skin pharmacology and physiology
pub_type: 临床试验,杂志文章
doi:10.1159/000085865
更新日期:2005-07-01 00:00:00
abstract:BACKGROUND:The use of antioxidants has become a common practice in the development of antiaging cosmetics. OBJECTIVE:The aim of this study was to evaluate the clinical efficacy of cosmetic formulations containing lycopene and melatonin antioxidants. METHOD:Thirty-six healthy women from 32 to 65 years were enrolled in...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000508673
更新日期:2020-01-01 00:00:00
abstract::An investigation was undertaken to determine the possible mechanisms of action of medicinal plants used for dermatological pathologies. A total of 14 plant species were selected from the readily available ethnobotanical literature. 5-Lipoxygenase and DPPH (2,2-diphenyl-1-picrylhydrazyl) assays were used to determine t...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000095253
更新日期:2006-01-01 00:00:00
abstract::Squalene is a major sebum lipid which is easily peroxidized by ultraviolet A (UVA) irradiation, generating products that can stress keratinocytes. Prevention of squalene photooxidation with antioxidants could potentially help defend skin from environmental stress. Previously, we have systematically characterized butyl...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000501731
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Percutaneous penetration of urea in vivo in man has been documented. If urea can penetrate the skin, it may also move laterally. Lateral spreading of topical substances leads to unpredictable penetration dynamics and increased skin surface area exposure. METHODS:The ability of urea, a low molecular-weight h...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000363148
更新日期:2015-01-01 00:00:00
abstract:PURPOSE:Polymethylmethacrylate (PMMA) plates generally used for the in vitro testing of sunscreens have failed to yield a satisfactory correlation between the sun protection factor (SPF) in vitro and that in vivo. In the present study, various polymers were investigated as alternative substrates to PMMA plates. PROCED...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000464471
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND/AIMS:Keloids result from aberrations in the normal wound healing cascade and can lead to pruritus, contractures and pain. The underlying mechanisms of excessive scarring are not yet understood, and most therapeutic strategies remain unsatisfactory. Psoriasin (S100A7) and koebnerisin (S100A15) are released by...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000363579
更新日期:2015-01-01 00:00:00
abstract::Neoplastic skin lesions are multifocal, diffuse skin infiltrations of particular relevance in the differential diagnosis of ulcerative, nodular, or crusting skin lesions. Nonmelanoma skin cancers (NMSCs), namely, basal cell carcinoma (BCC), squamous cell carcinoma (SCC), and also actinic keratosis (AK), are the most c...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章,评审
doi:10.1159/000479529
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Dry skin induced by rheumatoid arthritis (RA) causes itching, which negatively influences a patient's quality of life. We previously reported that mast cells are related to dry skin in arthritic mice. However, the mechanism of mast cell activation is unclear. In this study, we examined the mechanism underlyi...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000488250
更新日期:2018-01-01 00:00:00
abstract::Solid lipid nanoparticles (SLNs) can enhance drug penetration into the skin, yet the mechanism of the improved transport is not known in full. To unravel the influence of the drug-particle interaction on penetration enhancement, 3 glucocorticoids (GCs), prednisolone (PD), the diester prednicarbate (PC) and the monoest...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000324053
更新日期:2011-01-01 00:00:00
abstract:PURPOSE OF THE STUDY:To investigate the role of paraoxonase 1 (PON1) and vitamin E in the pathogenesis of some autoimmune diseases, and to correlate their levels with the disease activity. PROCEDURES:This randomized case control study was performed on 60 subjects: 45 patients [suffering from psoriasis, vitiligo and al...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000342124
更新日期:2013-01-01 00:00:00
abstract::The cyclicity of time affects virtually all aspects of our being and is the basis of the underlying rhythmicity which is typical of our lives. To 'tell time', most living organisms use internal timing mechanisms known as 'biological clocks'. These 'clocks' coordinate our physiological and behavioral functions and inte...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章,评审
doi:10.1159/000093113
更新日期:2006-01-01 00:00:00
abstract::The investigation of drug penetration into the stratum corneum (SC) by tape-stripping requires an accurate measure of the amount of SC on each tape-strip in order to determine the depth inside the SC. This study applies infrared densitometry (IR-D) to in vitro tape-stripping using the novel Squame Scan(R) 850A. The de...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000288165
更新日期:2010-01-01 00:00:00
abstract::The pH of the skin is tightly regulated by endogenous buffering systems. We examined the influence of buffers of different pH and composition on skin barrier repair, pH, inflammation, and epidermal thickness/proliferation/differentiation. After tape-stripping in hairless mice buffers with pH 4-7 were applied in patch ...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000501976
更新日期:2019-01-01 00:00:00
abstract::Combined ATR-FTIR (attenuated total reflection-Fourier transform infrared) spectroscopy and tape-stripping experiments in vitro on porcine ear skin were used to investigate the spatial distribution of different surfactants in the stratum corneum (SC). To reveal a possible connection between the size of the formed mice...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000368444
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND/AIMS:Extrinsic and intrinsic skin aging is subject to constant remodeling and degradation processes, primarily in components of the extracellular matrix. While collagen fibers thin out during the aging process, the amorphous elastin fibers accumulate. These are essential formative components of the dermis. S...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000477854
更新日期:2017-01-01 00:00:00
abstract::In a clinical study, the skin penetration properties of melatonin 0.01% in a cream and 0.01 and 0.03% in a solution were investigated by evaluation of the serum melatonin levels over a 24-hour time course in 15 healthy volunteers. Blood samples for melatonin measurements were taken at 9.00 a.m. before applying the tes...
journal_title:Skin pharmacology and physiology
pub_type: 临床试验,杂志文章
doi:10.1159/000078822
更新日期:2004-07-01 00:00:00
abstract:INTRODUCTION:Flare reactions arise due to the release of vasodilators from sensory nerves caused by antidromic transmission of action potentials after the induction of itch. OBJECTIVE:We investigated the link between flare and itch using 3 models of itch. METHODS:Skin provocations with histamine, capsaicin, and cowha...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000508795
更新日期:2020-01-01 00:00:00
abstract::Carotenoids could serve as marker substances of the antioxidant status of the human skin. In the present study, an optical skin scanner was used to analyse the carotenoid concentration obtained from 4 volunteers over a period of 13 days. The measurements were taken daily at different time points. In addition, the volu...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章
doi:10.1159/000357222
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:After birth, skin barrier function is in state of flux and at risk of dysfunction. In a prospective clinical study, we compared the effects of 2 standard cleansing procedures on skin barrier function in newborns. METHODS:Fifty-seven healthy full-term neonates aged < or = 48 h were randomly as...
journal_title:Skin pharmacology and physiology
pub_type: 杂志文章,随机对照试验
doi:10.1159/000235552
更新日期:2009-01-01 00:00:00