PEG-40 Hydrogenated Castor Oil Research Articles

Antinociceptive activity of transdermal nanostructured surfactant-based systems containing duloxetine hydrochloride

Duloxetine hydrochloride (DLX) is a serotonin and norepinephrine reuptake inhibitor that is effective in the treatment of chronic pain. However, the drug has several adverse reactions and extensive hepatic first-pass effect. This study aimed at developing surfactant-based formulations such as liquid crystals (LCs) and evaluating the influence of the formulations on DLX skin permeation and in vivo antinociceptive activity. Thereafter, the formulations were obtained using PEG-40 Hydrogenated Castor Oil, Tween 80, licuri oil and water. The systems selected showed isotropy, high viscosity and rheology suggestive of LCs. The systems presented ability to permeate DLX through the skin. ATR-FTIR demonstrated that formulations promoted lipid disorganization and modification of protein conformation, facilitating the drug diffusion through the stratum corneum. Moreover, the formulation loaded with DLX showed high antinociceptive activity in mice (tests of acetic acid-induced abdominal writhing, formalin and tail immersion) via the transdermal route. The antinociceptive activity was close to that of morphine (i.p.). In conclusion, the LC obtained proved to be a promising system for transdermal delivery of DLX and pain management.

Cosmetic degradation: A study on body lotions with botanical extracts

Lipid oxidation is a spontaneous process in fats and, consequently, in products with significant fat content. Many cosmetics fall into this category, presenting an intrinsic relationship between the productʼs quality, oxidation capacity, and market value. This study comprehensively investigated the aging of body lotions, accentuating the role of their chemical formulations. Sensory analysis clarified that controlled temperature-induced aging significantly altered the lotions' appearance, texture, color, and, to a lesser extent, odor, hinting at the onset of rancidity. As lipid peroxidation unfolds, the emergence of secondary oxidation products like aldehydes, ketones, and alcohols becomes prominent. These secondary products indicate a potential degradation in the lotion's quality and efficacy. Quantifying the primary oxidation products was possible using methods like the quantification of Conjugated Dienes (CD) expressed in percentage and the Peroxide Index (PI) method expressed in meqO2/kg of a dry sample. On the other hand, methods such as the p-Anidisine Index (pAi) and the thiobarbituric acid reactive substances (TBARS) with malonaldehyde (MDA) expressed as malonaldehyde concentration (mg/g of dry sample) provided the quantification of secondary oxidation products. Regarding lipid oxidation, lotions containing sunflower and soybean oils emerged as notably susceptible. Conversely, samples that demonstrated minimal oxidation, were attributed to protective elements such as Aloe barbadensis and Calendula officinalis extracts. Examining into secondary oxidation, four samples displayed the highest TOTOX values, indicating extensive oxidation. A discernible correlation was observed between TOTOX values and natural extracts' presence (or lack), underscoring their protective or exacerbating roles. Certain natural ingredients, including A. barbadensis leaf juice powder and C. officinalis flower extract, were recognized as supporters against oxidation. Yet, components like PEG-40 hydrogenated castor oil can, paradoxically, seem to intensify the oxidative cascade. This research provides crucial insights into the interplay between natural extracts and lipid oxidation in body lotions. The elucidated results accentuate the necessity for judicious ingredient selection, balancing the inclusion of natural extracts to ensure product quality, longevity, and safety.

The substantiation of the composition and technology of obtaining a microemulsion in laboratory conditions for pediatric use

Aim. To substantiate the composition and parameters of the technological process of obtaining a microemulsion with the essential oil of common fennel fruit for pediatric use. Materials and methods. The study objects were experimental samples of an emulsion with fennel essential oil (active pharmaceutical ingredient), acacia, xanthan and guar gums, soy lecithin, PEG-40 hydrogenated castor oil, PEG-100 stearate, glycerin monostearate, polysorbate-80 (emulsifiers) and purified water. Information-search, information-analytical, organoleptic, physicochemical, rheological and pharmacotechnological research methods were used. The rheological parameters were determined on a “Reotest-2” rotary viscometer (Germany) with coaxial cylinders, pH was measured potentiometrically on a pH‒150 MI pH-meter (Khimtest Ukraine+), thermal stability was determined in a SP50 drying cabinet. The microscopic studies of experimental emulsion samples were carried out using a Granum microscope with a Toupcam UCMOS video camera. The statistical processing of the data obtained was performed using Microsoft Excel 2007 spreadsheets. Results and discussion. The composition and technology of obtaining a microemulsion with the essential oil of fennel fruit in the conditions of a pharmacy for pediatric use were experimentally substantiated. The technological process consisted of the following stages: preparatory work, weighing of ingredients, mixing of ingredients, packaging, and registration of the drug for dispensing. The drug was manufactured in aseptic conditions. Standardization of the drug obtained was carried out: description, thermal and colloidal stability, pH value, viscosity, uniformity of the mass of doses extracted from multi-dose containers, mass of the contents of the container. The presence of anethole and terpenoids was proven by TLC method. Conclusions. At the current level of development of the pharmaceutical industry, the improvement of providing consumers with high-quality medicines is implemented by choosing the optimal dosage form, the composition of excipients, rational technology, and the use of modern equipment.

Enhancing stability and antimicrobial activity of spearmint essential oil nanoemulsion through formulation optimization by mixture experimental design and in vitro drug release study

Spearmint essential oil (SEO) has been widely recognized for its therapeutic properties in treating gastrointestinal, respiratory, carminative, diuretic, antispasmodic, and sedative ailments. Moreover, it is commonly utilized as a flavoring agent in various food and beverage products. However, the effectiveness of SEO for medicinal purposes is hindered by its limited water solubility. Hence, the objective of this research was to determine the optimal conditions for producing a nanoemulsion of SEO by measuring turbidity through a mixture experimental design. The study aimed to investigate the impact of different formulation variables on turbidity as the response variable. These variables included PEG-40 hydrogenated castor oil (HCO) (1%–2% w/w), Tween 80 (1%–3% w/w), Tween 20 (1%–3% w/w), propylene glycol (PG) (5%–20% w/w), and polyethylene glycol 400 (5%–20% w/w). The results of the experimental design showed that the obtained data could be adequately fitted in a second-order polynomial model for the prediction of nanoemulsion turbidity with a multiple regression coefficient of 0.9704. The particle size value at the optimum condition was 81.28 nm, which was matched with the result of transmission electron microscopy (TEM). The thermodynamic and long-term stability of the prepared nanoemulsion were investigated. Furthermore, the developed nanoemulsion exhibited better antimicrobial activity against E. coli. In vitro release testing showed that the release of the optimized nanoemulsion was significantly increased. This study demonstrated that SEO is capable of forming stable nanoemulsions for use in delivery systems of flavoring agents in the food industry.

Counterion optimization for hydrophobic ion pairing (HIP): Unraveling the key factors

In the present study, various surfactants were combined with insulin (INS), bovine serum albumin (BSA) and horseradish peroxidase (HRP) via hydrophobic ion pairing to increase lipophilicity and facilitate incorporation into self-emulsifying drug delivery systems (SEDDS). Lipophilicity of model proteins was successfully increased, achieving log Dn-butanol/water values up to 3.5 (INS), 3.2 (BSA) and 1.2 (HRP). Hereby, key factors responsible for complex formation were identified. In particular, surfactants with branched alkyl chains or chain lengths greater than C12 showed favorable properties for hydrophobic ion pairs (HIP). Furthermore, flexibility of the carbon chain resulted in higher lipophilicity and suitability of polar head groups of surfactants for HIP decreased in the rank order sulfonate > sulfosuccinate > phosphate = sulfate > carbonate > phosphonic acids = sulfobetaines. Stability studies of formed HIP complexes were performed in various gastrointestinal fluids and their solubility was determined in commonly used SEDDS excipients. Formed complexes were stable in simulated gastrointestinal fluids and could be incorporated into SEDDS formulations (C1: 10% caprylocaproyl polyoxyl-8 glycerides, 20% PEG-40 hydrogenated castor oil, 20% medium-chain triglycerides, 50% n-butanol; C2: 10% caprylocaproyl polyoxyl-8 glycerides, 20% PEG-40 hydrogenated castor oil, 20% medium-chain triglycerides, 40% n-butanol, 10% 1,2-butanediol), resulting in suitable payloads of up to 11.9 mg/ml for INS, 1.0 mg/ml for BSA and 1.6 mg/ml for HRP.

EVALUATION OF pH AND VISCOSITY OF JUICE OF Zingiber officinale var. officinale MOUTHWASH FORMULATION

Zingiber officinale var. officinale juice has many benefits. It can be used as a mixture of mouthwash. To analyse the difference of Zingiber officinale var. officinale mouthwashes 3,125%, 6,25%, and 12,5% on pH and viscosity values on day 0,14,28,42, and 56. Zingiber officinale var. officinale 3,125%, 6,25%, and 12,5% is mixed with propylene glycol, PEG-40 hydrogenated castor oil, oleum menthae, benzoic acid, sodium benzoate, calcium lactate, sorbitol 70% and calcium thiocyanate. The formulation has measured with pHmeter (Jenway, United Kingdom) and viscometer (Brookfield, Massachusetts) for 56 days. The pH data is analyzed using GLM Repeated Measures ANOVA and One-Way ANOVA (p<0,05). Viscosity data is analyzed using GLM Repeated Measured ANOVA and Kruskal Wallis (p<0,05). The pH value of 3,125% formulation shows significant difference for 56 days in range 5,50-5,61. The viscosity value shows no significant difference for 56 days in range 3,03-3,09 cP. The pH and viscosity values of 6,25% formulation shows no significantly different for 56 days with 5,78-5,83 pH value, while the viscosity is 3,12-3,13 cP. The pH and viscosity values of the 12,5% formulation shows no significantly different for 56 days with 4,90-4,97 pH value, while the viscosity is 3,43-3,50 cP. Zingiber officinale var. Officinale mouthwash formulations 3,125% has been unstable, but it has the lowest viscosity value and has been stabled for 56 days. The pH and viscosity values of 6,25% and 12,5% formulations have been stabled for 56 days. The highest pH value is in the formulation of 6,25%.

The theoretical and experimental substantiation of the composition of a mouthwash

Aim. To develop the composition and laboratory technology of a therapeutic and preventive mouthwash based on a plant active ingredient and study a number of its quality indicators. Materials and methods. When developing the composition and technology of the drug, active pharmaceutical ingredients (APIs) and excipients approved for medical use and widely used in pharmaceutical practice were selected. The information-search, information-analytical, organoleptic, physicochemical, pharmacotechnological and microbiological research methods were used. Statistical processing of the data obtained was performed using Microsoft Excel 2007 spreadsheets. Results and discussion. The composition and number of components of the therapeutic and preventive mouthwash have been theoretically substantiated. The theoretical and experimental substantiation of the composition of the original mouthwash of the multifaceted action with a deodorizing effect for use in halitosis (the liquid extract of burdock, pot marigold, fleaworts, horsetail, sage, inula, chicory (45 : 5 : 15 : 5 : 10 : 15 : 5, respectively) (1 : 4); thyme and lemon essential oil, xylitol, polysorbate-20, glycerin, PEG-40 hydrogenated castor oil, purified water) is given. The tests showed the need to add antimicrobial preservatives to the mouthwash composition. Taking into account the requirements of safety and cost-effectiveness, as well as slightly higher antimicrobial activity, potassium sorbate in the minimum effective concentration of 0.1 % was chosen as a promising preservative. Salivary diagnostics revealed a general tendency to improve the physicochemical properties of saliva by a number of parameters after applying an experimental sample of the mouthwash developed. There is a general tendency to improve the physicochemical properties of saliva by a number of parameters after using an experimental sample of the mouthwash developed. Conclusions. The composition of the therapeutic and preventive original drug – a mouthwash of the multifaceted action with the antimicrobial and deodorizing effects for use in halitosis has been developed.

The study on the development of self-emulsifying compositions with simvastatin

Self-emulsifying compositions are the basis of oral drug delivery systems used to improve the solubility and increase the bioavailability of active pharmaceutical ingredients that are poorly soluble in the aqueous medium of gastric juice. Aim. To develop self-emulsifying compositions using simvastatin as an active pharmaceutical ingredient. Materials and methods. During the development of the composition of the self-emulsifying mixture, excipients, such as solvents, co-solvents, surfactants and co-surfactants, allowed in pharmaceutical production were used. The studies of solubility, the formation rate of emulsions of the self-emulsifying composition and stability were carried out by generally accepted methods according to the methods of the SPhU and other valid normative documents. Results and discussion. The studies of the solubility of simvastatin allowed choosing a mixture of castor oil and PEG-40 GRO as a solvent, which improved the solubility of the substance in oil. It was determined that it was efficient to use Tween-80 as the main surfactant. Glycerol monostearate, distilled monoglycerides, polyethylene oxide-400, polyethylene oxide-1500 and polyethylene glycol-100 stearate were introduced into the composition as co-surfactants. It was found that the compositions, which included polyethylene oxide-400 and polyethylene oxide-1500, had significantly worse indicators of the formation rate of emulsions than the rest of the samples. The sample containing distilled monoglycerides did not withstand a decrease in the pH value of the medium. Conclusions. According to the results obtained, samples containing castor oil, PEG-40 hydrogenated castor oil, Tween-80, glycerol monostearate or PEG-100 stearate were selected for further research.

Development of Curcumin-Loaded Polymeric Mixed Micelle for Skin Moisturizing Antioxidant Formulation

Abstract The aim of this study was to fabricate curcumin-loaded polymeric mixed micelle which was a new nanocarrier of therpeutic agent for skin uses. Curcumin was extracted from dried turmeric rhizomes using ethanol and recrystallized. The purity of curcumin was 79±3.6 %w/w. Six curcumin-loaded polymeric micelles (PM1-PM6) were prepared by simple dissolution method using poloxamer 407 (5% and 10%) as a main core structure. PEG-40 hydrogenated castor oil (PEG-40HCO) was incorporated at two percentages (2.5% and 5.0%) to study the effect on the nanoparticle characteristics. The average particle sizes of PM1-PM6 were in the range of 33.3±6.6 nm to 171.3±52.8 nm. The entrapment efficiency and the loading capacity of curcumin were in the range of 47.45%-77.35% and 0.048%w/w-0.078%w/w, respectively. When PEG-40HCO was incorporated in to the polymeric micelles, the particle size decreased and the entrapment efficiency increased. Thus, PM4 and PM5 were selected for further study. Moisturizing antioxidant creams containing 0.005%w/w of curcumin loaded in PM4, PM5 and curcumin simply dissolved in propylene glycol (PG) were formulated. The resulted formulations showed good spreadability and good characteristics. After being subjected to accelerated test, all of the formulations remained with characteristic color, pH and showed no phase separation. The stability data showed that the moisturizing antioxidant creams were stable for the whole 3 months after storage at accelerated temperature (45°C/75%RH). The study demonstrated that polymeric mixed micelle spontaneously encapsulated a poorly water-soluble curcumin and increased the solubility up to 250 folds. The developed moisturizing cream containing 0.005%w/w of curcumin resulted a greenish-yellow color preparation. It had tolerable physicochemical properties based on curcumin content, pH and viscosity under the harsh condition. The cream also had satisfactory antioxidant activity, which can be regarded as an effective and acceptable therapeutic or skincare products for topical uses.

Effect of double bond in unsaturated long-chain monoglyceride in self-emulsified nanoemulsion on tight junction opening

Unsaturated long chain monoglycerides (LCMs) used to formulate self-emulsified nanoemulsion (SEN) are varied in their degree of unsaturation which may influence their activities on membrane permeability. Therefore, this study highlights the impact of double bond in LCMs on the tight junctions of Madin-Darby Canine Kidney (MDCK) cell monolayer. Two LCMs, Glyceryl monooleate (one double bond) and Glyceryl monolinoleate (two double bonds) were formulated into SENs (SEN2 and SEN3, respectively) with Glyceryl tricaprylate and PEG-40 hydrogenated castor oil (1:1:2), and compared to the SEN (SEN1) consisted of only Glyceryl tricaprylate and PEG-40 hydrogenated castor oil (1:4). Lucifer Yellow (LY, MW 457) or Fluorescein isothiocyanate–Dextran4K (FD4, MW 3000-5000) was added to the aqueous phase of the SENs and tested for their transport across the cell monolayer. The cumulative transport of LY and FD4 achieved by SEN2 and SEN3 were significantly (p < 0.05) higher than those in phosphate buffer, 0.5% PEG-40 hydrogenated castor oil, and SEN1, indicating that the tight junctions were opened by the SENs containing LCMs. The cumulative transport of FD4 achieved by SEN3 was also 2-3 folds higher than SEN2 (p < 0.05). Therefore, LCM with two double bonds have greater potency of opening tight junction than LCM with a single double bond in SEN formulation.

Development of the gel-mask composition with nettle juice intended for telogen effluvium cutaneous application

Taking into account the frequency of telogen effluvium in women, pharmaceutical market demand, a wide range of pharmacological effects of plant biologically active substances, it is important to develop a new medicinal cosmetic remedy in the form of a gel-mask with nettle juice.&#x0D; The aim of the work – the gel-mask composition development by the results of rheological, biological, microbiological and microscopic studies.&#x0D; The objects of the experiment were gel-mask model specimens with different ratios of nettle juice and auxiliary substances, gel base samples in combination with essential oils and different content of solubilizer PEG-40 hydrogenated castor oil (PEG-40 hсo). The structural viscosity was determined on a brookfield-type viscometer at a temperature of 20 ºc and a spindle speed of 20 rpm. The nettle juice optimal concentration was substantiated on a paramecium caudatum biological model with studying of gel-mask antioxidant properties. effectiveness confirmation of 0.1% potassium sorbate preservative was carried out using the method of the Ukraine state pharmacopoeia 2.0 (USP 2.0), paragraph 5.1.3. The influence of the peg-40 hсo concentration on the essential oil dispersion degree was studied with microscopic method.&#x0D; Considering influence of the auxiliary substances and nettle juice concentration on the gel-mask structural viscosity, the ingredients’ correlations were selected which reached the required viscosity limit for gels (2 000–10 000 mpa∙s), namely: carbopol ultrez 10 and sodium alginate by 0.5 %, potassium sorbate – 0.1 %, nettle juice – 10–20 the optimal concentration of nettle juice was 15%. It was justified by the results of the study of the antioxidant properties of the experimental samples on paramecium caudatum infusoria. The conducted microbiological studies confirmed the effectiveness of the application of 0.1% potassium sorbate preservative, which meets the requirements of criterion a for the USP 2.0. The influence of solubilizer peg-40 hco on the degree of mixture of essential oils dispersion when distributed on a gel basis was studied. it was confirmed that the optimal concentration of PEG-40 hco is 0.4%, namely the ratio 1:1 according to the content of the perfume.&#x0D; According to the complex experimental researches, the optimal composition of the gel-mask with nettle juice intended for telogen effluvium cutaneous application has been worked out.

Vegetable oil-based nanoemulsions containing curcuminoids: Formation optimization by phase inversion temperature method

This study aimed to investigate the formation of curcuminoid-loaded nanoemulsions (NE) with a nonionic surfactant, PEG-40 hydrogenated castor oil (RH40) prepared by phase inversion temperature (PIT). Various vegetable oils were screened and the results showed that coconut oil provided the highest curcuminoid solubility, suitable PIT and the largest NE region in the ternary phase diagram for the formation of NE (droplets size 20–100 nm and polydispersity below 0.2). Curcuminoid-loaded NE comprising 8.3 wt% coconut oil with different curcuminoid and RH40 concentrations were prepared. The results revealed that at the RH40 concentration of ≤10 wt%, an increase in curcuminoid concentration resulted in the migration of curcuminoids towards the oil phase, affirmed by the observation of increases in droplet size. Contrarily, no significant changes (p > .05) in droplet size with increased curcuminoid concentration were observed with the NE of RH40 > 10 wt%, related to the migration of curcuminoid molecules from oil droplets into microemulsion droplets in the aqueous phase. All formulations were physically stable for at least two months. However, the degradation of curcuminoids increased with increased temperature and surfactant concentration. Based on our results, the suitable RH40 concentration and storage condition for curcuminoid-loaded NE were 10 wt% and 4 °C, respectively.

Utilization of a nonionic surfactant for improved corrosion resistance of carbon steel in simulated fuel-grade ethanol.

In this study, a nonionic surfactant (PEG-40 hydrogenated castor oil, Abbrev. PEG-40 HCO) was used to improve the corrosion resistance of carbon steel in simulated fuel-grade ethanol (SFGE). The studies were conducted using cyclic voltammetry (CV) and potentiodynamic polarization techniques and complemented by scanning electron microscopy (SEM) investigations. The presence of water and chloride ions in SFGE strongly influences the electrochemical behavior of carbon steel. Polarization curves indicate that PEG-40 HCO has good inhibition efficiency and behaves as a mixed inhibitor. The inhibition efficiency increases with the concentration of PEG-40 HCO within the range of 20 to 100 ppm, reaching a maximum value of 93.8%. The adsorption of PEG-40 HCO obeys the Langmuir adsorption isotherm. Quantum chemical calculations were evaluated to confirm experimental results.

Influence of solubilizer PEG-40 hydrogenated castor oil on carbopol gels’ structural-mechanical properties

Rheological properties affect all stages of the drug development – from development to production, the characteristics of the final products and stability.A lot of substances have complex rheological properties; their viscosity and elasticity can vary depending on conditions acting from the outside, such as stress, deformation, time factor and temperature. Concentration, stability and composition also significantly affect the rheological properties of drugs.One of the current trends in modern pharmacy is the development of drugs in the form of gels. The rheological properties of gels are significantly influenced by surface-active substances, stabilizers, solubilizers, stabilizing their structure.A special group of stabilizers are hydrogenated vegetable oils and their compounds with polymers, which have the ability to structure formation in interphase layers and in the volume of phases. For this purpose, PEG-40 hydrogenated castor oil is widely used.The aim of this work is to study the effect of hydrogenated castor oil, used as an emulsifier, solubilizer, viscosity modifier and solvent in the technology of semisolid dosage forms, on the structural and mechanical properties of carbopol gels.Materials and methods. 1% gel carbopol with additives PEG-40 hydrogenated castor oil in the concentration range from 1 to 5 % was investigated as experimental samples of the gel base. A 10 % propylene glycol additive was used as humectant and plasticizer.Structural and mechanical studies were carried out using a rotational viscometer «RheolabQC», Anton Paar (Austria) with coaxial cylinders CCC27/SS. The graphs of the gels were automatically plotted using the computer program.Results. Analysis of the rheological parameters of the carbopol with PEG-40 hydrogenated castor oil gel base shows that the solubilizer has an active influence on the structural and mechanical properties of the base.Addition of PEG-40 GMM to the carbopol gel increases the yield strength by 53 % (to 188.22 Pa at 5 % PEG-40 GKM injection), reduces the value of the yield strength of the base to 337.0–374.0 Pa s and, accordingly, increases the structure breakdown from 1.56 Up to 2.39 Pa s with an increase in the shear rate to 350 s-1, increases the hysteresis loop to 22525.9 Pa/s while reducing the stability of the system by more than 2 times and increases the value of mechanical stability to 1.16–1.37, that at the end can affect the deterioration of the restoration of the structure after deformation.Conclusions. Was studied the effect of the solubilizer PEG-40 hydrogenated castor oil on the structural and mechanical properties of carbopol gels using the «RheolabQC», Anton Paar rotary viscometer. It has been found that the use of this solubilizer in excess of 5 % is impractical due to the deterioration of the rheological properties of the gel, a decrease in mechanical stability and a decrease in the consumer qualities of the drug.

The In Vitro-In Vivo Safety Confirmation of PEG-40 Hydrogenated Castor Oil as a Surfactant for Oral Nanoemulsion Formulation.

Evaluation on the safety use of high concentration of polyoxyl 40 (PEG-40) hydrogenated castor oil as a surfactant for oral nanoemulsion was performed in Webster mice. As previously reported, nearly 20% of PEG-40 hydrogenated castor oil was used to emulsify the glyceryl monooleate (GMO) as an oil to the aqueous phase. Thermodynamically stable and spontaneous nanoemulsion was formed by the presence of co-surfactant polyethylene glycol 400 (PEG-400). Standard parameters were analyzed for nanoemulsion including particle size and particle size distribution, the surface charge of nanoemulsion, and morphology. To ensure the safety of this nanoemulsion, several cell lines were used for cytotoxicity study. In addition, 5000 mg/kg body weight (BW) of the blank nanoemulsion was given orally to Webster mice once a day for 14 days. Several parameters such as gross anatomy, body weight, and main organs histopathology were observed. In particular, by considering the in vivo data, it is suggested that nanoemulsion composed with a high amount of PEG-40 hydrogenated castor oil is acceptable for oral delivery of active compounds.

Development of the composition and technology of a caries preventive gel

Prevention of dental caries involves remineralization of the tooth surfaces with calcium and phosphorus medicines, but the use of fluorine- containing remedies in the form of a cream, gel and varnish is more effective. The aim of our work was to substantiate the composition and technology of a gel with cetylpyridinium hexafluorosilicate having the caries preventive action. A gelling agent – hydroxyethyl cellulose that provides stability and the essential structural and mechanical properties of the gel has been selected experimentally. Microscopic studies have substantiated introduction of the solubilizer PEG-40 hydrogenated castor oil in the concentration of 0.5% that promotes dissolution of the peppermint essential oil with preserving the gel transparency. The use of 10% sorbitol has been substantiated to provide the moderate osmotic properties and to prevent the gel drying. Microbiological studies have shown the necessity of using sodium benzoate as a preservative in the concentration of 0.3%. The temperature regimen of cetylpyridinium hexafluorosilicate introduction in the composition of the gel base has been substantiated by thermogravimetric studies. The technology of gel has been developed.

Safety Evaluation of Polyethylene Glycol (PEG) Compounds for Cosmetic Use.

Polyethylene glycols (PEGs) are products of condensed ethylene oxide and water that can have various derivatives and functions. Since many PEG types are hydrophilic, they are favorably used as penetration enhancers, especially in topical dermatological preparations. PEGs, together with their typically nonionic derivatives, are broadly utilized in cosmetic products as surfactants, emulsifiers, cleansing agents, humectants, and skin conditioners. The compounds studied in this review include PEG/PPG-17/6 copolymer, PEG-20 glyceryl triisostearate, PEG-40 hydrogenated castor oil, and PEG-60 hydrogenated castor oil. Overall, much of the data available in this review are on PEGylated oils (PEG-40 and PEG-60 hydrogenated castor oils), which were recommended as safe for use in cosmetics up to 100% concentration. Currently, PEG-20 glyceryl triisostearate and PEGylated oils are considered safe for cosmetic use according to the results of relevant studies. Additionally, PEG/PPG-17/6 copolymer should be further studied to ensure its safety as a cosmetic ingredient.

Water-Dilutable Biocompatible Microemulsion Systems: Design and Characterisation

Abstract The present study describes a screening approach in design of microemulsion preconcentrates (self-microemulsifying systems) comprising: PEG-8 caprylic/capric glycerides (Labrasol®) (surfactant), PEG-40 hydrogenated castor oil (Cremophor® RH40) (cosurfactant) (at surfactant-to-cosurfactant mass ratios 9:1, 7:3, 5:5, 3:7 and 1:9), and 10% w/w or 20% w/w of medium-chain triglycerides or olive oil (oil). The self-microemulsifying ability of the prepared surfactant/cosurfactant/oil mixtures in water and 0.1 M HCl (pH 1.2), was evaluated by droplet size and zeta potential analysis and cross-polarized light microscopy. The formation of microemulsions was observed only in the presence of medium-chain triglycerides at surfactant-to-cosurfactant ratios 7:3 and 5:5 (in the mixtures containing 10% w/w of the oil phase) and 3:7 and 1:9 (when 20% w/w of the same oil was used). The obtained results provide new implications for development of microemulsion preconcentrates suitable as delivery systems for food and pharmaceutical applications.

Characterization and evaluation of solid self-microemulsifying drug delivery systems with porous carriers as systems for improved carbamazepine release

The purpose of this study was to investigate solid self-microemulsifying drug delivery system (SSMEDDS), as potential delivery system for poorly water soluble drug carbamazepine (CBZ). Self-microemulsifying drug delivery system (SMEDDS) was formulated using the surfactant polyoxyethylene 20 sorbitan monooleate [Polysorbate 80] (S), the cosurfactant PEG-40 hydrogenated castor oil [Cremophor(®) RH40] (C) and the oil caprylic/capric triglycerides [Mygliol(®) 812] (O). Four different adsorbents with high specific surface area were used: Neusilin(®) UFL2, Neusilin(®) FL2 (magnesium aluminometasilicate), Sylysia(®) 320 and Sylysia(®) 350 (porous silica). Microemulsion area at the surfactant to cosurfactant ratio (K(m)) 1:1 was evaluated and for further investigation SMEDDS with SC/O ratio 8:2 was selected. Solubilization capacity of selected SMEDDS for CBZ was 33.771±0.041 mg/ml. Rheological measurements of unloaded and CBZ-loaded SMEDDS at water content varied from 10 to 60% (w/w) were conducted. It has been found that CBZ has great influence on rheological behaviour of investigated system upon water dilution. Photon correlation spectroscopy has shown the ability of CBZ-loaded SMEDDS to produce microemulsion droplet size. SSMEDDS improved release rate of CBZ, but the type of adsorbent significantly affects release rate of CBZ. For SSMEDDS with different magnesium aluminometasilicate adsorbents, release rate of CBZ decreased with increasing specific surface area due to entrapment of liquid SMEDDS inside the pores and its gradual exposure to dissolution medium. With porous silica adsorbents no difference in release rate was found in comparison to physical mixtures. In physical mixtures at 12.5% (w/w) CBZ content, presence of amorphous CBZ led to high dissolution rate.

Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions

The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol®). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma® 2421 and Solubilisant gamma® 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol®/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (Km) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1–M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief®, Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70–6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and Km value. Solubilisant gamma® 2429 as well as higher Km (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly solubilized within the interface film. The amount of drug released from the formulations M3 (10.75%, w/w) and M6 (13.45%, w/w) (Km 60:40) was limited in comparison with the reference (22.22%, w/w) and follows the Higuchi model. Microemulsions M2 and M5 (Km 50:50) gave zero order drug release pattern and ∼15% (w/w) ibuprofen released. The release profiles from microemulsions M1 and M4 (Km 40:60) did not fit well with the models used for analysis, although the amounts of ibuprofen released (24.47%, w/w) and 17.99% (w/w), respectively) were comparable to that of the reference hydrogel. The drug release mechanism was related with the surfactant/cosurfactant synergism, thus the lower efficiency of the tensides corresponded to the faster drug release.