Emollients in dermatological creams: Early evaluation for tailoring formulation and therapeutic performance.

The targeted choice of the emollient of a cream determines its physicochemical properties and clinical effectiveness. This work researched the effects of emollient properties on the final characteristics and potential performance of oil-in-water dermatological creams. Seven emollients with different chemical characteristics and structures (alkane, triglyceride, ether, silicone, vegetable oils, and mineral oil) were tested in a model formulation. Early stability, pH, droplet size distribution, rheology, tackiness, adhesivity, spreadability, tribology, and release profile of a lipophilic substance model (in Franz cells, through a synthetic membrane, for six hours) were assessed. The creams had acid epicutaneous pH and a "shear-thinning" "solid-like" viscoelastic behavior. Among the seven emollients' properties, polarity, density, and viscosity were the most influential. Droplet parameters were the most impacted, pH and release were moderately affected, and the textural properties were lowly to moderately impacted. The emollient substitution in the model formulation affected the experimental parameters differently, allowing formulation optimization and tailoring its potential therapeutic performance regarding drug release, coadjutant effects, and dwell time on the skin. By looking at the creams' characteristics, it was possible to select the best-suited emollients for releasing a lipophilic drug, applying on painful skin, and formulation in wash-off products or leave-on protective barrier creams.

Formulation and characterization of a Helianthus annuus - alkyl polyglucoside emulsion cream for topical applications.

BACKGROUND: Green formulations with herbal oils and natural nonionic emulsifiers project several advantages, like favorable viscosity profiles, for use as topical applicants. Their inherent constituents also protect the skin against free radical damage and lipid peroxidation. They may hence serve as alternatives for synthetic chemical-based formulations. OBJECTIVE: Formulation and characterization of Helianthus annuus-alkyl polyglucoside cream for topical application has been attempted. Its inherent sun protection factor has been measured and compared with a similar commercial formulation. It is well known that the internal network of liquid crystals of such emulsifiers can store depot water to maintain moisturization for long time, thus bestowing beneficial dermatological effects. METHODS: Physicochemical characterization of the oil was done. The formulation process for the cream was optimized for reduced particle size with respect to ultrasonication conditions. It was characterized extensively; its inherent sun protection factor was measured and compared with a similar commercial cream. RESULTS: The cream was smooth, creamy, and showed non-Newtonian thixotropic behavior and good shear-thinning features with an SPF of 6.3 that compared favorably with a similar commercial cream. CONCLUSIONS: The cream may serve as a good topical applicant and also help in skin hydration due to the inherent nature of the emulsifier. It may protect against UV radiations due to the antioxidant and anti-inflammatory nature of the natural oil constituents. It may be used as a low-SPF formulation.

Efficacy of a moisturizer containing a pseudo-ceramide and a eucalyptus extract for Japanese patients with mild atopic dermatitis in the summer.

BACKGROUND: Skin moisturizing is advocated to take care of the skin of patients with atopic dermatitis (AD). However, many patients stop using moisturizers in the summer because of excessive sweating and high humidity. OBJECTIVES: To examine the efficacy of a moisturizing gel containing a pseudo-ceramide and a eucalyptus extract, which enhances epidermal ceramide synthesis of patients with mild AD in the summer. METHODS: We performed a single-blinded 4-week clinical trial of body care on 44 Japanese subjects who had mild AD. They had not applied any moisturizer on their body in the summer. Twenty-seven subjects used the moisturizing gel containing a pseudo-ceramide and a eucalyptus extract twice a day and the 17 other subjects did not use any moisturizer. Prior to and at the end of weeks 2 and 4, the skin conditions of each subject were evaluated. RESULTS: During the test period, the atmospheric temperature increased and skin dryness and scaling significantly improved with or without application of the moisturizing gel. However, the improvement in dryness of the treated group was significantly higher than that of the nontreated group. Erythema and itchiness were significantly improved only in the treated group. The skin hydration on the forearm increased significantly only in the treated group. Accompanying those improvements, the quality of life of the subjects, evaluated by Skindex-16® , was significantly improved. CONCLUSION: The usage of a moisturizer containing a pseudo-ceramide and a eucalyptus extract is effective for care of the skin of AD subjects even in the summer.

Safety Assessment of Plant-Derived Fatty Acid Oils.

The Cosmetic Ingredient Review Expert Panel (Panel) assessed the safety of 244 plant-derived fatty acid oils as used in cosmetics. Oils are used in a wide variety of cosmetic products for their skin conditioning, occlusive, emollient, and moisturizing properties. Since many of these oils are edible, and their systemic toxicity potential is low, the review focused on potential dermal effects. The Panel concluded that the 244 plant-derived fatty acid oils are safe as used in cosmetics.

Spreading properties of cosmetic emollients: Use of synthetic skin surface to elucidate structural effect.

The study focuses on the impact of structural and physicochemical properties of emollients on their spreadability. Fifty-three emollients, among which esters, silicones, vegetable and mineral oils, have been characterized. Their viscosity, surface tension, density and spreadability have been measured. Vitro-skin®, an artificial skin substitute, was used as an artificial porous substrate to measure spreadability. Two different methods have been selected to characterize spreadability, namely contact angle and spreading value. Dynamic contact angle measurements showed that emollient spreadability is first governed by spontaneous spreading and that, in a second phase, absorption and migration into the porous substrate becomes the driver of the extension of the spreading area. Statistical analysis of physicochemical and spreading value data revealed that viscosity has a major impact on the spreading behavior of emollients whatever their chemical type. A special emphasis was placed on the ester family in which chemical diversity is very wide. The results highlighted a difference between "high viscosity esters" for which viscosity is the main factor impacting spreadability and "low viscosity esters" for which structural variations (mono/diester, saturated/unsaturated chain, linear/branched chain) have to be considered in addition to viscosity. Linear regressions were used to express spreading value as a function of viscosity for each of the four emollient families tested (esters, silicones, vegetable and mineral oils). These regressions allowed the development of reliable predictive models as a powerful tool for formulators to forecast spreadability of emollients.

ß-Glucan-based cream (containing pleuran isolated from pleurotus ostreatus) in supportive treatment of mild-to-moderate atopic dermatitis.

BACKGROUND: Atopic dermatitis (AD) is one of the most common chronic inflammatory skin diseases with serious impact on quality of life. ß-Glucans are natural substances with potent immunomodulatory and anti-inflammatory activity. METHODS: In a multicentre open split-body study, we studied the effect of Imunoglukan P4H® cream in a group of 105 patients with AD (39 males, 37%). Evaluation of subjective (visual analogue scale, VAS) and objective (EASI score, eczema area and severity index) characteristics of AD was carried out. RESULTS: In total, 80 patients (76.2%) completed the study. Topical ß-glucan application resulted in the significant improvement of both objective and subjective symptoms of AD. On the application side, significant decline in the number of days with AD exacerbation and its severity was observed. Moreover, the subjects experienced decline of pruritus on the ß-glucan half of the body (VAS score: 1.68 vs. 1.95, p < 0.001). During the study, the continual and significant decline of EASI scores on the site of ß-glucan application was observed (V4: 1.57 vs. 1.85, p < 0.001). The preparation was in general well tolerated. CONCLUSIONS: This is the first study evaluating and confirming the potential use of ß-glucan-based cream as a supportive complementary therapy of atopic dermatitis.

Safety Assessment of Panax spp Root-Derived Ingredients as Used in Cosmetics.

The Cosmetic Ingredient Review Expert Panel (Panel) reviewed the safety of 13 Panax spp root-derived ingredients as used in cosmetics. Panax "spp" indicates that multiple species within the genus are used in cosmetics, but not all species within that genus. Four species are being considered in this safety assessment. These ingredients function mostly as skin-conditioning agents-miscellaneous, fragrance ingredients, skin-conditioning agents-humectant, skin-conditioning agents-emollient, and cosmetic astringents. The Panel reviewed available data related to these ingredients and addressed the issue of pulegone, a constituent of these ingredients and other ingredients, such as peppermint oil. The Panel concluded that these Panax spp root-derived ingredients are safe in the practices of use and concentration as given in this safety assessment.

Safety and efficacy of Sclerocarya birrea (A.Rich.) Hochst (Marula) oil: A clinical perspective.

ETHNOPHARMACOLOGICAL RELEVANCE: Sclerocarya birrea (A.Rich.) Hochst (Marula) nut oil is a popular ingredient in cosmetics such as skin lotions, lipsticks and foundations. The demand for this African oil increased tremendously such that in 2008 almost US$ 20 million was spent on Marula oil for cosmetic product manufacturing. The ethnobotanical literature states that the Zulu people in South Africa amongst others applied the oil to maintain a healthy skin. Scientific studies to support the traditional use as well as the inclusion of Marula oil in cosmetic products is lacking. This study evaluated the irritancy potential (safety), the moisturising and hydrating effects as well occlusivity properties (efficacy) of Marula oil after topical application. In addition, the Marula oil used in this study was comprehensively characterised using two-dimensional gas chromatography coupled to mass spectrometry. METHODS AND MATERIALS: Quantification of the fatty acid methyl esters (FAMEs) was done using a LECO Pegasus 4D GC × GC-MS. To determine the safety and efficacy of Marula oil healthy caucasian adult female volunteers (n = 20) who complied with the inclusion and exclusion criteria for the irritancy patch, moisture efficacy, hydrating and occlusivity tests were recruited for each study. A 2 × magnifying lamp (visual observation), Chromameter®, Aquaflux® and Corneometer® instruments were used to evaluate and monitor the irritancy level, skin barrier function, transepidermal water loss, hydrating and occlusive effects of topically applied Marula oil. RESULTS: The GC × GC-MS analysis identified several saturated as well as unsaturated fatty acids. Oleic acid was the major fatty acid constituting 69.0% of the oil followed by palmitic acid (15.3%), linoleic acid (9.2%), palmitoleic acid (4.1%) and stearic acid (1.5%). The clinical study revealed that Marula oil is non-irritant (p < 0.001), with moisturising and hydrating properties (p < 0.001) when applied to a lipid-dry (xerosis) skin. Additionally the oil exhibited occlusive effects (p < 0.001) when applied to normal skin. These findings may be linked to the absorption of the oil into the skin due to the high percentage of oleic acid and the presence of palmitic acid which are known to disturb the stratum corneum intercellular lipids. These fatty acids present in Marula oil are very similar to those present in the epidermis, and can be considered biomimetic. CONCLUSIONS: Marula oil rich in fatty acids exhibits moisturising, hydrating and occlusive properties. As the oil is non-irritating and provides a moisturising effect with moderate prevention of transepidermal water loss, average moisture retention properties and noteworthy occlusive effects, its inclusion in cosmetic products based on its traditional use may be justified depending on the application.

Formulation and evaluation of herbal anti-acne moisturizer.

The moisture content present in human skin makes it look young and the use of moisturizer results in fastening the moisture with a surface film of oil. Acne vulgaris is one of the most commonly seen diseases among the youth. The present study is focused on the use of herbs as moisturizer for acne treatment. The anti-acne moisturizer was formulated from herbal crude extracts and investigated the physico-chemical parameters as well as antibacterial activity of the formulation. The study revealed that ethanol extract of Andrographis paniculata, Glycyrrhiza glabra, Ocimum sanctum, Azadiracta indica and Green tea possessed the potential for inhibiting acne. It was observed that the optimal formula of anti-acne moisturizer was satisfactorily effective to control acne inducing bacteria i.e., Staphylococcus epidermis and Propionibacterium. The physico-chemical parameters of the formulation were also optimal with no signs of irritation.

An occlusive dressing containing betamethasone valerate 0.1% for the treatment of prurigo nodularis.

INTRODUCTION: Prurigo nodularis is a distressing condition characterized by the presence of multiple nodules associated with intense pruritus. OBJECTIVE: To assess the clinical efficacy and safety of betamethasone valerate 0.1% tape and a moisturizing itch-relief cream in prurigo nodularis. METHODS: Twelve patients were enrolled in this pilot comparison of betamethasone valerate 0.1% tape versus a moisturizing itch-relief cream containing feverfew. The study period was 4 weeks. Clinical evaluation was performed weekly. RESULTS: Eleven subjects completed the 4 weeks of therapy. The mean visual analogue scale (VAS) for pruritus at baseline was 8.75 for both sides of the body. The side treated with betamethasone valerate 0.1% tape showed a higher clinical response (VAS score at week 4: 3.9; p < 0.005) compared with the side treated with moisturizing itch-relief cream (VAS score at week 4: 5.6; p < 0.005). CONCLUSION: Both treatments were effective. However, the occlusive dressing enhanced the efficacy of the treatment, preventing scratching.

Biological and pharmacological activities of squalene and related compounds: potential uses in cosmetic dermatology.

Squalene is a triterpene that is an intermediate in the cholesterol biosynthesis pathway. It was so named because of its occurrence in shark liver oil, which contains large quantities and is considered its richest source. However, it is widely distributed in nature, with reasonable amounts found in olive oil, palm oil, wheat-germ oil, amaranth oil, and rice bran oil. Squalene, the main component of skin surface polyunsaturated lipids, shows some advantages for the skin as an emollient and antioxidant, and for hydration and its antitumor activities. It is also used as a material in topically applied vehicles such as lipid emulsions and nanostructured lipid carriers (NLCs). Substances related to squalene, including beta-carotene, coenzyme Q10 (ubiquinone) and vitamins A, E, and K, are also included in this review article to introduce their benefits to skin physiology. We summarize investigations performed in previous reports from both in vitro and in vivo models.

New emollient with topical corticosteroid-sparing effect in treatment of childhood atopic dermatitis: SCORAD and quality of life improvement.

Emollients are commonly used for their effectiveness on atopic skin, supported by a few clinical studies suggesting their potential role as corticosteroid sparing agents. We investigated the effect of a new natural emollient on corticosteroid sparing and quality of life of young atopic children and their family. Eighty-six patients (4-48 mos) with moderate atopic dermatitis were randomized by 20 pediatricians to five groups for 21 days: corticosteroids (from twice daily to one application every other day) combined or not with the studied cream (twice daily), and evaluated by SCORAD and specific quality of life questionnaires. At the end of the study, all five groups were statistically improved in terms of SCORAD and quality of life index. Thus, application of a topical corticosteroid every other day in addition to the studied cream was as effective as a once or twice daily application of the steroid alone. The studied cream had a significant impact on lichenification, excoriation and quality of life. A twice daily application of a new natural emollient provided a major corticosteroid sparing, improved lichenification and excoriation and improved the quality of life in children and their parents.

Characterization of cosmetic cream with Mesembryanthemum crystallinum plant extract: influence of formulation composition on physical stability and anti-oxidant activity.

Cosmetic or pharmaceutical composition containing superoxide dismutase (SOD) was usually used in topical administration, particularly, in fighting against skin ageing and in the protection of the skin against radiation exposure. Mesembryanthemum crystallinum is a halophyte plant widely used in the traditional medicine, characterized by the presence of anti-oxidants enzymes in responses to abiotic stresses. In the present study, we prepared a formulation with M. crystallinum extract characterized by naturally occurring SOD and catalase in association with other anti-oxidants molecules. The SOD activity was measured by 3-(4,5-dimethyldiazol-2-yl)-2,5-diphenyl-tetrazolium bromide/riboflavin method, catalase by colorimetric method and the total anti-radical activity was measured by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) method. Formulations contain a significant SOD activity (8.33 U mg(-1)), a catalase activity (0.5 x 10(7) UC) and an anti-radical activity (30% of DPPH inhibition). The formulation storage (15 days at 4 degrees C) showed a marked loss of total anti-oxidant capacity. The addition of the M. crystallinum extract induced also a reduction in formulation viscosity and pH.

Preparation and characterization of herbal creams for improvement of skin viscoelastic properties.

The aim of this study was to formulate and evaluate herbal cosmetic creams for their improvement of skin viscoelastic and hydration properties. The cosmetic cream formulations were designed by using ethanolic extracts of Glycyrriza glabra, Curcuma longa (roots), seeds of Psorolea corlifolia, Cassia tora, Areca catechu, Punica granatum, fruits of Embelica officinale, leaves of Centella asiatica, dried bark of Cinnamon zeylanicum and fresh gel of Aloe vera in varied concentrations (0.12-0.9%w/w) and characterized using physicochemical and physiological measurements. The ethanolic extracts of herbs were incorporated in a cream base that is prepared by a phase inversion emulsification technique. The cream base was prepared by utilizing oil of Prunus amagdalus, Sesamum indicum, honey, cetyl alcohol, stearic acid, polysorbate monoleate, sorbitan monostearate, propylene glycol and glycerin. Physicochemical assessments and microbiological testing were completed for all formulations according to the methods of the Indian Standard Bureau. The studies were carried out for 6 weeks on normal subjects (6 males and 12 females, between 22 and 50 years) on the back of their volar forearm for evaluation of viscoelastic properties in terms of extensibility via a suction measurement, firmness using laboratory fabricated instruments such as ball bouncing and skin hydration using electric (resistance) measurement methods. The physicochemical parameters of formulations CAA1-CAA6, i.e. pH, acid value, saponification value, viscosity, spreadability, layer thickness microbial count and skin sensitivity were found to be in the range of 5.01 +/- 0.4-6.07 +/- 0.6, 3.3-5.1 +/- 0.2, 20-32, 5900-6755 cps, 60-99%, 25-50 mum, 31-46 colony-forming units (CFU) and a 0-1 erythema score. The formulations, CAA4 and CAA5, showed an increase in percentage extensibility (32.27 +/- 1.7% and 29.89 +/- 1.64%, respectively), firmness (28.86 +/- 0.86% and 29.89 +/- 2.8%, respectively) and improved skin hydration (15.97 +/- 0.55 and 18.27 +/- 0.99%, respectively) and were found more effective compared with the control product (C7) after the 6- week study.

Effects of some emollients on the transmission of ultraviolet.

BACKGROUND/PURPOSE: Various topical agents which can be used in combination with phototherapy may have blocking or enhancing effects. In this in vivo study, the effects of topical petrolatum, basis cream, glycerine and olive oil on the transmission of ultraviolet B (UVB) were investigated. METHODS: A phototest was performed to determine the minimal erythema dose (MED) on 32 volunteers and the test was repeated with white petrolatum, basis cream, glycerine, olive oil and sunscreen (0.3 cm3/25 cm2). The effects of each agent on MED was determined after 24 h. RESULTS: MEDs were increased with the application of white petrolatum and basis cream. However, MEDs were not changed with the application of glycerine and olive oil. CONCLUSION: The application of white petrolatum and basis cream, which have blocking effects, immediately before UVB therapy is not recommended. However, glycerine and olive oil, which does not have any effect, can be used before phototherapy.

Modulation of ultraviolet (UV) transmission by emollients: relevance to narrowband UVB phototherapy and psoralen plus UVA photochemotherapy.

BACKGROUND: Patients with psoriasis undergoing or about to undergo ultraviolet (UV) phototherapy and photochemotherapy often have thick scale on their plaques which can prevent the penetration of UV radiation. Emollients are used to moisturize the skin and to prevent or reduce some of the milder side-effects ('dryness', itching) sometimes experienced during UV therapy. However, emollients can alter the UV transmission of skin and thus may alter the clinical effects of phototherapy and photochemotherapy. OBJECTIVES: We tested 30 of the topical emollients in the British National Formulary (BNF) using a standard in vitro technique used to test sunscreens. We also surveyed U.K. phototherapy units to establish routine practice for emollient use in phototherapy and photochemotherapy. METHODS: We used a standard in vitro technique to measure the monochromatic protection factors (MPFs) of 30 non-bath emollients from the BNF. An application rate of 2 mg cm-2 was used. For the assessment of effects during narrowband UVB (TL-01) phototherapy, the mean of the protection factors at 310 and 315 nm was calculated; for psoralen plus UVA photochemotherapy the mean UVA protection factor was used. A questionnaire survey was used to assess routine practice concerning emollient use prior to phototherapies in phototherapy units throughout the U.K. RESULTS: In the UVA range, 17 of the 30 emollients gave protection factors of 1.2 or above. In the UVB range, 23 of 30 had an MPF of 1.2 or above. Yellow soft paraffin had the highest protection factor in the UVB range. Of 78 centres surveyed, 57 returned completed questionnaires (73%). Seventeen of 57 (30%) centres routinely used emollients immediately prior to administering phototherapy treatments. The remaining 40 of 57 (70%) did not. Forty-five (79%) responding centres recommended the use of emollients after phototherapy. CONCLUSIONS: This study has revealed considerable variability in the practice of emollient use before phototherapy treatments. Although the majority of centres included in this study did not routinely use emollients, almost one third did. Our in vitro measurement of 30 emollients revealed marked variation in UV transmission, with many emollients blocking sufficient UV to affect the response to therapy.

[Analysis of spectral properties of oil matrix raw materials in skin care products].

There are many kinds of oil matrix raw materials used in skin care products. Their spectral properties are different. The matrix raw material that has better ultra-violet absorption will enhance the sun-screening agent effect obviously. In the present article the spectral properties of six oil matrix raw materials often used in skin care products were mainly measured and analyzed by spectrophotometer. The analysis of T-lambda spectra shows that castor oil can absorb ultraviolet as well as near infrared light. It was shown that castor oil chosen as the matrix raw material will improve the effect of sun-screening agent and enhance the products. The function of sun-screening agent and skin health care product will stand out clearly.

Effect of skin care with an emollient containing a high water content on mild uremic pruritus.

Skin care is very important for preventing uremic pruritus. However, mild uremic pruritus has usually been treated with antihistamine and urea-containing ointments. We therefore examined the effects of an aqueous gel with higher water content. Twenty hemodialysis patients with mild pruritus who were not being treated with any emollient were divided into two groups of 10 each. Patients in one group were treated with an aqueous gel containing 80% water. This emollient was applied twice daily for 2 weeks. No emollient was applied for the next 2 weeks. The other group of patients were not treated with any emollient for the 4 weeks. Visual analog scale scores for itching in the experimental group at week 2 were significantly decreased compared with that at week 0 (3.5 +/- 0.3 vs 0.6 +/- 0.2, P < 0.01). Skin dryness in the experimental group was significantly improved at week 2 compared with that at week 0. The visual analog scale score for itching increased to 1.2 +/- 0.5 and skin dryness reappeared in 40% of patients by week 4, i.e. after the emollient was stopped. There were no significant changes in the control group during the study. It is concluded that the aqueous gel with high water content reduced itching and improved xerosis in patients with mild uremic pruritus. It is reasonable that skin care with an emollient containing a high water content is first started for hemodialysis patients with xerosis, even if they do not feel itching.

Effects of topical petrolatum and salicylic acid on the erythemogenicity of UVB.

Various topical agents used in combination with phototherapy have blocking effects, however in contrast to in vitro studies there were not enough in vivo studies about this subject. Our purpose was to examine the photoprotective effects of white petrolatum and salicylic acid which can be used before UVB therapy in psoriasis patients. In 35 volunteers, a phototest was performed to determine the minimal erythema dose (MED) and the test was repeated with thin (0.1 cc/25 cm2) and thick (0.3 cc/25 cm2) petrolatum, thin and thick salicylic acid (20%) in petrolatum and sunscreen. After 24 hrs, the effects of each agent on MED was investigated. MED values detected after pure UVB and after application of topical agents were compared one by one, and the differences between all of them have been found statistically significant. These showed that MED values were increased by thin or thick petrolatum and also by thin and thick salicylic acid (20%) in petrolatum. The highest MED values were detected with thick salicylic acid in petrolatum followed by thin salicylic acid in petrolatum, thick petrolatum and thin petrolatum. The application of petrolatum and salicylic acid, which can block UVB, before phototherapy is not recommended.