Formulation of Tioconazole and Melaleuca alternifolia Essential Oil Pickering Emulsions for Onychomycosis Topical Treatment

Onychomycosis is a disease that affects many adults, whose treatment includes both oral and topical therapies with low cure rates. The topical therapy is less effective but causes fewer side effects. This is why the development of an effective, easy to apply formulation for topical treatment is of high importance. We have used a nanotechnological approach to formulate Pickering emulsions (PEs) with well-defined properties to achieve site-specific delivery for antifungal drug combination of tioconazole and Melaleuca alternifolia essential oil. Silica nanoparticles with tailored size and partially hydrophobic surface have been synthesized and used for the stabilization of PEs. In vitro diffusion studies have been performed to evaluate the drug delivery properties of PEs. Ethanolic solution (ES) and conventional emulsions (CE) have been used as reference drug formulations. The examination of the antifungal effect of PEs has been performed on Candida albicans and Trichophyton rubrum as main pathogens. In vitro microbiological experimental results suggest that PEs are better candidates for onychomycosis topical treatment than CE or ES of the examined drugs. The used drugs have shown a significant synergistic effect, and the combination with an effective drug delivery system can result in a promising drug form for the topical treatment of onychomycosis.     

Formulation and Characterization of Chitosan-Decorated Multiple Nanoemulsion for Topical Delivery In Vitro and Ex Vivo

In the present study, chitosan-decorated multiple nanoemulsion (MNE) was formulated using a two-step emulsification process. The formulated multiple nanoemuslion was evaluated physiochemically for its size and zeta potential, surface morphology, creaming and cracking, viscosity and pH. A Franz diffusion cell apparatus was used to carry out in vitro drug-release and permeation studies. The formulated nanoemulsion showed uniform droplet size and zeta potential. The pH and viscosity of the formulated emulsion were in the range of and suitable for topical delivery. The drug contents of the simple nanoemulsion (SNE), the chitosan-decorated nanoemulsion (CNE) and the MNE were 71 ± 2%, 82 ± 2% and 90 ± 2%, respectively. The formulated MNE showed controlled release of itraconazole as compared with that of the SNE and CNE. This was attributed to the chitosan decoration as well as to formulating multiple emulsions. The significant permeation and skin drug retention profile of the MNE were attributed to using the surfactants tween 80 and span 20 and the co-surfactant PEG 400. ATR-FTIR analysis confirmed that the MNE mainly affects the lipids and proteins of the skin, particularly the stratum corneum, which results in significantly higher permeation and retention of the drug. It was concluded that the proposed MNE formulation delivers drug to the target site of the skin and can be therapeutically used for various cutaneous fungal infections.     

Formulation of Topical Dosage Forms Containing Synthetic and Natural Anti-Inflammatory Agents for the Treatment of Rheumatoid Arthritis

Topical anti-inflammatory and analgesic effect for the treatment of rheumatoid arthritis is of major interest because of their fewer side effects compared to oral therapy. The purpose of this study was to prepare different types of topical formulations (ointments and gels) containing synthetic and natural anti-inflammatory agents with different excipients (e.g.,: surfactants, gel-forming) for the treatment of rheumatoid arthritis. The combination of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), diclofenac sodium, a topical analgesic agent methyl salicylate, and a lyophilized extract of Calendula officinalis with antioxidant effect were used in our formulations. The aim was to select the appropriate excipients and dosage form for the formulation in order to enhance the diffusion of active substances and to certify the antioxidant, analgesic, and anti-inflammatory effects of these formulations. To characterize the physicochemical properties of the formulations, rheological studies, and texture profile analysis were carried out. Membrane diffusion and permeability studies were performed with Franz-diffusion method. The therapeutic properties of the formulations have been proven by an antioxidant assay and a randomized prospective study that was carried out on 115 patients with rheumatoid arthritis. The results showed that the treatment with the gel containing diclofenac sodium, methyl salicylate, and lyophilized Calendula officinalis as active ingredients, 2-propenoic acid homopolymer (Synthalen K) as gel-forming excipient, distilled water, triethanolamine, and glycerol had a beneficial analgesic and local anti-inflammatory effect.     

Characterization of New Egyptian Linseed Varieties and the Effects of Roasting on Their Pigments,Tocochromanols, Phytosterols,Omega-3 Fatty Acids,and Stability

The purpose of this study was to explore the effects of roasting linseeds on the pigment, lipid profile, bioactive components, and oxidative stability of the extracted oils. The linseed varieties Giza 11, Giza 12, Sakha 3, and Sakha 6 were roasted at 180 °C for 10 min, and the oils were extracted by cold pressing. The results showed that, after roasting, there was an increase in oil percentage and peroxide value, as well as small increases in p-anisidine and acid values. Roasting also caused an increase in chlorophyll content, while lutein and β-carotene tend to slightly decrease, except in the Giza 11 variety. The total phenolics content was markedly enhanced after roasting. Omega-3 fatty acids were not affected by the roasting process. The total amounts of tocochromanol were found to decrease in the Giza 12 and Sakha 6 varieties after roasting. Plastochromanol-8 increased in all varieties after roasting. The phytosterol composition was minimally affected by roasting. Roasting enhanced the stability of the extracted oils, increasing the induction period and decreasing EC50 values. These results may thus help to discriminate between the different linseed varieties and serve to recommend the use of roasting to enhance the oxidative stability of extracted oil.     

杏仁油的物化性能及其脂肪酸组成的分析

用３种不同溶剂萃取杏仁得到杏仁油,并对其物化常数进行测定。杏仁油用饱和氢氧化钾 甲醇皂化,再用甲醇 硫酸（体积比为４∶１）甲酯化后,将乙醚萃取液作气相色谱分析。太原杏仁油中脂肪酸的主要成分为油酸（Ｃ１８∶１,质量分数约６８％）和亚油酸（Ｃ１８∶２,质量分数约２５％）,少量棕榈酸（Ｃ１６∶０）、棕榈烯酸（Ｃ１６∶１）和硬脂酸（Ｃ１８∶０）,微量花生酸（Ｃ２０∶０）。     

Fatty Acid Composition of Tobacco Seed Oil and Synthesis of Alkyd Resin

The fatty acid composition of tobacco seed oil revealed that the oil is rich in unsaturated fatty acids, having linoleic acid （71.63%）, oleic acid （13.46%） and palmitic acid （8.72%） as the most abundant unsaturated and saturated fatty acids respectively. So the tobacco oil was characterized as semi-drying type on the basis of fatty acid composition. The synthesis of alkyd resin was carried out by alcoholysis or monoglyceride process using an alkali refined tobacco seed oil, pentaerythritol, cis-1,2,3,6-tetrahydrophthalic anhydride along with lithium hydroxide as catalyst. The alkyd resin so prepared was found to be bright and of low color with high gloss. The drying and hardness properties and adhesion of the tobacco seed oil derived alkyd resin were also found a bit superior to those of other alkyd resins of the same oil length. In addition, the water and acid resistance of the said alkyd was also found comparable to the other alkyds.     

Mechanisms of Penetration Enhancement and Transport Utilizing Skin Keratine Liposomes for the Topical Delivery of Licochalcone A

Keratin liposomes have emerged as a useful topical drug delivery system given theirenhanced ability to penetrate the skin, making them ideal as topical drug vehicles. However, the mechanisms of the drug penetration enhancement of keratin liposomes have not been clearly elucidated. Therefore, licochalcone A(LA)-loaded skin keratin liposomes (LALs) were prepared to investigate their mechanisms of penetration enhancement on the skin and inB16F10 cells. Skin deposition studies, differential scanning calorimetry (DSC), attenuated total reflection-Fourier Transform Infrared Spectroscopy (ATR-FTIR), and skin distribution and intracellular distribution studies were carried out to demonstrate the drug enhancement mechanisms of LALs. We found that the optimal application of LALs enhanced drug permeation via alterations in the components, structure, and thermodynamic properties of the stratum corneum (SC), that is, by enhancing the lipid fluidization, altering the skin keratin, and changing the thermodynamic properties of the SC. Moreover, hair follicles were the main penetration pathways for the LA delivery, which occurred in a time-dependent manner. In the B16F10 cells, the skin keratin liposomes effectively delivered LA into the cytoplasm without cytotoxicity. Thus, LAL nanoparticles are promising topical drug delivery systems for pharmaceutical and cosmetic applications.     

In Vitro and Human Pilot Studies of Different Topical Formulations Containing Rosa Species for the Treatment of Psoriasis

The aim of this study was to evaluate the phytochemical profile and antioxidant properties of the extracts from three Rosa species (R. canina, R. damascena, R. cairo), to develop and investigate topical formulations with lyophilized forms of extracts for the treatment of psoriasis. Phytochemical screening and in vitro total antioxidant capacity (DPPH, FRAP, CUPRAC, SOD) of studied samples were examined and compared. Lyophilized extracts of roses were dissolved in Transcutol HP and different formulations of creams were prepared. Franz diffusion method was used to evaluate the drug release and biocompatibility was tested on HaCaT cells. Rosa damascene had the best results regarding all the analyses that were conducted. After the evaluation of topical products, the formulation with Rosa damascena extract in a self-emulsifying drug delivery system was tested on a human clinical study that involved 20 patients. At the end of the clinical study an improvement in the quality of life of the patients was observed and erythema, induration and scaling were reduced. The present study indicates that our examined extracts exhibited great phenolic content, antioxidant capacity and safety profile of topical formulation and therefore can be used as a reliable source of natural antioxidants and may be used as a complementary treatment to improve the quality life of patients with psoriasis or may be tested on another diseases.     

Molecular Mechanism of Antioxidant and Anti-Inflammatory Effects of Omega-3 Fatty Acids in Perilla Seed Oil and Rosmarinic Acid Rich Fraction Extracted from Perilla Seed Meal on TNF-α Induced A549 Lung Adenocarcinoma Cells

Industrially, after the removal of oil from perilla seeds (PS) by screw-type compression, the large quantities of residual perilla seed meal (PSM) becomes non-valuable waste. Therefore, to increase the health value and price of PS and PSM, we focused on the biological effects of perilla seed oil (PSO) and rosmarinic acid-rich fraction (RA-RF) extracted from PSM for their role in preventing oxidative stress and inflammation caused by TNF-α exposure in an A549 lung adenocarcinoma culture model. The A549 cells were pretreated with PSO or RA-RF and followed by TNF-α treatment. We found that PSO and RA-RF were not toxic to TNF-α-induced A549 cells. Both extracts significantly decreased the generation of reactive oxygen species (ROS) in this cell line. The mRNA expression levels of IL-1β, IL-6, IL-8, TNF-α, and COX-2 were significantly decreased by the treatment of PSO and RA-RF. The Western blot indicated that the expression of MnSOD, FOXO1, and NF-κB and phosphorylation of JNK were also significantly diminished by PSO and RA-RF treatment. The results demonstrated that PSO and RA-RF act as antioxidants to scavenge TNF-α induced ROS levels, resulting in decreased the expression of MnSOD, FOXO1, NF-κB and JNK signaling pathway in a human lung cell culture exposed to TNF-α.     

A Mini-Review on Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: Topical Delivery of Phytochemicals for the Treatment of Acne Vulgaris

Acne vulgaris (acne) is one of the most common dermatological problems affecting adolescents and young adults. Although acne may not lead to serious medical complications, its psychosocial effects are tremendous and scientifically proven. The first-line treatment for acne is topical medications composed of synthetic compounds, which usually cause skin irritation, dryness and itch. Therefore, naturally occurring constituents from plants (phytochemicals), which are generally regarded as safe, have received much attention as an alternative source of treatment. However, the degradation of phytochemicals under high temperature, light and oxygen, and their poor penetration across the skin barrier limit their application in dermatology. Encapsulation in lipid nanoparticles is one of the strategies commonly used to deliver drugs and phytochemicals because it allows appropriate concentrations of these substances to be delivered to the site of action with minimal side effects. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are promising delivery systems developed from the combination of lipid and emulsifier. They have numerous advantages that include biocompatibility and biodegradability of lipid materials, enhancement of drug solubility and stability, ease of modulation of drug release, ease of scale-up, feasibility of incorporation of both hydrophilic and lipophilic drugs and occlusive moisturization, which make them very attractive carriers for delivery of bioactive compounds for treating skin ailments such as acne. In this review, the concepts of SLNs and NLCs, methods of preparation, characterization, and their application in the encapsulation of anti-acne phytochemicals will be discussed.     

热分离进样/气相色谱-质谱法测定橄榄油中脂肪酸乙酯

建立了热分离进样/气相色谱-质谱快速测定橄榄油中4种脂肪酸乙酯(棕榈酸乙酯、硬脂酸乙酯、油酸乙酯、亚油酸乙酯)的分析方法。采用热分离进样技术进样,以DB-5MS色谱柱分离,选择离子监测模式检测。结果显示,4种脂肪酸乙酯在0.01～0.20 mg/L范围内线性良好(r²>0.999),方法的检出限(LOD)和定量下限(LOQ)分别为0.3 mg/kg和1.0 mg/kg,在低、中、高3个加标水平(1.0、2.0、10 mg/kg)下的回收率为82.4%～109%,相对标准偏差(RSD)为0.68%～6.8%。该方法灵敏度高,准确度和重现性好,可用于橄榄油中4种脂肪酸乙酯的快速检测。     

Enzymatic Synthesis of Fatty Acid Isoamyl Monoesters from Soybean Oil Deodorizer Distillate: A Renewable and Ecofriendly Base Stock for Lubricant Industries

In this study, soybean oil deodorizer distillate (SODD), a mixture of free fatty acids and acylglycerides, and isoamyl alcohol were evaluated as substrates in the synthesis of fatty acid isoamyl monoesters catalyzed by Eversa (a liquid formulation of Thermomyces lanuginosus lipase). SODD and the products were characterized by the chemical and physical properties of lubricant base stocks. The optimal conditions to produce isoamyl fatty acid esters were determined by response surface methodology (RSM) using rotational central composite design (RCCD, 2³ factorial + 6 axial points + 5 replications at the central point); they were 1 mol of fatty acids (based on the SODD saponifiable index) to 2.5 mol isoamyl alcohol, 45 °C, and 6 wt.% enzymes (enzyme mass/SODD mass). The effect of the water content of the reactional medium was also studied, with two conditions of molecular sieve ratio (molecular sieve mass/SODD mass) selected as 39 wt.% (almost anhydrous reaction medium) and 9 wt.%. Ester yields of around 50 wt.% and 70 wt.% were reached after 50 h reaction, respectively. The reaction products containing 43.7 wt.% and 55.2 wt.% FAIE exhibited viscosity indices of 175 and 163.8, pour points of −6 °C and −9 °C, flash points of 178 and 104 °C, and low oxidative stability, respectively. Their properties (mainly very high viscosity indices) make them suitable to be used as base stocks in lubricant formulation industries.     

GC/MS法快速测定食用植物油中脂肪酸含量

脂肪酸以甘油三酯的形式存在于植物油中,我们先用KOH-甲醇方法将它转化为甲酯,用正交设计法探索出最佳的酯交换条件,整个过程5分钟可完成。然后用GC/MS/MSD进行定性定量分析。测定了8种食用植物油中六种脂肪酸的含量。     

An Analysis of Oxidative Changes and the Fatty Acid Profile in Stored Poultry Sausages with Liquid and Microencapsulated Fish Oil Additives

This study deals with the fatty acid profile and oxidative changes (TBARS) in vacuum-packed (VP) or modified-atmosphere-packed (MAP) finely-comminuted poultry sausages with liquid fish oil and microencapsulated fish oil (MC) additives. An analysis of omega-3 fatty acids (EPA and DHA) showed that their content in the samples with the fish oil additive decreased from the initial value of 0.22 g∙100 g⁻¹ of the product to 0.18 g∙100 g⁻¹ (MAP) and 0.17 g∙100 g⁻¹ (VP), respectively. After in vitro digestion, the total EPA and DHA content in the sample with microencapsulated oil amounted to 0.17 g∙100 g⁻¹ of the product. The TBARS values showed the VP samples with both forms of the fish oil additive had the lowest values on the first day of storage. Storage of the samples for 21 days caused a slight increase in the degree of lipid oxidation. The research indicated that the forms of the oil additive did not have a negative influence on the sensory features or the physicochemical properties of the sausages. The EPA and DHA levels in samples with liquid fish oil and those with oil microcapsules were sufficient for the sausage producer to declare high content of these fatty acids in accordance with the current EC regulation.     

葵子油脂肪酸2-氨基-2-甲基-丙醇化学修饰气相色谱-质谱分析

以2-氨基-2-甲基-丙醇为脂肪酸的化学修饰试剂,气相色谱一电子轰击质谱（GC-EI MS）分析葵子油脂肪酸。2-氨基-2-甲基-丙醇将脂肪酸羧基修改为含氮杂环,使在EI源中避免了链烯基中碳碳双键的移动。解析了葵子油脂肪酸2-氨基-2-甲基-丙醇化学修饰产物的EI质谱图,讨沦了烯酸中碳碳双键的定位规则,确定了葵子油脂肪酸中碳碳双键的位置。鉴定出葵子油6种脂肪酸,不饱和脂肪酸相对含量为89．41％,其中人体必需脂肪酸9,12-十八碳二烯酸含量占65．30％。本方法为不饱和脂肪酸中双键的定位提供了新的技术手段。     

2-氨基-2-甲基丙醇衍生气相色谱/质谱分析深海鱼油脂肪酸

以2-氨基-2-甲基丙醇为衍生化试剂,皂化和衍生化充氮气保护,柱前衍生气相色谱／EI质谱分析深海鱼油脂肪酸。通过修改官能团抑制了脂肪链中碳碳双键的移位,并使质谱呈现显示双键位置的规范信息。解析隐藏羧基的脂肪酸衍生物2-烯基-4,4-二甲基噁唑的质谱图,确定了深海鱼油多不饱和脂肪酸中双键的位置。共鉴定出23种脂肪酸。结果表明：深海鱼油由C12～C22脂肪酸组成,多不饱和脂肪酸含量占56．82％(峰面积百分比,下同),其中以9,12,15-十八碳三烯酸(6．96%),9,12-十八碳二烯酸(7．15％),5,8,11,14,17-二十碳五烯酸(20．83％),5,8,11,14-二十碳四烯酸(2．15％),4,7,10,13,16,19-二十二碳六烯酸(12．7％)和4,7,10,13,16-二十二碳五烯酸(2．59％)为主。为多不饱和脂肪酸中双键的定位提供了新的技术手段。     

Development of an Analytical Methodology for Quantification of Strong Acid in Diesel Oil

Many factors can affect the quality of diesel oil, in particular the degradation processes that are directly related to some organosulfur compounds. During the degradation process, these compounds are oxidized into their corresponding sulfonic acids, generating a strong acid content during the process. p‐Toluene sulfonic acid analysis was performed using the linear sweep voltammetry technique with a platinum ultramicroelectrode in aqueous solution containing 3 mol L^?1 potassium chloride. An extraction step was introduced prior to the voltammetric detection in order to avoid the adsorption of organic molecules, which inhibit the electrochemical response. The extraction step promoted the transference of sulfonic acid from the diesel oil to an aqueous phase. The method was accurate and reproducible, with detection and quantification limits of 5 ppm and 15 ppm, respectively. Recovery of sulfonic acid was around 90%.     

Effects of Seed Roasting Temperature on Sesame Oil Fatty Acid Composition,Lignan, Sterol and Tocopherol Contents,Oxidative Stability and Antioxidant Potential for Food Applications

Roasting is a key step for preparing sesame oil that leads to important changes in its organoleptic properties and quality. In this study, white sesame seeds were roasted for 20 min in an electric oven at different temperatures (120, 150, 180, 210, 250 and 300 °C). The oils extracted from unroasted and roasted seeds were compared for their chemical composition: fatty acids (including trans isomers), phytosterols, lignans (sesamin and sesamolin), tocopherols and total phenolic compounds, as well as their oxidative stability and antiradical capacity. There were no obvious differences in the oil densities, refractive indexes or iodine values, but the saponification values were affected by temperature. Relevant primary and secondary lipid oxidation were observed at T > 250 °C, resulting in a higher p-anisidine value and K232 as well as K268 values. Roasting improved oil yield (from 33.5 to 62.6%), increased its induction period (from 5.5 to 10.5 h) and enhanced the total phenolic content (from 152 to 194 mg/100 g) and antiradical activity of the extracted oil. Depending on roasting temperature, a gradual decline was recorded in total amounts of phytosterols (up to 17.4%), γ-tocopherol (up to 10.6%), sesamolin (maximum of 27.5%) and sesamin (maximum of 12.5%). All the investigated oils presented a low quantity in triglyceride polymers, clearly below the maximum tolerated quantity according to the European regulation. The optimal roasting temperature for obtaining high nutritional grade oil within the permissible values was 210 °C. The unsaponifiable components (including lignans and sterols) extracted from roasted seeds have been shown to be natural additives to fresh meatball products to extend shelf life. The results of this study may help to boost the nutritional content of plant-based diets by allowing for the use of roasted sesame seed oil and its components.     

YDHC-10催化剂用于不饱和植物油脂肪酸氢化工艺条件的研究

采用自制的催化剂YDHC-10对氢化工艺条件进行了研究。找出了植物油脂肪酸氢化时,氢化压力2MPa、氢化温度180-200℃、氢化时间60min以及催化剂浓度对植物油脂肪酸氢化的影响．