Natural Polyphenols Selectively Inhibit β‐Carbonic Anhydrase from the Dandruff‐Producing Fungus Malassezia globosa: Activity and Modeling Studies

Around 50 % of the worldwide population is affected by dandruff, which is triggered by a variety of factors. The yeast Malassezia globosa has been labeled as the most probable causative agent for the onset of dandruff. The β‐carbonic anhydrase (CA) of MgCA was recently validated as an anti‐dandruff target, with its inhibition being responsible for in vivo growth defects in the fungus. As classical CA inhibitors of the sulfonamide type give rise to permeability problems through biological membranes, finding non‐sulfonamide alternatives for MgCA inhibition is of considerable interest in the cosmetic field. We recently screened a large library of human (h) CA inhibitors for MgCA inhibition, including different chemotypes, such as monothiocarbamates, dithiocarbamates, phenols, and benzoxaboroles. Herein, we expanded the research toward new MgCA inhibitors by considering a set of natural polyphenols (including flavones, flavonols, flavanones, flavanols, isoflavones, and depsides) that exhibited MgCA inhibitory activity in the micromolar range, as well as selectivity for the fungal isozyme over off‐target human isoforms. The binding mode of representative derivatives within the MgCA catalytic cleft was investigated by docking studies using a homology‐built model.     

Efficacy of a piroctone olamine/climbazol shampoo in comparison with a zinc pyrithione shampoo in subjects with moderate to severe dandruff

Dandruff is a chronic scalp disorder characterized by scaling and itching. A successful anti‐dandruff shampoo not only has to provide superior anti‐dandruff relief to ensure patient compliance. It also needs to offer excellent cosmetic and hair conditioning benefits at the same time. In this study, the efficacy of a shampoo containing 0.5% piroctone olamine and 0.45% climbazole (shampoo 1) was compared with a widely available commercial shampoo containing 1% zinc pyrithione (shampoo 2). In vitro studies investigating the anti‐mycotic efficacy of a combination of 0.5% piroctone olamine and 0.45% climbazole as well as 1% zinc pyrithione were performed. To study substantivity, pig skin punches were used as a model system and a test of wet combability was performed to characterize combing ease. In vivo home‐in‐use studies were carried out to determine the efficacy of both shampoos to improve scalp condition and reduce itching in subjects suffering from moderate to severe dandruff. Results demonstrated a comparable anti‐fungal effectiveness for 0.5% piroctone olamine plus 0.45% climbazole and 1% zinc pyrithione, respectively. Shampoo 1 showed a significantly higher anti‐mycotics substantivity compared to shampoo 2. After treatment with shampoo 1, the wet combing force was significantly reduced compared with shampoo 2, suggesting a better combability following the use of shampoo 1. In an in vivo split head design study, shampoo 1 was shown to be equally effective in reducing the amount of dandruff on the scalp compared with shampoo 2. The approval rate of volunteers regarding the question ‘The use of this shampoo decreases the itching of my scalp?’ after a 4‐week treatment with shampoo 1 equaled 90%. Overall, the shampoo formulation with 0.5% piroctone olamine and 0.45% climbazole effectively reduces the amount of dandruff and, at the same time, provides hair conditioning advantages.     

天然蛋白去屑止痒剂在化妆品中的应用与展望

概述了头皮屑及其形成的机理,同时介绍了新型去屑止痒剂——天然蛋白去屑止痒剂的产品性能及其在日化行业中的应用情况,并对该产品在日化行业中的应用进行了展望。     

Nudging hair shedding by antidandruff shampoos. A comparison of 1% ketoconazole, 1% piroctone olamine and 1% zinc pyrithione formulations

Hair shedding and hair thinning have been reported to be affected by dandruff and seborrhoeic dermatitis. The present study was conducted in 150 men presenting with telogen effluvium related to androgenic alopecia associated with dandruff. They were randomly allocated to three groups receiving each one of the three shampoos in the market containing either 1% ketoconazole (KTZ), 1% piroctone olamine (PTO) or 1% zinc pyrithione (ZPT). Shampoos had to be used 2-3 times a week for 6 months. Hair shedding during shampoo was evaluated semiquantitatively. Hair density on the vertex was evaluated on photographs using a Dermaphot. Trichograms were used for determining the anagen hair percentage and the mean proximal hair shaft diameter using computerized image analysis. The sebum excretion rate (SER, mug cm(-2) h(-1)) was also measured using a Sebumeter. The three treatments cleared pruritus and dandruff rapidly. At end point, hair density was unchanged, although hair shedding was decreased (KTZ: -17.3%, PTO: -16.5%, ZPT: -10.1%) and the anagen hair percentage was increased (KTZ: 4.9%, PTO: 7.9%, ZPT: 6.8%). The effect on the mean hair shaft diameter was contrasted between the three groups of volunteers (KTZ: 5.4%, PTO: 7.7%, ZPT: -2.2%). In conclusion, telogen effluvium was controlled by KTZ, PTO and ZPT shampoos at 1% concentration. In addition, KTZ and PTO increased the mean hair shaft thickness while discretely decreasing the sebum output at the skin surface.     

十一烯酸单乙醇酰胺琥珀酸酯磺酸钠合成工艺改进研究

在传统工艺基础上 ,采取以活性炭脱色代替减压蒸馏、酰胺无需精制等改进、精简措施 ,合成了符合质量规格要求的十一烯酸单乙醇酰胺琥珀酸酯磺酸钠盐 ,并探讨了 pH值、温度对产品透明度的影响 ,实验表明 ,pH值小(<7)、温度高 ,则产品的透明度就好。     

Enhanced efficacy and sensory properties of an anti‐dandruff shampoo containing zinc pyrithione and climbazole

Dandruff is a common complaint and is suffered by as much as half of the population at some time post puberty. The condition is characterized by the presence of flakes on the scalp and in the hair, and is often accompanied by itch. The most common treatment for dandruff is the use of shampoo formulations that contain fungistatic agents such as zinc pyrithione (ZPT) and octopirox. Whilst most antidandruff shampoos are effective in resolving the symptoms of dandruff these shampoos can often result in hair condition that is less than acceptable to consumers which can lead to a tendency for them to revert to use of a non‐antidandruff shampoo. This can result in a rapid return of dandruff symptoms. The aim of this investigation was to study the impact of using a combination of antidandruff actives and silicones on the resolution of dandruff and to deliver superior sensory properties to the hair. We have demonstrated that shampoo containing the dual active system of ZPT/Climbazole deposits both active agents onto a model skin surface (VitroSkin) and reduces Malassezia furfur regrowth in vitro. Clinical evaluation of the dual active shampoo demonstrated superior efficacy and retained superiority during a regression phase where all subjects reverted to using a non‐antidandruff shampoo. We have also demonstrated that it is possible to deposit silicone materials from antidandruff shampoo uniformly over both virgin and damaged hair fibres that results in smoother hair fibres (as evidenced by reduced dry friction). This combination of antidandruff agents and conditioning silicones delivered from a shampoo provides subjects with superior antidandruff efficacy and desired end sensory benefits ensuring compliance and longer term dandruff removal.     

Zinc‐containing compounds for personal care applications

It is well‐known that zinc ions are widely used in cosmetic products. Their popularity is associated with the multifunctional profile of Zn²⁺, which is classified as an essential chemical element in the human body. This review examines numerous beneficial biological properties of zinc‐containing compounds and classifies the compounds used in cosmetic products according to their functionality profile: antioxidant, sunscreen, anti‐inflammatory, anti‐pigmentation, anti‐ageing, anti‐acne, antimicrobial, anti‐odour, cleansing or stabilizing activity. It also underlines the significance of zinc in enzymatic processes, which depends on the enzyme type acts as inhibitor or enzymatic stimulator. Moreover, the article describes the chemical nature of the most interesting groups of Zn compounds.     

Safety and efficacy of lotilaner ophthalmic solution, 0.25% for the treatment of blepharitis due to demodex infestation: A randomized,controlled, double-masked clinical trial

PurposeTo evaluate the safety and efficacy of lotilaner ophthalmic solution, 0.25% for the treatment of blepharitis due to Demodex infestation compared to vehicle control.MethodsIn this phase II, randomized, controlled, double-masked clinical trial, 60 eligible participants with Demodex blepharitis were randomly assigned in a 1:1 ratio to receive either topical lotilaner ophthalmic solution, 0.25% (Tarsus Pharmaceuticals, Inc., Irvine, CA) (study group) or the vehicle without lotilaner (control group) bilaterally twice a day for 28 days. Participants were followed at Days 7, 14, 28, 60 and 90. The efficacy parameters were change in collarette grade and Demodex density at Day 28. Safety parameters were adverse events, changes in corrected distance visual acuity (CDVA), intraocular pressure (IOP) and slit-lamp biomicroscopy.ResultsThe study group showed a statistically significant decrease in collarette grade compared to the control group beginning at Day 14 (p = 0.003) in the upper eyelid and at Day 28 (p = 0.003) in the lower eyelid. Decreases in both lids were maintained through Day 90 (p < 0.001). At Day 28, mite eradication was achieved in 66.7% and 25.9% of eyes in the study and control group (p = 0.005); at Day 90, these proportions were 68.2% and 18.5% (p = 0.001), respectively. No serious adverse events or clinically significant changes in CDVA and IOP were observed.ConclusionFor Demodex blepharitis, treatment with lotilaner ophthalmic solution, 0.25% for 4 weeks is safe and effective. The improvement in collarette grade and mite density observed during the treatment period persisted for at least two months following treatment cessation.