Glyceryl Monostearate Research Articles

Enhanced foamability and stability of aqueous foams through novel pickering fat globules formulated with solid lipid particles

Pickering fat globules (PFGs), known for their remarkable stability via the Pickering effect, eco-friendliness, and ability to carry hydrophobic flavors and nutrients, play a pivotal role in the advancement of food foam systems. This study investigates highly unsaturated and exceptionally stable aqueous foams stabilized by PFGs with interfacial activity. These PFGs are derived from two types of solid lipid particles (SLPs): fully hydrogenated soybean oil with sodium caseinate (FHSO-SC-SLPs-PFGs) and glyceryl stearate citrate (GSC-SLPs-PFGs), which were formulated with varying SLPs concentrations (0.5 wt%, 2.5 wt% and 5 wt%) while coating 10 wt% and 20 wt% oil droplets. Remarkably, 0.5 wt% SLPs could accommodate up to 20 wt% of low-melting-point liquid oil, enhancing the unsaturation of PFGs. GSC-SLPs-PFGs generated foams with overrun values reaching up to 235%, exhibiting stability for at least 40 days. In contrast, foams derived from FHSO-SC-SLPs-PFGs, with the highest overrun value of 145%, remained stable for only 2 h. Compared with FHSO-SC-SLPs-PFGs, GSC-SLPs-PFGs exhibited superior foaming performance and stability attributed to their properties such as smaller particle size, enhanced hydrophilicity, higher apparent viscosity, increased surface potential, and superior surface tension reduction. Furthermore, increasing the concentration of SLPs and/or reducing the oil phase can also improve the properties of SLPs-PFGs, resulting in greater foamability and foam stability. Surface dynamic adsorption, interfacial shear rheology, and microstructural observations revealed robust adsorption of all SLPs-PFGs at the air-liquid interface, indicative of pronounced Pickering stabilization, with GSC-SLPs-PFGs also exhibited three-dimensional network structure. These SLPs-PFGs stabilized foams presented heightened stability and reduced saturated fat content, paving the way for novel and healthier foam-based food products.

Combining solid lipid-nanoparticles in Alginate coating formulation to prepare enteric-released Diclofenac pellets

In the trend of using natural-resource substances in current pharmaceutical industry, alginate (ALG) film was used to coat tablets. To further develop ALG film-coating, solid lipid nanoparticles of cetearyl alcohol (ACS) or glycerol monostearate (GMS) were added in the coating formulation, applying to the diclofenac sodium (Na-D) pellet. Na-D pellets were prepared by the extrusion-spheronization method. Coated pellets were characterized with anti-moisture and acidic-resistant, and dissolution properties. Also, coating morphology was observed by microscopy and scanning electron microscopy (SEM); difference-scanning-calorimetry (DSC) and infrared (IR) spectroscopy were used to characterize the coating structure. The results showed that the nanoparticles were uniformly distributed into ALG structure. Interestingly, lipid nanoparticles enhaced the flexibility of the film, in which GMS nanoparticles improved the film-formed process (significantly lowering glass transition temperature). Regarding functions of the coating membrane, the moisture resistance and acid resistance of Na-D pellets increased only when nanolipids were present in the membrane.

Effect of the gelling mechanism on the physical properties of bigels based on whey protein isolate

The effect of the cold-set and heat-set gelling mechanism of whey protein isolate on bigel production was assessed. For this purpose, hydrogel phase was produced with whey protein isolated (10 % w/v) and for oleogel sunflower oil and glycerol monostearate (7.5 % w/v) were used. Bigels were produced by hot emulsification of different hydrogel:oleogel ratios (from 90:10 up to 10:90). For cold-set bigels (CSB) NaCl (200 mM) was added to the aqueous phase prior to the emulsification and the emulsion was cooled to promote the 3D network formation. On the other hand, heat-set bigels (HSB) were produced by heating the emulsion (80 °C, 60 min). Bigels were evaluated through microscopy, FTIR, thermal and texture analyzes. Results showed that depending on the hydrogel:oleogel ratio and gelling mechanism different structures organization were obtained. CSB were more organized, showing that the rate of gelation was the mechanism responsible for the structure. However, for HSB the heat treatment destabilized the emulsion and disorganized structures were observed for high oleogel content. FTIR corroborates the visual observation and showed that the arrangement was purely physical. In addition, the structural arrangement led to different mechanical properties. In general, HSB produced gels with rubber-like behavior, higher elasticity modulus and the presence of a breaking point. In contrast, CSB behaves as squeezing gel, with no breaking point and lower values of elasticity modulus. Moreover, for O/W bigels the dispersed oleogel particles disrupted the WPI network decreasing the gel strength in comparison to pure hydrogels. However, for systems where oleogel was the continuous phase, the gel strength was recovered due to the metastable and dynamic character of these systems. Thus, results showed that the gelling mechanism of the protein exerted an effect on the physical properties of bigels. In addition, the mechanical properties also can be modulated according to the bigel composition, allowing its application in products with different sensorial characteristics.

Fabrication and characterization of dihydromyricetin-loaded microcapsules stabilized by glyceryl monostearate and whey protein–xanthan gum

Dihydromyricetin (DMY) is a lipophilic nutrient with various potential health benefits; however, its poor storage stability and low solubility and bioavailability limit its applications. This study aims to encapsulate DMY in microcapsules by membrane emulsification and freeze-drying methods to overcome these issues. Glyceryl monostearate (GMS, solid lipid) and octyl and decyl glycerate (ODO, liquid lipid) were applied as the inner cores. Whey protein and xanthan gum (XG) were used as wall materials. The prepared microcapsules had an irregular blocky aggregated structure with rough surfaces. All the microcapsules had a DMY loading of 0.85 %–1.1 % and encapsulation efficiency (EE) >85 %. GMS and XG increased the DMY loading and EE. The addition of GMS and an increased XG concentration led to a decrease in the rehydration rate. The in vitro release and digestion studies revealed that GMS and XG controlled the release and digestion of DMY. The chemical stability results indicated that GMS and XG protected DMY against oxidation. An antioxidant capacity study showed that GMS and XG helped DMY in the microcapsules exert antioxidant effects. This research study provides a platform for designing microcapsules with good stability and high bioavailability to deliver lipophilic bioactive compounds.

One Platform Comparison of Polymeric and Lipidic Nanoparticles for the Delivery of Amphotericin B.

Amphotericin B (AmB) is a membrane-acting antibiotic used for the treatment of fungal and protozoal infections. AmB exists in various molecular forms, i.e., monomeric, super-aggregated, and oligomeric forms, where oligomeric forms are highly toxic because of their relative affinity toward cholesterol present over human cell membrane. Hence, the objective of our research work was to study the aggregation state of AmB in two different nanoformulations, i.e., solid lipid nanoparticles (SLNs) and zein-based nanoparticles (PNPs), with the aim of enhancing the fraction of less toxic form of AmB, and a comparative study was performed. The zein and glyceryl monostearate can intercalate the polyenic domain of AmB and thereby hinder the hydrophobic attractions between the AmB molecules, which allows their existence in monomeric forms. The particle size of AmB-SLNs and AmB-PNPs were 378.90 ± 9.50 nm and 184.90 ± 6.00 nm, while zeta potential was -34.97 ± 0.51 mV and +28.93 ± 2.29 mV, respectively. In vitro release studies showed more controlled release of AmB from PNPs (52.48 ± 1.07%) as compared to SLNs (86.33 ± 0.93%). The predominant aggregation state of AmB in both formulations was determined by UV-visible and circular dichroism spectrophotometry, where a higher degree of monomerization of AmB was reported in AmB-SLNs as compared to AmB-PNPs. Toxicity of the nanoformulations was evaluated through hemolysis test, where the results suggested that AmB-SLNs and AmB-PNPs were less hemolytic as compared to pure AmB. The nanoformulations demonstrated the predominant monomeric form of AmB, which may offer higher selectivity index toward microbial membrane.

Sulconazole-Loaded Solid Lipid Nanoparticles for Enhanced Antifungal Activity: In Vitro and In Vivo Approach.

Solid lipid nanoparticles (SLNs) have the advantages of a cell-specific delivery and sustained release of hydrophobic drugs that can be exploited against infectious diseases. The topical delivery of hydrophobic drugs needs pharmaceutical strategies to enhance drug permeation, which is a challenge faced by conventional formulations containing a drug suspended in gel, creams or ointments. We report the fabrication and optimization of SLNs with sulconazole (SCZ) as a model hydrophobic drug and then a formulation of an SLN-based topical gel against fungal infections. The SLNs were optimized through excipients of glyceryl monostearate and Phospholipon® 90 H as lipids and tween 20 as a surfactant for its size, drug entrapment and sustained release and resistance against aggregation. The SCZ-SLNs were physically characterized for their particle size (89.81 ± 2.64), polydispersity index (0.311 ± 0.07), zeta potential (-26.98 ± 1.19) and encapsulation efficiency (86.52 ± 0.53). The SCZ-SLNs showed sustained release of 85.29% drug at the 12 h timepoint. The TEM results demonstrated spherical morphology, while DSC, XRD and FTIR showed the compatibility of the drug inside SLNs. SCZ-SLNs were incorporated into a gel using carbopol and were further optimized for their rheological behavior, pH, homogeneity and spreadability on the skin. The antifungal activity against Candida albicans and Trichophyton rubrum was increased in comparison to a SCZ carbopol-based gel. In vivo antifungal activity in rabbits presented faster healing of skin fungal infections. The histopathological examination of the treated skin from rabbits presented restoration of the dermal architecture. In summary, the approach of formulating SLNs into a topical gel presented an advantageous drug delivery system against mycosis.

FORMULATION AND EVALUATION OF NANOPARTICLE DRUG DELIVERY SYSTEM FOR TREATMENT OF HYPERTENSION

Objective: The aim of the current research is to formulate and evaluate Trandolapril loaded solid lipid nanoparticles (SLNs) for the management of high blood pressure. Methods: SLNs were formulated using Glyceryl monostearate and poloxamer 188 by hot homogenisation and ultrasonication method. Different concentrations of lipid and surfactant were used for the preparation adopting 32 full factorial design. The prepared formulations were initially evaluated for particle size, PDI, zeta potential and entrapment efficiency to obtain the optimised formulation. Results: The optimised formulation TF 6 reported the particle size of 212.6±5.39 nm and entrapment efficiency of 91.02±0.57%; this was further characterised for FT-IR, DSC and scanning electron microscopy. The in vitro release of drug for the prepared formulations was performed for 24 h and the optimised formulation showed better-controlled drug release compared to other formulations. Conclusion: The pure Trandolapril solution was collated with the optimised formulation TF 6 and the result concluded that the formulation showed controlled drug release compared to pure drug. This study proves that Trandolapril SLNs can be prepared for increasing the release of drug for prolonged period.

Development and characterization of hydrogel-in-oleogel (bigel) systems and their application as a butter replacer for bread making.

Butter has been widely used in bakery products and it contains high level of saturated fats. However, excessive consumption of saturated fats would increase the risk of chronic disease. This study was to fabricate water-in-oil (W/O) type bigels as butter replacers to improve the quality attributes of breads. A stable water-in-oil (W/O) type bigel system was fabricated based on mixed oleogelators (rice bran wax and glycerol monostearate) and sodium alginate hydrogel. The ratios of oleogel to hydrogel could significantly affect the stability, microstructure and rheological properties of bigels. All of the bigels exhibited solid-like properties, with increased oleogel fractions, and the network structure of bigel became more compact and orderly with smaller sodium alginate gel particles. Meanwhile, the viscoelastic modulus and firmness of bigel increased, contributing to a higher stability. The bigel dough exhibited lower gel strength and relatively higher extensibility compared to the butter dough. Regardless of oleogel fractions, all the bigel produced bread with a higher specific volume and softer texture than the butter bread. When the oleogel fractions was less than 80%, increasing the oleogel fractions was more beneficial for improving the specific volume, softness and fluffy structure of bread. W/O type bigel as butter replacers showed great potential in improving the appearance, structure and textural properties of bread. © 2023 Society of Chemical Industry.

Quality and shelf life evaluation of gluten‐free blends and cake premix

AbstractBakery premixes are composed of a blend of ingredients that offer convenient and quick baking solutions. In the present study, four blends were prepared by taking buckwheat, chickpea, plantain flour, and rice flour in the ratio of (40:20:10:30) T1, (40:20:20:20) T2, (40:20:30:10) T3, and (40:20:40:0) T4. Cake premixes were formulated by adding sugar, baking powder, baking soda, corn starch, and glycerol monostearate in the ratio of 60:5:2.5:1:2 in all the four blends. Blends were analyzed for physicochemical, functional, thermal, bioactive, and antioxidant properties, and premixes were evaluated for cake baking quality. The T3 premix was selected based on evaluated parameters, and the prepared cake contained about 5.02% protein, 27.70% fat, and 1.22% fiber. Textural attributes of cake from the premix were comparable to nongluten cakes available in the market. The cake premix T3 remained acceptable in terms of quality with progression of the storage period of 120 days in aluminum laminates under ambient conditions. During storage, the moisture content decreased from 9.52% to 6.72%, the free fatty acid increase was up to 0.117%, and the peroxide value increased up to 0.48 meq O2/kg. The developed gluten‐free premix will provide nutritional, economic, and better texture attributes to the target segment of consumers.

A novel approach for the development of edible oleofoams using double network oleogelation systems.

Whipped oleogels (oleofoams) are commonly stabilized by crystalline particles. Still, external factors like temperature fluctuations could change the state of the crystals (phase transitions), leading to the destabilization and disruption of oleofoams. Herein, a double network oleogelation system comprised of a primary crystalline network (using glycerol monostearate) and a secondary colloidal network (stabilized by soy protein isolate-anionic polysaccharides Mailard conjugates) is proposed as a novel strategy to overcome these challenges. It was observed that the incorporation of the secondary network resulted in a lower over-run, but a higher melting point, elasticity, foam stability, and more uniform bubble size distribution. This was explained by the strong interfacial stabilization provided by the colloidal network that can protect the crystalline particle against coarsening and oil drainage. These double network oleofoams, which could retain 41-48 % air (oleogel-based), display great potential for utilization in low-calorie lipid-based products.

Encapsulation of vitamin D3 using rhamnolipids-based nanostructured lipid carriers.

This work had as main objective to encapsulate vitamin D3 (VD3) into nanostructured lipid carriers (NLCs) using rhamnolipids as surfactant. Glycerol monostearate and medium chain triglycerides with 2.625 % of VD3 were used as lipid materials. The three formulations of NLCs with VD3 (NLCs+VD3) were composed by 99 % of aqueous phase, 1 % of lipid phase and 0.05 % of surfactant. The difference between them was the ratio of solid:liquid in lipid phase. The NLCs+VD3 sizes ranged between 92.1 and 108.1nm. The most stable formulation maintaining their caracteristics for 60days at 4°C. The NLCs+VD3 cytotoxicity demonstrated that concentrations of 0.25mg/mL or lower up had a good biocompatibility in vitro. During the in vitro digestion, formulations with lower sizes and higher content on solid lipid had higher lipolysis rate and consequently higher VD3 bioaccessibility. The rhamnolipids-based NLCs are a good option for the encapsulation of VD3.

Encapsulation of essential oil to prepare environment friendly nanobio-fungicide against Fusarium oxysporum f.sp. lycopersici: An experimental and molecular dynamics approach

This study aims to develop a nano-biofungicide comprising of volatile essential oil molecules to enhance its efficacy in the field of agriculture through easily scalable green synthesis technique. It was prepared through one pot hot melt ultrasonication technique with easy water dispersability and long term stability. The effective surface-active agent concentration which controls the size and stability of nano bio-fungicide was studied. The small particle size (158 nm) and narrow particle distribution (0.36) were obtained for the nano bio-fungicide at 20 mg of lecithin and 100 mg of surfactant concentration. The physico-chemical analysis revealed that, nano bio-fungicides were amorphous sphere-shaped nanoparticles with low melting point. The greater molecular level affinity of essential oil towards lipids and their interfacial interaction towards essential oil to achieve stabilised dispersion in aqueous environment were deciphered through molecular dynamics simulation. The unique preferential binding of eugenol, bornanone and cinnamaldehyde with the hydrocarbon chain of glycerol monostearate and phospholipid enhanced their biological stability in aqueous environment by preventing its autoxidation. It was further confirmed through accelarated ageing studies. The major components of essential oil like alpha-terpineol, linalool, thymol and cinamaldehyde had an encapsulation efficiency of 29 %, 65 %, 21 % and 50 % respectively. Subsequently, all these bioactives of essential oil follows Higuchi model of release kinetics. Besides, the essential oil loaded nanostructured lipid carrier had significantly higher mycelial growth inhibition than pure essential oil at the same concentration. Thus, our results suggest that essential oil compactly packed at the intramolecular spaces of lipids and surfactants were having enhanced bio-efficacy with long term storage potential. Hence, the present nano-biofungicide could be a good alternative to the harsh pesticidal chemicals with easy and simple large scale production protocol for the eco- friendly management of wilt disease caused by Fuarium oxysporum.

Cutinolytic esterases are induced by growth of the fungus Trichoderma harzianum on glyceryl monostearate in solid-state fermentation

Cutinolytic esterase are enzymes utilized in a wide variety of industrial applications, and they are capable of degrading emerging environmental pollutants. Due to the application and importance of these enzymes, it is crucial to develop an efficient method for cutinase production using a cost-effective inductor and an efficient microbial production system. In this work, the growth and cutinolytic esterase production of Trichoderma harzianum were evaluated in glucose-yeast extract media containing different glyceryl monostearate (GMS) concentrations (1, 3, and 5 g/L). It was used as inducer in solid-state fermentation. A medium lacking GMS was used as control. Biomass production and enzyme productivity were higher in inducer-added (1 g/L) medium than in the control medium. T. harzianum produced constitutive and inducible cutinolytic esterase, in which production was enhanced by GMS. In GMS-added cultures, two bands with cutinolytic esterase activity (60 and 150 kDa approximately) were observed by zymography, which were not observed in control culture. GMS represents a promising inducer for cutinolytic esterase production by fungi. This research represents the first approach for the study of cutinolytic esterase production using a synthetic molecule as an inducer.

Green Processing of Black Raspberry Pomace: Application of Sonotrode-Based Extraction Technique and Particles from Gas-Saturated Solutions (PGSS) Technology.

The aim of this study was to develop, for the first time, anthocyanin-enriched fractions from black raspberry pomace (BRP) using ultrasound-assisted extraction (UAE) via sonotrode and the Particles from Gas-Saturated Solutions (PGSS) process. UAEs with different amplitudes and sonication times were evaluated and showed relevant effects on the yields of target analytes. The raspberry pomace extracts were formulated in a powder form by PGSS using glyceryl monostearate as a carrier at different extract-to-carrier ratios of 1:11, 1:5, and 1:3. The effects of all variables were evaluated in terms of extraction yield, total phenolic content, and encapsulation yield. UAE was strongly affected by amplitude, and the highest amplitude (100%) provided the best results for extraction yield and total phenolics. HPLC of UAE extracts and powders was utilized for quantification of polyphenol compounds, showing cyanidin-3-rutinoside as a main compound, followed by cyanidin-3-glucoside, rutin, ellagic acid, and gallic acid. These results show that these time-efficient and high-performance techniques enable the production of natural fractions from industrial BRP with acceptable characteristics to be used for the development of nutraceuticals and different food formulations.

Efficacy evaluation and metabolomics analysis of raw and salt-processed Achyranthes bidentata Radix in zebrafish larvae for osteoporosis treatment

Osteoporosis, characterized by reduced bone density and the deterioration of bone tissue, poses a significant health challenge. The mechanisms underlying the protective effects of both raw and salt-processed Achyranthes bidentata Radix in osteoporosis remains unclear. This study endeavors to unravel and analyze the therapeutic mechanisms of these two forms of Achyranthes bidentata Radix in osteoporotic zebrafish larvae, utilizing GC/MS-based metabolomics. Zebrafish larvae were categorized into five groups: blank control, model, positive control, and groups treated with raw and salt-processed Achyranthes bidentata Radix. Following drug administration, notable enhancements were observed in both mineralized bone area and cumulative optical density. Various data mining techniques were employed, encompassing principal component analysis, orthogonal projections to latent structures discriminant analysis, and metabolic pathway analysis. These analyses unveiled 26 differential endogenous metabolites with significant biological implications in the zebrafish osteoporosis model. Among these metabolites, 12 (including acetamide, L-lactic acid, threonine, glycerol, rhamnose, azelaic acid, palmitic acid, inositol, stearic acid, hexadecane, sucrose, and glyceryl monostearate) were validated using standard compounds, exhibiting strong linear correlation coefficients (R2) ranging from 0.9917 to 0.9999. Furthermore, the method demonstrated excellent repeatability, as evidenced by relative standard deviation (RSD) values below 7.37%. The average spiked recoveries of the standard compounds fell within the range of ± 15%, ranging from 85.45% to 114.28%. Additionally, the stability of the standard compounds was confirmed after three freeze-thaw cycles, with RSD values remaining below 14.40%. Collectively, the metabolomic analysis unearthed potential biomarkers that could serve as indicators of the therapeutic effects of raw and salt-processed Achyranthes bidentata Radix on osteoporosis. This research offers valuable insights into the potential utilization of these herbal remedies as natural interventions for osteoporosis.

Effect of composition of emulsifier blends on aerated emulsions: Stability, thermodynamic, interfacial behavior and aeration properties

In this study, we investigated the effect of emulsifier blends with different structures and lipophilic-hydrophilic balance (HLB) on the interfacial composition and crystallization behavior, as well as on the aeration properties of emulsions. The droplet size, physical stability, rheological properties, and partial aggregation rate of the quiescent emulsions were determined. Further, the interfacial protein content, interfacial tension, interfacial rheological properties, and thermodynamic properties were analyzed, and the aeration and texture of the foams were recorded. First, there was a significant difference in emulsion droplet size after compounding with glyceryl monostearate (GM) even though sucrose ester S-1570 (SE) and polysorbate 80 (TW) had the same HLB (p < 0.05), but sorbitan monooleate 80 (SP)-TW performed consistently with GM-TW, having the smallest particle size. Secondly, the addition of GM-SE changed the thermodynamic properties and significantly increased the crystallization temperature of fat (15.79 °C), but had no significant effect on the aeration process. In addition, although GM-SE resulted in emulsions with the lowest interfacial tension, the fat globule surface exhibited viscous behavior (E' < E″) and the worst physical stability of the emulsion, while triglycerol monostearate (TMS)-TW balanced the interfacial tension and strength giving good performance in both emulsion stability and aeration characteristics. In general, the design of compounding emulsifiers should pay more attention to the structural of the emulsifier. These results provide an interesting point of departure for further development of compounding emulsifiers for different needs.

Spray-dried Solid Lipid Nanoparticles for Enhancing Berberine Bioavailability via Oral Administration.

Berberine (BBR), an Eastern traditional medicine, has expressed novel therapeutic activities, especially for chronic diseases like diabetes, hyperlipemia, hypertension, and Alzheimer's disease. However, the low oral bioavailability of BBR has limited the applications of these treatments. Hence, BBRloaded solid lipid nanoparticles (BBR-SLNs) were prepared to improve BBR absorption into systemic circulations via this route. BBR-loaded solid lipid nanoparticles (BBR-SLNs) were prepared by ultrasonication and then transformed into solid form via spray drying technique. The size morphology of BBR-SLNs was evaluated by dynamic light scattering (DLS) and scanning electron microscope (SEM). Crystallinity of BBR and interaction of BBR with other excipients were checked by spectroscopic methods. Entrapment efficiency of BBR-SLNs as well as BBR release in gastrointestinal conditions were also taken into account. Lastly, SLN's cytotoxicity for loading BBR was determined with human embryonic kidney cells (HEK293). Stearic acid (SA), glyceryl monostearate (GMS), and poloxamer 407 (P407) were selected for BBRSLNs fabrication. BBR-SLNs had homogenous particle sizes of less than 200 nm, high encapsulation efficiency of nearly 90% and loading capacity of above 12%. BBR-SLN powder could be redispersed without significant changes in physicochemical properties and was stable for 30 days. Spray-dried BBR-SLNs showed a better sustained in vitro release profile than BBR-SLNs suspension and BBR during the initial period, followed by complete dissolution of BBR over 24 hours. Notably, cell viability on HEK293 even increased up to 150% compared to the control sample at 100 μg/mL BBR-unloaded SLNs. Hence, SLNs may reveal a promising drug delivery system to broaden BBR treatment for oral administration.

QbD-driven development of phospholipid-embedded lipidic nanocarriers of raloxifene: extensive in vitro and in vivo evaluation studies.

Raloxifene (RLX) is popularly indicated in treatment of osteoporosis and prevention of breast cancer. Owing to its poor aqueous solubility, high pre-systemic metabolism, intestinal glucuronidation, and P-glycoprotein (P-gp) efflux, however, it demonstrates low (< 2%) and inconsistent oral bioavailability. The current work, Quality by Design (QbD)-driven development of phospholipid-embedded nanostructured lipidic carriers (NLCs) of RLX, accordingly, was undertaken to potentiate its lymphatic uptake, augment oral bioavailability, and possibly reduce drug dosage. Factor screening and failure mode effect analysis (FMEA) studies were performed to delineate high-risk factors using solid lipid (glyceryl monostearate), liquid lipid (vitamin E), and surfactant (Tween 80). Response surface optimization studies were performed employing the Box-Behnken design. Mathematical and graphical methods were adopted to embark upon the selection of optimized NLCs with various critical quality attributes (CQAs) of mean particle size as 186nm, zeta potential of - 23.6mV, entrapment efficiency of 80.09%, and cumulative drug release at 12h of 83.87%. The DSC and FTIR studies, conducted on optimized NLCs, indicated successful entrapment of drug into the lipid matrix. In vitro drug release studies demonstrated Fickian diffusion mechanism. In vivo pharmacokinetic studies in rats construed significant improvement in AUC0-72h (4.48-folds) and in Cmax (5.11-folds), unequivocally indicating markedly superior (p < 0.001) oral bioavailability of RLX-NLCs vis-à-vis marketed tablet formulation. Subsequently, level "A" in vitro/in vivo correlation (IVIVC) was also successfully attempted between the percentages of in vitro drug dissolved and of in vivo drug absorbed at the matching time points. In vitro cytotoxicity and cellular uptake studies also corroborated higher efficacy and successful localization of coumarin-6-loaded NLCs into MG-63 cells through microfluidic channels.

Molecular docking and antibacterial activity of Sargassum fusiforme extracts against major coral pathogens.

The present study evaluates the antibacterial properties of alkaloids and the crude extracts (ethanol, n-hexane and ethyl acetate) from seaweed Sargassum fusiforme against coral pathogens (Photobacterium galatheae, Vibrio harveyi, Bordetella trematum,and Ochrobactrum pseudogrignonese) isolated from coral Porites lutea. To our knowledge, this is the first in vitro assay for such extracts on Porites lutea coral pathogens. Bacterial pathogens have been identified using 16S RNA and BankIt into gene bank and given the accession numbers (OR401000; OR401001; OR401336, and OR400998 respectively). GC-Mass profiling conducted for n-hexane compounds confirmed the presence of thirty-eight molecules, twelve of which have been previously reported for their bioactivity. The results revealed that alkaloids and n-hexane extract demonstrated eminent antibacterial activity compared to the other extracts against the tested coral pathogenic bacteria. Molecular docking was conducted to evaluate the twelve previously mentioned bioactive molecules to get a full understanding of the interaction of those bioactive molecules on vital bacterial proteins (Hemolysin protein (PDB ID: 1XEZ) and Cytoplasmic proteins (PDB ID: 3TZC)). Docked twelve molecules against hemolysin protein (PDB ID: 1XEZ) came exactly in line with the docked result of the same molecules with cytoplasmic proteins (PDB ID: 3TZC), proving the bioactivity of 6-O-Palmitoyl-L-ascorbic acid, 3TMS derivative; Glycerol monostearate, 2TMS derivative and Eicosanoic acid complexes in antibacterial activity action and score higher than reference ligand. Those three compounds will be investigated separately in future in vitro assay soon. Our conclusions align with the study's antibacterial in vitro assay results. The present study reports the novelty of different extracts of S. fusiforme as an antibacterial agent against coral pathogenic bacteria that trigger diseases in Porites lutea.

Alginate-based gel beads with bigel structures: Preparation, characterization and bioactive encapsulation

The current study developed novel gel beads with bigel structures based on alginate hydrogel and glycerol monostearate oleogel. Bigel beads with different structures were prepared by varying oleogel content, and the beads were also used to co-encapsulate lipophilic and hydrophilic biaoctives. All the beads had high sphericity (>0.94), and the bead size was increased with the increase in oleogel content. Beads with higher content of oleogel had lower shrinking rates and higher level of oil filling the gel pores. The oil droplets were generally acting as inactive fillers in the gel beads, as the mechanical strength (Young's modulus and hardness) was declining with the increase in oleogel content, and no interaction between the oleogel and hydrogel was detected by FTIR. Swelling studies revealed that beads in salt solution at higher temperature had higher swelling ratio, and the increase in oleogel content could inhibit the swelling. The bigel beads were able to encapsulate EGCG and curcumin simultaneously, and beads with higher oleogel content generally had lower encapsulation efficiency of EGCG but higher efficiency of curcumin. The gel structures provided good protection for curcumin, and about 70% of the original curcumin was retained after a 40-day storage test. The study provided novel information regarding the structure-function relationship of the bigel beads, which could be useful for the development of functional food materials.