Glyceryl Monostearate Research Articles

Development of Antioxidant-Fortified Oleogel and Its Application as a Solid Fat Replacer to Muffin.

Oleogelation has recently received a great deal of attention in the food industry as a novel alternative technology that physically converts liquid oil into semi-solid gel. Since the functional characteristics of oleogels are dependent on the gelators or bioactive compounds incorporated, this study was undertaken to evaluate the rheological properties and oxidative stability of candelilla wax oleogels fortified with glycerol monostearate (GMS) and β-carotene, and also to investigate their applications to muffin as a shortening replacer. The interaction between candelilla wax and GMS contributed to strengthening the oleogel structure. The oleogels with β-carotene showed the lowest peroxide values than the other samples. The muffins prepared with oleogels for shortening had greater specific gravity and harder texture, but there was no significant difference in the specific volume between the shortening and oleogel samples with GMS. In addition, muffins with β-carotene oleogels showed the highest oxidative stability. Therefore, this study indicated that the incorporation of β-carotene and GMS in oleogels positively affected the storage stability of muffin.

Kinetic and docking study of synthesis of glyceryl monostearate by immobilized lipase in non-aqueous media

Glyceryl monostearate is extensively used as an emulsifier in many industries. Mono acylation of glycerol was carried out by utilizing immobilized Candida antarctica lipase B (Cal B) as a biocatalyst and vinyl stearate as an acyl donor. Different reaction parameters, such as selection of lipases from various sources (like Candida antarctica, Candida rugosa, and Mucor meihei) and their quantity, shaking speed, temperature, substrate concentration, and reusability were studied in detail to achieve excellent conversion. Overall, 98% conversion of glycerol was obtained at a mole ratio of 1:1 of glycerol to vinyl stearate, using 12 mg of immobilized Cal B at 45 °C for 3 h. The mechanism of the given reaction was anticipated based on the results of the Lineweaver-Burk plots. It was found that the reaction followed the Ping-Pong Bi Bi mechanism with inhibition of glycerol. As it was a kinetically controlled synthesis, different kinetic constants were estimated by non-linear regression analysis. The activation energy for Cal B was found to be 10.3 kcal/mol. Further, biocatalyst can be reused up to four catalytic cycles with an average four percent loss of activity. A molecular docking study was done to find out the confirmation of substrates and their binding positions in an enzyme. It was noticed that the reaction proceeds through acyl-enzyme complex formation followed by the transfer of that acyl group to another substrate.

Effect of surfactant and fat on chapati making quality and control of its staling

Chapati is an unleavened flat baked product and it is prepared using whole wheat flour. One of the problems with chapatis is that they stale rapidly during storage and therefore, they have to be consumed immediately after their preparation. With changing socio-economic conditions and lifestyles, there is an increasing demand for ready to eat chapatis. In the present study, to control staling, chapatis were prepared using whole wheat flours of four different varieties by incorporating additives such as surfactant and fat. The chapatis stored at room temperature for 24 h, 48 h, 72 h and 96 h were evaluated for their quality parameters such as moisture content, chemical properties, sensory attributes, microstructure and amylograph characteristics. The moisture, soluble starch and soluble amylose contents in control chapatis decreased steadily with storage time and at the end of 96 h, the decrease in moisture, soluble starch and soluble amylose contents in chapatis prepared from different varieties were 3–8%, 80–82% and 78–85%, respectively. However, these changes were found to be at a very lesser rate in chapatis prepared from doughs treated with glycerol monostearate (GMS) and fat compared to that of control. Decrease in amylograph paste viscosity was more in control chapatis during storage compared to that of treated chapatis. Scanning electron microscopic studies of chapatis stored up to 96 h revealed that starch granules were uniform in both GMS and fat treated chapatis, when compared to control chapatis. Sensory studies showed that overall quality scores for chapatis prepared from GMS and fat treated doughs did not show any significant differences on storage. Thus, the results suggested that incorporation of surfactant and fat in dough not only improved the overall quality attributes of chapatis but also controlled their staling, during their storage.

Formulation and Evaluation of Polyherbal Antiaging Cream

Moringa oleifera family Moringaceae and Ocimum sanctum family Labiatae has been reported to possess antioxidant, antimicrobial, antiinflammatory, antibacterial and antifungal properties. Moringa oleifera and Ocimum sanctum extracts have been used to treat antimicrobial infections. The aim of this present study is to formulate and evaluate of polyherbal anti-aging cream by combining the extract of Moringa oleifera with Ocimum sanctum to achieve multipurpose skin effects such as anti-aging, fairness, softening and antiseptic effects.The polyherbal anti-aging cream formulations comprising of hydroalcoholic extract of Moringa oleifera and Ocimum sanctum, carbapol 940, xanthan gum, stearic acid, glycerol monostearate and cetyl alcohol were prepared and evaluated for physicochemical parameters and the results showed the production of stable polyherbal anti-aging cream. The formulated polyherbal anti-aging cream (O/W) was subjected to characterize like visual inspection, pH, viscosity, good spreadability, good consistency, homogeneity, no evidence of phase separation and ease to washable from skin. Formulation (F4) exhibited fulfilled the objectives of the current research and % drug release is 98.78 and exhibit good anti-microbial activity.

Design expert assisted formulation, characterization and optimization of microemulsion based solid lipid nanoparticles of repaglinide.

Repaglinide, a member of the meglitinide class of drugs, is a new anti-diabetic agent that is utilized as an oral hypoglycemic agent. Using glyceryl monostearate, cetyl palmitate, and tristearin as lipids and poloxamer 188 as a surfactant, repaglinide-loaded solid lipid nanoparticles were created. Solid lipid nanoparticles were prepared utilizing an o/w microemulsion technique, which included the lipids glyceryl monostearate and tristearin, as well as waxes such as cetyl palmitate and the surfactant poloxamer 188. The mean particle size of the solid lipid nanoparticles formed was around 339nm, with an entrapment efficiency of 82.20%. In-vitro release studies continued to be conducted using the dialysis bag diffusion technique. Within 12h, the cumulative drug release was 88.4%. The results indicate that repaglinide was released more slowly from solid lipid nanoparticles made from tristearin and glyceryl monostearate in an equal ratio. Tristearin found the controlled release and extreme entrapment from other lipid carriers like glyceryl monostearate and cetyl palmitate. Differential scanning calorimetry demonstrates that repaglinide is entangled in amorphous or molecular state within solid lipid nanoparticles. SEM microscopy revealed that the produced repaglinide solid lipid nanoparticles had a spherical shape. After one month of storage at 2-8°C, short-term stability testing revealed no significant alteration.

Solid nanostructured lipid carriers loaded with silymarin for oral delivery: Formulation development and evaluation

The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of silymarin loaded nanostructured lipid carriers (NLCs). The prepared silymarin loaded NLCs and DANs were characterized for various quality parameters. Silymarin loaded NLCs were prepared by a modified hot melt emulsification ultra-sonication method using glyceryl monostearate (GMS), capmul MCM C8 EP (CAP) and gelucire 50/13 (G50/13) as solid lipid, liquid lipid and surfactant respectively. For better stability, NLC dispersion was converted into DANs by adsorbing them onto some suitable carriers. NLCs and DANs were characterized for particle size, polydispersity index, zeta potential, entrapment efficiency, drug loading, assay, thermal behavior, crystallinity and morphological study. The optimized NLCs have a mean particle size of 206.1±012.5 nm (size distribution of 0.249±0.058), a zeta potential of -32.5±1.2 mV with high entrapment of 95.60±0.45% and drug loading of 1.90±0.08%. The X-ray diffraction and endothermic peaks confirmed the maximum encapsulation of active in lipid matrices. The particles were spherical with smooth surface morphology. In-vitro release studies showed sustained drug release for up to 24 h. Ex-vivo permeation in the presence and absence of lymphatic blocker indicates the uptake of silymarin loaded NLCs by the lymphatic route. Silymarin loaded NLCs prepared had a nanosize distribution with high entrapment efficiency. The ex-vivo permeation study for optimized NLC formulation exhibited the lymphatic uptake of active. Dispersion stability was increased by preparing the DANs. The solid dry powder is used for oral reconstitution and can be further converted into tablets or filled into capsules.

Formulation and Characterization of Bitter Melon (Momordica charantia Linn.) Fruit Fraction Loaded Solid Lipid Nanoparticles

Background: The main active compound of bitter melon (Momordica charantia Linn.) fruit is charantin, which is believed to have important role on antihyperglycemic effect. However, charantin compound has a large molecular weight and is easily hydrolysed when given orally. Therefore, a colloidal drug delivery system, such as solid lipid nanoparticles (SLN), is required to provide a suitable and effective delivery of charantin, which is contained in a bitter melon fraction (BMF). Objective: This study aimed to prepare and evaluate SLN containing BMF with an appropriate characteristic for transdermal delivery. Methods: Bitter melon fruits were extracted with ionic liquid of [BMIM]BF4 using ultrasound-assisted extraction (UAE) and fractionated with dichloromethane. Four formulas of BMF loaded SLN were prepared with various ratio of BMF to surfactant and various ratio of lipids using high-shear homogenization followed by ultrasonication method. The obtained SLN were characterized, including morphology, particle size distribution, zeta potential, and entrapment efficiency. Furthermore, the stability study of BMF-loaded SLN was also conducted. Results: The result showed that BMF was a dry powder and brownish fraction with a specific smell. The BMF loaded SLN showed a spherical shape with the SLN F1 formula as a selected formula. The SLN F1 showed a particle size (Z-average) of 98.3±1.98 nm, polydispersity index of 0.26±0.01, zeta potential of -39.53±0.15 mV, and entrapment efficiency of 82.96±1.42 %. According to the stability study, it revealed that the BMF loaded SLN F1 had an acceptable stability, which the charantin content in the SLN was 96.52% after 3 months storage at 25°C ± 2°C. Conclusion: The BMF loaded SLN F1 with 1:12 ratio of BMF to surfactant and 1:2 ratio of capric caprylic triglyceride to glyceryl monostearate was selected as the best formula with the appropriate characteristics for transdermal delivery.

Intranasal delivery of chitosan decorated nanostructured lipid carriers of Buspirone for brain targeting: Formulation development, optimization and In-Vivo preclinical evaluation

The current research was portrayed to design and optimize the Chitosan (CH) coated Buspirone-loaded nanostructured lipid carriers (BPE-CH-NLCs) for nose to brain delivery. NLCs were developed by solvent diffusion evaporation technique, coated with CH, and then optimized to the maximum efficiency using the quality by design (QbD) based Box-Behnken design (BBD). Glyceryl monostearate (GMS) & oleic acid mixture and tween 80 were used as a lipid and surfactant, respectively. The prepared NLCs were subjected to in-vitro characterization. In-vivo pharmacokinetic and neuro-pharmacokinetic (drug targeting efficiency-DTE, direct transport percentage-DTP) parameters were evaluated on Wister rats. The results revealed that the optimized formulation exhibited acceptable PS (190.98 ± 4.72 nm), ZP (+17.47 mV), and EE (80.53 ± 1.26% w/w), and the TEM image showed that the drug was incorporated adequately in NLCs. DSC findings exposed that the drug was present in amorphous form within the NLCs. The optimized formulation exhibited 27.61 months shelf life and was found to be stable under studied conditions. The value of AUC (bioavailability) for BPE-CH-NLCs administered i.n was found to be 3.06 folds compared to BPE-CH-NLCs administered i.v, and 2.17 folds compared to BPE-Sol administered i.n. A higher value of DTE (1462.49%) for developed NLCs confirmed the brain targeting efficiency of these lipid nanoparticles. DTP value for BPE-CH-NLCs (93.16%) was significantly (p < 0.05) higher than BPE-Sol (81.63%), indicating the efficient targeting potential of lipid nanoparticles compared to drug solutions. Finally, it could be possible to infer that GMS-Oleic acid-based NLCs coated with CH might be effective carriers to administer BPE to the brain via the nasal route.

Oral colon delivery platform based on a novel combination approach: Design concept and preliminary evaluation

An oral colon delivery platform based on a novel combination strategy, leveraging multiple physiological characteristics of the intestine, is proposed. The system comprises a drug core, a water-swellable/soluble inner layer based on a hydrophilic cellulose derivative and an enteric outer layer (Eudragit® S) containing a microbially-degradable polysaccharide (high-amylose starch, Amylo N460), acting synergistically to prevent early release in the small intestine on the one hand, and release failure on the other. The Eudragit® S:Amylo N460 solid weight ratio in the external coating was 7:3; triethyl citrate and glyceryl monostearate were used as a plasticizer and an anti-tacking agent, respectively. The outer Eudragit® S/Amylo N460 layer was applied in a fluid bed using hydro-alcoholic or aqueous coating formulations. Two types of “inner” systems were studied: (i) Drug-loaded tablets coated with a low-viscosity hydroxypropyl methylcellulose (by aqueous spray-coating), and (ii) hydroxypropyl cellulose capsules prepared by injection-molding (filled with paracetamol as an analytical tracer). The obtained dosage forms were thoroughly characterized, including in vitro release measurements in various media. In all cases, pulsatile release profiles were obtained after medium change from 0.1 N HCl to phosphate buffer pH 7.4, with lag phases depending on the type and preparation technique of the hydrophilic polymer layer. The role of the microbiota on the release performance was explored in simulated colonic fluid (SCF), consisting in culture medium inoculated with fecal samples from inflammatory bowel disease patients. Clear differences in drug release were observed in SCF versus culture medium free of feces, indicating the effect of microbial degradation.

Development and characterization of structured water-in-oil emulsions with ethyl cellulose oleogels

The food industry confronts an enormous challenge to develop stable margarine-type water-in-vegetable oil (W/O) emulsion-based table spreads with reduced concentration of saturated fat and without trans fats. In the present work, we developed a gelled W/O emulsion (Gelled-W/O-E) containing 20% of water using a mixture of a conventional W/O emulsion (W/O-E) stabilized with glycerol monostearate (GMS), and an ethyl cellulose (EC) oleogel. The mechanical, microstructure and stability of the resulting gelled emulsion (Gelled-W/O-E) was compared with control systems consisting of conventional W/O emulsions (W/O-E) and EC-GMS oleogels (EC-GMS-O; no water added) formulated using the same GMS (0.5% and 1.0%) and EC (7%) concentration as in the Gelled-W/O-E. The Gelled-W/O-E showed higher elasticity and emulsion stability in comparison with the control systems. This in spite the EC and GMS concentrations used were below the minimal concentration required to develop a gel, and the tentatively lower solid content in the Gelled-W/O-E than in the EC-GMS-O because the presence of water. We observed that by increasing the GMS concentration in the Gelled-W/O-E, the water droplet size decreased as gel elasticity and W/O emulsion stability significantly increased. We associated this behavior to a synergistic GMS-EC interaction that kept the GMS at the water–oil droplet interface. These results showed the role of water droplets as active fillers in determining the rheological properties of the Gelled-W/O-E, and that the GMS efficiency as emulsifier increased in the presence of EC in the oil phase. After comparing the microstructural properties of commercial margarine spreads with those of the Gelled-W/O-E, we concluded that the structured W/O emulsion is a novel way to achieve similar functionality to margarine spreads, without the use of saturated and trans-fats.

Optimization of Diclofenac Sodium-Loaded Nanostructured Lipid Carriers (NLCs) Using the Box-Behnken Design

This study aimed to prepare diclofenac sodium (DCF)–loaded nanostructured lipid carriers (NLCs) (DCF-loaded NLCs) for optimizing the NLCs by using the Box-Behnken design. A hot emulsification method using an ultrasonic probe was employed to prepare DCF-loaded NLCs. The active ingredient, solid lipid, oil, and emulsifier were DCF, glyceryl monostearate (GMS) (X1), oleic acid (X2), and polysorbate 80 (X3), respectively. The DCF-loaded NLCs had particle sizes of 69.29–187.3 nm. The polydispersity index (PDI) was in the range of 0.216–0.516, indicating a relatively narrow size distribution. The zeta potential of all formulations revealed the negative charge and ranged between -26.0 and -42.13 mV. The percentage encapsulation efficiency (%EE) was 92.71%–104.21%. The responses of all model formulations were created and the optimized formulation was selected by Design-Expert® software. The optimal formulation was composed of 2 g GMS, 0.926 g oleic acid, and 2.724 g polysorbate 80. The particle size and PDI experimental values with the optimal formulation did not differ from those predicted and were within the 95% CI. Therefore, the Box-Behnken design could be efficient in formulating and optimizing DCF-loaded NLCs.

Physical properties of kelulut honey emulsions with different oil types and emulsifier concentrations

Kelulut honey (KH) is a honey produced by stingless bee species, known for its high nutritional content and health benefits. Even though it is very healthy, some people cannot consume it directly. Therefore, incorporating this type of honey into an emulsion system is a good strategy to increase its consumption. Emulsion technology is one of the alternative technologies nowadays which combines two or more immiscible liquids to form a solution. In this study, KHemulsions were emulsified with glyceryl monostearate (GMS) and stabilised by xanthan gum. There were two stages involvedto determine the effects of variations in oil types and emulsifier concentrations on the physical properties of KH emulsions. In the first stage, three types of oil were used as the dispersed phase, which were palm oil, canola oil, and sunflower oil. Then in the second stage, different concentrations of GMS (0.25, 0.5, 0.75 and 1%) were applied. From the droplet size analysis, the emulsion with sunflower oil and the highest concentration of GMS gave the smallest diameter of 0.78 ± 0.01µm and the lowest polydispersity index (pdI) of 16.2±2.03 %. Meanwhile, the texture analysis shows that emulsion with palm oil has the highest firmness (45.16±2.83 g) and consistency (305.44±14.91 g.sec) values. The foaming index on the other hand depicts that emulsion with palm oil and that with the lowest concentration of GMS gave the highest foam stability. From this study, a physically stable oil-in-water KH emulsion was produced, which should undergo further chemical, sensory and storage studies for commercial production in the future.

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery.

Lidocaine, a commonly used local anesthetic, has recently been developed into a number of ointment products to treat hemorrhoids. This study examined its efficient delivery to the dermis through the pharmaceutical improvement of hemorrhoid treatment ointments. We attempted to increase the amount of skin deposition of lidocaine by forming a nanoemulsion through the self-nanoemulsifying effect that occurs when glycerol monostearate (GMS) is saturated with water. Using Raman mapping, the depth of penetration of lidocaine was visualized and confirmed, and the local anesthetic effect was evaluated via an in vivo tail-flick test. Evaluation of the physicochemical properties confirmed that lidocaine was amorphous and evenly dispersed in the ointment. The in vitro dissolution test confirmed that the nanoemulsifying effect of GMS accelerated the release of the drug from the ointment. At a specific concentration of GMS, lidocaine penetrated deeper into the dermis; the in vitro permeation test showed similar results. When compared with reference product A in the tail-flick test, the L5 and L6 compounds containing GMS had a significantly higher anesthetic effect. Altogether, the self-nanoemulsifying effect of GMS accelerated the release of lidocaine from the ointment. The compound with 5% GMS, the lowest concentration that saturated the dermis, was deemed most appropriate.

FLOATING IN SITU RAFT FORMING LIQUID GASTRORETENTIVE DRUG DELIVERY SYSTEM CONTAINING POORLY WATER-SOLUBLE DRUG

Present work was aimed to develop a liquid in situ raft forming floating gastroretentive system of repaglinide using gellan gum, pectin, and sodium alginate. The formulations were characterized in terms of compatibility of drug-excipient by Fourier transform infrared, drug content, effect of processing parameters on physical form of drug (crystalline or amorphous) by X-ray diffraction analysis, thermal behaviour by differential scanning calorimetry, and in vitro drug release study. The results confirm no interaction between the drug-excipients and fusion of drug crystals within the polymer matrix in amorphous form. The gel raft-floated for more than 24 h. All the formulations showed instantaneous gelation within 30 seconds in 0.1N HCl (pH 1.2). Formulation containing gellan gum (500 mg), pectin (500 mg), and glycerol monostearate (500 mg) released 21% of the drug in first 4 h, 69% in 6 h and reached 97% in 7 h. Without gellan gum, 35% of the drug was released in the first 2 h and reached 90% in 4 h. Based on these results it is suggested that the incorporation of drug into the liquid in situ raft forming floating system may be an appropriate strategy to improve the dissolution profile of poorly soluble drugs.

Colon-targeted protein delivery by using solid lipid nanoparticles

Recently, therapeutic proteins have been used to combat life-threatening diseases. To date, oral routes have been developed to deliver proteins. Since the proteolytic degradation in the upper gastrointestinal tract frequently occurs, we need a formulation and strategy to protect and deliver protein to the colon. In this research, solid lipid nanoparticles (SLNs) were prepared in eight formulae for colon-targeted delivery with various glyceryl monostearate, Tween 80, soy lecithin, and polyethylene glycol 6000 concentrations. Bovine serum albumin (BSA) was used for the protein model in the system. All formulae were characterized by their morphology, particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. The distribution of particle sizes varied between 94.24 and 186.8 nm and the zeta potential value ranged from −22.8 to −34.3 mV. Formula 4 (F4) showed the best entrapment efficiency of 78.69% with a particle size of 102.1 nm, PDI of 0.349, and zeta potential of −26.1 mV. F4 was then coated with Eudragit S100 and measured for its drug release profile in vitro. F4 coated with Eudragit S100 held the drug released in the gastric and released all the BSA in the colon condition. These results indicated that BSA�SLN F4 could be a promising delivery system to obtain optimal colon-targeted parameters.

Enhancement on vacuum foam mat quality parameters of papaya powder by using chemical preservatives

Vacuum foam-mat drying is a technique that involves whipping a liquid concentration with an appropriate foaming agent into a stable foam that is then dehydrated into a thin mat of foam at a low temperature. The effect of variables on responses was determined using response surface methodology (RSM). The moisture content of raw papaya pulp was 856.023 % (db.). The total soluble solid (TSS) was tested by hand refractrometer i.e. 12.8 o Brix. Parameters such as whipping time (10 minute) , papaya pulp thickness (4 mm) and vacuum oven pressure (25 inch Hg), pH value 5.56 and TSS(10 o Brix) remain constant throughout the work. The drying time, drying rate and moisture ratio varies from 60 minutes to 840 minutes, 0.001-1.279 and 0.01-4.402 respectively. The drying duration, drying rate, and moisture ratio range from 60 to 840 minutes, respectively, 0.001-1.279 and 0.01-4.402. In experiment number 2, the ingredients, temperature (70 oC), maltodextrin 0.30 (w/w), glycerol monostearate 2.0 percent, and tricalcium phosphate 2.0 percent of dried papaya powder were combined to achieve a minimum drying time of 660 minutes. Experiments also revealed that increasing the amount of tricalcium phosphate (2%) and glycerol monostearate 2.0 percent in the materials reduced drying time, which helped to lower the moisture content of the papaya powder. As the drying time increases, the moisture ratio for all samples decreases in a nonlinear manner. The moisture ratio of each sample declined rapidly while the drying period was very short, but the rate of decrement of moisture ratio became quite slow as the drying time increased. The solubility of papaya powder is found to be as low as 69.08 percent in experiment number 24 and as high as 96.45 percent in experiment number 20. Ascorbic acid is found in the range of 88.43 to 115.75 (mg/100g) in experiment numbers 28 and 1, while beta carotene is found in the range of 10-51 (g/100g) experiment numbers 24 and 12. L* (Lightness) is varied from 53.1 to 82.79 experiment numbers 14 and 10, chromatic component a* (from green to red) is varied from 27.25 to 105.92 experiment numbers 3 and 17, and chromatic component b* (from blue to yellow) is varied from -15.92 experiment number 3 to 73.67 experiment number 10 during colour value estimation. It is reported that solubility increases with increase in maltodextrin at 5% level of significance. The interaction between maltodextrin and glycerol monostearate are significant at P

Edible composite bi-layer coating based on whey protein isolate, xanthan gum and clove oil for prolonging shelf life of tomatoes

Coatings plays an imperative role in increasing shelf life of fruit and have potential to minimize postharvest losses. In this study, impact of coating formulated from whey protein isolate, xanthan gum, clove oil and glycerol monostearate on tomato was evaluated. The tomatoes were divided in six groups and coated by dipping technique. Non-coated and differently treated tomatoes were evaluated under controlled environmental conditions (20 °C and 85% RH). The effectiveness of coatings on different quality attributes was investigated at time interval of 3, 6, 9, 12 and 15 days of storage. Storage life of coated samples exhibited improvement in firmness and color. The titrable acidity, ascorbic acid content, total phenolics content, total sugars and reducing sugars showed better retention in coated samples than non-coated sample. The results depicted that all formulated coatings have potential to maintain quality characteristics and increase the shelf life of tomatoes. The coatings made from whey protein isolate and xanthan gum in equal proportion exhibited best combination among all the coating as maximum quality attributes were retained by this coating because of inhibiting respiration and minimize starch conversion into sugar. Therefore, coatings were proven to be feasible for application due to edible, non-reactive and biodegradable nature.

Synchronizing In Silico, In Vitro, and In Vivo Studies for the Successful Nose to Brain Delivery of an Anticancer Molecule.

Sesamol is a sesame seed constituent with reported activity against many types of cancer. In this work, two types of nanocarriers, solid lipid nanoparticles (SLNs) and polymeric nanoparticles (PNs), were exploited to improve sesamol efficiency against the glioma cancer cell line. The ability of the proposed systems for efficient brain targeting intranasally was also inspected. By the aid of two docking programs, the virtual loading pattern inside these nanocarriers was matched to the real experimental results. Interactions involved in sesamol-carrier binding were also assessed, followed by a discussion of how different scoring functions account for these interactions. The study is an extension of the computer-assisted drug formulation design series, which represents a promising initiative for an upcoming industrial innovation. The results proved the power of combined in silico tools in predicting members with the highest sesamol payload suitable for delivering a sufficient dose to the brain. Among nine carriers, glyceryl monostearate (GMS) and polycaprolactone (PCL) scored the highest sesamol payload practically and computationally. The EE % was 66.09 ± 0.92 and 61.73 ± 0.47 corresponding to a ΔG (binding energy) of -8.85 ± 0.16 and -5.04 ± 0.11, respectively. Dynamic light scattering evidenced the formation of 215.1 ± 7.2 nm and 414.25 ± 1.6 nm nanoparticles, respectively. Both formulations demonstrated an efficient cytotoxic effect and brain-targeting ability compared to the sesamol solution. This was evidenced by low IC50 (38.50 ± 10.37 μM and 27.81 ± 2.76 μM) and high drug targeting efficiency (7.64 ± 1.89-fold and 13.72 ± 4.1-fold) and direct transport percentages (86.12 ± 3.89 and 92.198 ± 2.09) for GMS-SLNs and PCL-PNs, respectively. The results also showed how different formulations, having different compositions and characteristics, could affect the cytotoxic and targeting ability.

Formulation and Evaluation of Clarithromycin Loaded Nanostructured Lipid Carriers for the Treatment of Acne

Background: Clarithromycin is a macrolide antibiotic used in acne treatment, but it has poor solubility, which decreases its permeability through lipid barriers such as skin. Nanostructured lipid carriers can enhance the permeability of clarithromycin through the skin, thus improving its potential for controlling acne.&#x0D; Aim: To formulate and evaluate Nanostructured lipid carriers of clarithromycin for topical delivery in acne treatment&#x0D; Methods: Nanostructured lipid carriers were prepared by emulsification and ultrasonication methods using lipids such as glycerol monostearate and oleic with poloxamer 188 as stabilizer. These nano-carriers were optimized with the help of the Quality by Design (QbD) approach employing Design-Expert® software. The nanoparticles were characterized for particle size analysis, zeta potential, drug-excipient compatibility, entrapment efficiency, and surface morphology by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The nano-carriers were also investigated for in vitro drug release and ex vivo permeation through excised goat skin. The optimized formulation was incorporated into topical carbopol gel base, formulated and examined for pH, viscosity, spreadability, in vitro drug release, ex vivo permeation, and stability under accelerated conditions.&#x0D; Results: The average particle size of the optimized nanoparticles was 164.8 nm, and zeta potential was -39.2 mV. FTIR studies showed that drug and lipids are compatible with each other. The morphology study by SEM and TEM showed spherical shaped particles. The entrapment efficiency of the optimized formulation was found to be 88.16%. In vitro drug release studies indicated sustained release from the formulation due to diffusion through the lipid matrix of the particles. The ex vivo permeation study using goat skin produced greater permeation from the NLC gel (89.5%) than marketed gel (65%) due to the lipid solubility of the nanoparticles in the skin. The formulation was stable under accelerated conditions.&#x0D; Conclusion: The optimized formulation can be considered as promising nano-carriers suitable for the sustained release of clarithromycin into the skin for effective control of acne.

The Serum Metabolomics Study of Liver Failure and Artificial Liver Therapy Intervention.

BackgroundThis study was designed to study the serum metabolites of patients with liver failure.Material/MethodsThe study included 50 patients with liver failure, 30 patients with chronic hepatitis B treated with an artificial liver, 11 patients with an artificial liver, and 32 healthy controls. Clinical data were recorded, and blood samples were analyzed by gas chromatography–mass spectrometry (GC-MS). The random forest algorithm was used to construct a multidimensional scale map to preliminarily reflect the differences between samples. The data were then analyzed to obtain the correlation of different variables among samples, from which the differential metabolites were screened.ResultsThirty-five metabolites were identified by GC-MS. There were significant differences in serum metabolites levels before and after treatment in the liver failure group and in the chronic hepatitis group, healthy control group, and artificial liver group. Different metabolites were screened according to the importance of different variables among samples. Significant differences were found between the liver failure group, the chronic hepatitis group, and the healthy control group. In addition, there were significant differences in the liver group before and after treatment with an artificial liver, including differences in boric acid, 2-(methoxyamino)-propionic acid, glycine, l-methionine, aminopropionic acid, glyceryl monostearate, cholesterol, and other substances.ConclusionsA variety of differences in metabolites were found in each group, some of which revealed possible metabolic pathways leading to differences between groups. Blood metabolomics analysis has great potential in real-time dynamic monitoring of liver failure and evaluation of artificial liver therapy.