Housty & Hospital, 1967) and the β form crystallizes in C2/c (Housty & Hospital, 1967). For both polymorphs, the structures present in the CSD (AZELAC10 and AZELAC01; Allen & Kennard, 1993) are derived from room-temperature data with R factors ca 10% and ambiguities in the treatment of H atoms. We have, therefore, re-examined azelaicacid and report here the structure of the β form measured at 180 K to significantly greater precision.
Fig. 3 indicates the score measurement of the baseline sebum level of the skin versus SER values in the same patients (r= 0.76,p<0.OOl). Azelaicacid could significantly reduce the grade of acne lesions (Fig. 4) and this reduction was related to SER.
Purpose: To design, develop and evaluate an Azelaicacid encapsulated Ethosomal formulation for acne. Methods: Encapsulated ethosomes were prepared by three methods viz. hot method, cold method and thin film hydration method. Central Composite Design was employed for optimisation of ethosomal formulations. Concentrations of phospholipid, cholesterol and ethanol were selected as independent variables and their effect on the dependent variables (Entrapment Efficiency and Drug Diffused) was studied. The optimised vesicular carriers were evaluated for vesicle size, entrapment efficiency, in-vitro and ex-vivo diffusion studies, anti-microbial activity, skin irritation studies and stability studies as per ICH guidelines. Ethosomal formulations with varying soya phosphatidylcholine, cholesterol and ethanol were prepared. Results: Vesicles were spherical, unilamellar with a smooth surface. The optimised formulation showed a vesicle size of 4.25 ± 1.35 μm and entrapment efficiency of 91.86 ± 2.25%. In-vitro and ex- vivo drug diffusion of the ethosomal gel was compared with a conventional gel and a marketed cream. The developed novel formulation exhibited enhanced anti-acne activity as compared to conventional gel and a marketed cream. Conclusion: We can conclude that the ethosomal formulation is an efficient vesicular carrier system for topical delivery.
The study is designed to develop a simple, rapid, selective and robust stability indicating reversed phase- high performance liquid chromatography method for quantitative analysis of azelaicacid in pharmaceutical preparations. The chromatographic separation and estimation of azelaicacid was carried out using a Waters high-performance liquid chromatography system employing Kromasil 100-5C18 column (250× 4.6 mm; 5 µm particle size) as a stationary phase. The mobile phase comprised of 75 volumes of sodium di-hydrogen orthophosphate (pH 3.5; 50 mM) and 25 volumes of acetonitrile, eluted at a flow rate of 1.2 ml/min. The eluents were monitored at 206 nm using 2487 dual wavelength ultra violet detector. The method was developed and validated in terms of stability as per International Conference on Harmonisation and Center for Drug Evaluation and Research guidelines. A linear relationship between peak area and concentration of azelaicacid was observed in a concentration range of 5-400 µg/ml (correlation coefficient, r 2 = 0.998). The method showed acceptable levels of precision (%RSD ≤2), accuracy (>96 % recovery),
Background: Pigmentation in human skin is an important defense mechanism against sunlight or oxidative stress. Despite the protective role of melanin, abnormal hyperpigmentation such as freckles and chloasma sometimes can be serious aesthetic problems. Because of these effects of hyperpigmentation, people have considered the effect of depigmentation. Azelaicacid (AZ) is a saturated dicarboxylic acid found naturally in wheat, rye, and barley.
The present study deals with the oxidative cleavage of oleic acid (OA) using hydrogen peroxide and tungstic acid as a catalyst to produce azelaicacid. A two-step method has been expanded for the optimization of a new route of azelaicacid synthesis with the addition of sodium hypochlorite as the co-oxidation. The Central Composite Design (CCD) and Response Surface Methodology (RSM) were performed to optimize the production of azelaicacid. The interaction effect among catalyst concentration, substrate molar ratio and temperature were done for optimization the conversion of oleic acid. Maximum oleic acid conversion of 99.11% was reached at substrate molar ratio of 4/1 (H 2 O 2 /OA), a catalyst concentration of 1.5% (w/wOA) and temperature of 70 o C. The GC analysis
Increased conversions can occur because high temperatures can increase the reaction rate and can increase transfers between substrates . At temperature more than 75 o C the catalyst is less actively working. This condition indicates that temperature can also trigger the catalyst activity on the substrate in the synthesis of azelaicacid. The use of high temperatures can cause the catalyst to undergo a denaturation process. If this process occurs, the catalyst will decrease and the reaction rate will decrease. This condition greatly affects the resulting % conversion, in which the catalyst is no longer able to transfer oxygen in oxidative breakdowns in the synthesis of azelaicacid.
Transfersome was prepared by thin layer hydration method. Transfer some formulation of azelaicacid shown in Table 1. Phospholipid was dissolved in dichlormethane, azelaicacid was dissolved in ethanol. Those lipid phase were mixed in a roundbottom flask, and then evaporated by rotary evaporator under temperature 53°C and 50150 rpm, which was applied for 2.5 h. Streamed with N 2 gas and closed using wrap plastic,
From the decades, it has been reported in the literature that topical treatment of acne is more effective as compared to systemic therapy. It is because of its occurrence in the pilosebaceous unit of the skin. In this study, azelaicacid is selected as a model drug. It is a naturally occurring aliphatic dicarboxylic acid found in whole grain cereals and animal products. It possesses various biological activities with topical application. It has demonstrated efficacy in the treatment of acne vulgaris, rosacea, and various hyperpigmentary disorders. Due to its poor water solubility it results in difficulties in the preparation of topical formulation. The present investigation aims to reduce the concentration of the active drug concentration of azelaicacid by maintaining the therapeutic efficacy by using different types of penetration enhancers. In this study, hydrogel based polymer is used for preparation of formulation i.e. carbopol. Due to its high stability, good bio-compatibility and less toxicity it is used. In this study, two penetration enhancers were used dimethylsulphoxide (DMSO) and piperine.
All chemicals and solvents were purchased from Sigma Aldrich (UK), unless otherwise indicated. Novozym 435 (CaLB immobilised on cross-linked acrylic resin beads) was kindly donated by Novozymes (Denmark) stored at 4 °C and dried for 24 h under vacuum (100 mbar) at room temperature (RT) before use. Azelaicacid was purchased from Alfa Aesar (UK) and dried for 24 h under vacuum (100 mbar) at 50 °C before use. The other reagents were dried at RT for 24 h under vacuum (100 mbar) before use. All the solvents were of analytical grade, or Chromasolv® were specified, and used as received. Supercritical Fluid Chromatography (SFC) grade 4.0 CO 2
cream control once daily switched to azelaicacid 15% gel twice daily. In studies 1 and 2, ivermectin 1% cream showed increasing efficacy from week 12 to week 52. In study 1, the percentage of patients with IGA score of “clear” or “almost clear” increased from 38.4% at week 12 to 71.1% at week 52. In study 2, the percentage of patients with IGA score of “clear” or “almost clear” increased from 40.1% at week 12 to 76.0% at week 52. Most of the patients who received ivermectin 1% cream in either study 1 or study 2 denied stinging, burning, dryness, or itching associated with the medication, whereas more subjects who received azelaicacid 15% gel twice daily reported these symptoms. The initial and follow-up studies demonstrated that ivermectin 1% cream is an appropriate long-term therapy for papulopustular rosacea as the medication was effective and safe for 52 weeks of treatment. 2,31
Chemical peels are one of the most frequently used agents for acne treatment. 13,14 The repeated peeling of the epidermis layer of the skin stimulates the upper dermis to produce new collagen, leading to regeneration and remo- deling of the skin, improved texture and reduction in sur- face abnormalities. 14,15 AA (azelaicacid) is also helpful to reduce the hyperpigmentation that may occur following in ﬂ ammation, without inducing bacterial resistance. 16,17 AA has an established history of effectiveness; however, PA is a newer, safer, and potentially more effective peeling agent. 13,14 However, to our best knowledge, no study compares the effectiveness of treatment with AA and PA peeling on subjective QOL in young adult women. There is also scarce evidence comparing systemic and local therapies. 5 The study ’ s objective is to parallel the ef ﬁ cacy of acne treatment using AA and PA peels in the subjective assessment of QOL in young adult women.
Abstract: Acne vulgaris is a common skin disorder that can affect individuals from childhood to adulthood, most often occurring in the teenage years. Acne can have a significant physical, emotional, and social impact on an individual. Many different treatment options are available for the treatment of acne vulgaris. Commonly used topical treatments include benzoyl peroxide, antibiotics, sulfur and sodium sulfacetamide, azelaicacid, and retinoids. Systemic treatment is frequently used and includes the use of systemic antibiotics, oral contraceptives, antiandro- gens, and retinoids. Other treatment modalities exist such as the use of superficial chemical peels as well as using laser and light devices for the treatment of acne. With the multitude of treatment options and the rapidly expanding newer technologies available to clinicians, it is important to review and be aware of the current literature and studies regarding the treatment of acne vulgaris.
Background: Acne vulgaris is a common disorder affecting 79% - 95% of the adolescent popula- tion. The choice of treatment depends on the severity, patients with mild to moderate acne should receive topical therapy such as azelaicacid. Rising antibiotic drug resistance consequent to the widespread use of topical antibiotics is causing concern and effective non-antibiotic treatments are needed. Objective: To compare the efficacy and side effects of topical azelaicacid cream 20% versus active lotion containing triethyl citrate and ethyl linoleate (TCEL) in treatment of mild to moderate acne vulgaris. Patients and Methods: This single, blinded, comparative, therapeutic study was done in the Department of Dermatology-Baghdad Teaching Hospital, Baghdad, Iraq; from May 2013-July 2014. Scoring of acne was carried out and the patients were examined every 2 weeks for 10 weeks of treatment. One month after stopping drugs, patients were evaluated for drug complications and disease recurrence. Sixty patients fulfilling enrollment criteria were in- cluded in this study. Patients were divided into 2 groups: Group A (30 patients) treated twice daily with TCEL lotion and Group B (30 patients) treated twice daily with topical azelaicacid cream 20%. Results: Both topical TCEL lotion and azelaicacid cream were statistically an effective therapy for treatment of mild to moderate acne vulgaris. TCEL lotion was more effective and act earlier than
DOI: 10.4236/ojapps.2018.811042 529 Open Journal of Applied Sciences fluence of pathogenic bacteria and antagonist, the types of organic acid increased to 51.61%, with a rise of 21.44% and 15.35% respectively. The change rule of root exudates of black shank pathogen and its antagonist was similar to that of bac- terial wilt pathogen and its antagonist. However, the types of organic acid in- creased to 47.22% and 53.33%, with a rose of 28.18% and 12.93%. Data has shown that through the treatment of bacterial wilt, black shank pathogen and their antagonistic bacteria, the content of propionic acid, isophthalic acid, myristic acid, ethyl benzoate and azelaicacid fluctuated abundantly, while the control group was 0. The treatment group of bacterial wilt pathogen reached the highest its peak, and the content decreased to 0 after the addition of antagonistic bacteria, followed by terephthalic acid and benzoic acid, which increased from 0.78 to 1.53 and 2.27 respectively, yet decreased to 0.86 and 1.01 separately after adding antagonistic bacteria. The results showed that propionic acid, isophthalic acid, myristic acid, ethyl benzoate and azelaicacid were direct inducers of bac- terial wilt and black shank pathogens, and their antagonistic bacteria could alle- viate harmful bacteria that induced tobacco to produce allelochemicals (tereph- thalic acid, isophthalic acid and benzoic acid). The dramatical increase of the abundance of pathogen in soil was a vital factor which led to continuous crop- ping obstacles. It was speculated that the possible mechanism was due to the in- crease of the abundance of pathogen , which induced crops to produce alle- lopathic substances, thus allelochemicals provide nutrients for the colonization of harmful bacteria. It formed a vicious circle that eventually resulted in conti- nuous cropping obstacles. Although this conjecture needs further confirmation, the study provides new clues for exploring tobacco continuous cropping disord- ers and soil-borne diseases.
(a conservative uncertainty and systematic errors were con- sidered on vapour pressures). A different method was used by Booth et al. (2009), who directly measured the steady- state vapour pressure using the Knudsen effusion mass spec- trometry (KEMS) method with a solid sample. In Booth et al. (2009), the working pressure and heating method of the sample was similar to ours: there was a temperature step of 5 ◦ C considering 10 min of stabilization time. The enthalpy obtained for adipic and succinic acids is smaller than that measured in this work and is larger than that for the ox- alic acid. However, it should be noted that their measure- ments are affected by a large uncertainty; in particular, the errors obtained for oxalic acid (19 kJ mol −1 ) are the result of the variation in the three calibration compounds used for that determination, whereas the high error on the adipic acid (26 kJ mol −1 ) is the result of low pressures, resulting in de- creased signal-to-noise ratio. Regarding the oxalic acid, as discussed above, it is highlighted that these authors mea- sured the value of the α-orthorhombic anhydrous form and a difference from our results is expected. This difference is evident in de Wit et al. (1983) results, where the analysis of the dehydrate and anhydrous form (prepared by a prolonged evacuation of the hydrate substance and vacuum sublima- tion) of the oxalic acid has been performed. The enthalpy of sublimation of oxalic acid, as listed in Table 4, agrees within 5.5 % of the average value obtained from the dehy- drated results (de Wit et al., 1983; Granovskaya, 1948). In- stead, Ribeiro da Silva et al. (1999, 2001) present Knudsen mass-loss effusion, a method similar to Booth et al. (2009) in order to study the vapour pressures of crystalline dicar- boxylic acids at much higher temperatures. The vapour pres- sures were calculated with a Langmuir equation, whereas the enthalpy of sublimation at the mean temperature was de- rived by the Clausius–Clapeyron equation. Ribeiro da Silva et al. (1999) results show larger values than ours (Table 4): 32 kJ mol −1 for azelaicacid (Ribeiro da Silva et al., 1999) and 10 kJ mol −1 for succinic acid (Ribeiro da Silva et al., 2001). As stated by Bilde et al. (2015) the enthalpy of subli- mation values between the different experimental methods can differ by tens of kilojoules per mole. The results of Davies and Thomas (1960), who measured heat and entropy of sublimation by means of the effusion method at 1.013 bar pressure, are in agreement with our values (within 9.5 % for adipic acid and within 4 % for succinic acid). Albyn (2001) used two different 15 MHz microbalances cooled at − 42 ◦ C in a vacuum chamber to measure the deposition rates of adipic acid from 25 to 60 ◦ C. The enthalpy of sublimation
In oil painting the binding medium used by artists is a drying oil which allows effective color application and helps in providing optic properties to pigments in drying place. Linseed oil, walnut oil and poppyseed oil are trad- itionally used in paintings. Different characteristic can be considered for identifying a binding medium. Therefore, one or more characteristic components of the oil used, should be detected. For example, a lipidic fraction may be characterized according to certain mono- or di-carboxylic fatty acids, or by using the ratio between azelaicacid and palmitic acid, or the one between palmitic acid and stearic acid. During ageing, drying oils show the production and progressive increase of dicarboxylic acids, while saturated fatty acids are so stable that they are not involved in the oil polymerization process. The palmitic and stearic acid concentrations change due to the evaporation over time but their ratio remains more or less stable. Several authors have evaluated the efficiencies of the ratio between pal- mitic acid and stearic acid (P/S) as an identifying param- eter of linseed, walnut and poppyseed oil. They found P/S values included in the range 1.4-1.9 for linseed oil [20,32- 34]; 2.4-2.9 for walnut oil [20,32-34]; 2.9-3.7 for poppyseed oil [34-38]. Starting from these considerations, over the chromatographic profile above reported, we found pres- ence of both saturated acids (palmitic acid and stearic
The effect of temperature on the removal of the aliphatic dicarboxylic acids by ZnO was tested using different temperatures in the range of 20-60 °C. Figure 5 displays the effect of the temperature on the adsorption of Malonic acid, Succinic acid, Adipic acid, and Azelaicacid on ZnO. There is clearly good adsorption efficiency at low temperature with initial values of about %70. As the temperature increased, the level of the acid removal decreased for all considered acids. This suggests that adsorption process of the studied acids is an exothermic process, and rising the temperature would result in reducing the adsorption ability (21).
Unlike LC–MS or NMR, GC–MS we used in the present study prefers to offer information about primary metabo- lites, such as sugar, protein, lipid and organic acids et al. Generally, primary metabolites could be the precursors for the secondary metabolites, like various terpenoids including cyasterone. In the present study, a wild range of variation of primary metabolites that related sugar metabolism showed regular change in different growth years, like mannose, acetol and d-glyceric acid (detail see Additional file 3). Those metabolites related sugar metabolism pathway could further offer some important metabolic intermediates, like pyruvic acid and phos- phoglyceraldehyde, which were used in the biosynthesis pathways of terpenoids .
donebecause it was not distinctly isolated) showed anti- MRSA activities at 2.0 mg/ml. The least mean zone of inhibition against MRSA isolates was 8.0 mm for F5 and the highest was 22.5 mm for F2 and F3. There was significant difference in anti-MRSA activities between the fractions (P<0.05). Fractions with mean values with different letters were significantly different in activities from each other (P<0.05) while fractions with same letter were not significantly different from each other (P>0.05). Table 2 shows the GC-MS analysis of chemical contents of the fractions (except F6 which was not done as it was lost). F1 contained: camphene (20.5%), α-pinene (20.0%), cymene (18.0%), 1.8-cineole (10.0%), linalool (8.0%), hexanoic and octanoic acid (2.0% each). The total of chemical content identified was 80.5%. F2: camphene (50.0%), α-pinene (30.0%), cymene (10.0%), linalool (5.0%), undecanone, octanoic and decanoic acids were in traces. The total was above 95%. F3: decanoic