Development of microparticles and microparticulated tablets containing piperine

Abstract Piper nigrum (black pepper) is used in Indian traditional medicine and its main alkaloid, Piperine (PIP), presents antioxidant, antitumor and neuroprotective pharmacological properties. This substance is insoluble in aqueous media and can irritate the gastrointestinal tract. Aiming to avoid these inconvenient characteristics and enable PIP oral administration, this study suggested the PIP microencapsulation through the emulsion-solvent evaporation method and the preparation of microparticulated tablets by direct compression. An UV-spectroscopy method was validated to quantify PIP. Microparticles and microparticulated tablets were successfully obtained and the microparticles exhibited excellent flow. The scanning electron microscopy images showed that PIP microparticles were intact after compression. The in vitro release showed a controlled release of PIP from microparticles and PIP microparticles from tablets in comparison to PIP and PIP tablets. The release profiles of PIP microparticles and the microparticulated tablets were similar. Therefore, tablets containing PIP microparticles are promising multiparticulated dosage forms because a tablet allows microparticles administration and the intact ones promote a controlled release, decreasing its irritating potential on the mucosa.

The use of Dalmatian pyrethrum daisy and an excipient in the treatment of seborrheic dermatitis.

The active ingredients of the Pyretrin-D trichological cosmetic series, namely benzyl benzoate, Dalmatian pyrethrum daisy, Cistus incanus, tea tree oil and geranium oil, almond acid and arginine were tested in respect to the treatment of seborrheic dermatitis. The paper describes the application of Dalmatian pyrethrum daisy and the excipient. Methods and devices used to confirm the effectiveness of the tested formulations included the TrichoScope Polarizer Dino-Lite (MEDL4HM) and the scanning electron microscope (SEM).

Biofabrication of ZnO nanoparticles using Acacia arabica leaf extract and their antibiofilm and antioxidant potential against foodborne pathogens.

Emergence of multidrug resistant pathogens is increasing globally at an alarming rate with a need to discover novel and effective methods to cope infections due to these pathogens. Green nanoparticles have gained attention to be used as efficient therapeutic agents because of their safety and reliability. In the present study, we prepared zinc oxide nanoparticles (ZnO NPs) from aqueous leaf extract of Acacia arabica. The nanoparticles produced were characterized through UV-Visible spectroscopy, scanning electron microscopy, and X-ray diffraction. In vitro antibacterial susceptibility testing against foodborne pathogens was done by agar well diffusion, growth kinetics and broth microdilution assays. Effect of ZnO NPs on biofilm formation (both qualitatively and quantitatively) and exopolysaccharide (EPS) production was also determined. Antioxidant potential of green synthesized nanoparticles was detected by DPPH radical scavenging assay. The cytotoxicity studies of nanoparticles were also performed against HeLa cell lines. The results revealed that diameter of zones of inhibition against foodborne pathogens was found to be 16-30 nm, whereas the values of MIC and MBC ranged between 31.25-62.5 µg/ml. Growth kinetics revealed nanoparticles bactericidal potential after 3 hours incubation at 2 × MIC for E. coli while for S. aureus and S. enterica reached after 2 hours of incubation at 2 × MIC, 4 × MIC, and 8 × MIC. 32.5-71.0% inhibition was observed for biofilm formation. Almost 50.6-65.1% (wet weight) and 44.6-57.8% (dry weight) of EPS production was decreased after treatment with sub-inhibitory concentrations of nanoparticles. Radical scavenging potential of nanoparticles increased in a dose dependent manner and value ranged from 19.25 to 73.15%. Whereas cytotoxicity studies revealed non-toxic nature of nanoparticles at the concentrations tested. The present study suggests that green synthesized ZnO NPs can substitute chemical drugs against antibiotic resistant foodborne pathogens.

Preparation and structural properties of starch phosphate modified by alkaline phosphatase.

In this study, a method for the synthesis of starch phosphate using the transferase properties of alkaline phosphatase was explored. Maize starch was treated with a pyrophosphate solution containing alkaline phosphatase and catalytic ions under pH 8 at 37 °C. The synthesis of starch phosphate was evaluated and compared with untreated and treated starch controls. The phosphorus content of the samples increased up to 8500% with the catalytic ion concentration, whereas the peak viscosity by up to 41.4% decreased. The crystallinity and enthalpy of the phosphorylated samples were reduced by up to 26.8% and 23.3%, respectively; however, no significant was observed by Fourier-transform infrared spectrometer. The roughness of the starch surface and the distribution of elemental phosphorus were observed by scanning electron microscopy and energy dispersive Spectrometry. X-ray photoelectron spectroscopy and time of flight secondary ion mass spectrometry results further indicated the grafting of the phosphate radical.

Calendula officinalis L. flower extract-mediated green synthesis of silver nanoparticles under LED light

Abstract Silver nanoparticles (AgNPs) are among the most known nanomaterials being used for several purposes, including medical applications. In this study, Calendula officinalis L. flower extract and silver nitrate were used for green synthesis of silver nanoparticles under red, green and blue light-emitting diodes. AgNPs were characterized by Ultraviolet-Visible Spectrophotometry, Field Emission Scanning Electron Microscopy, Dynamic Light Scattering, Electrophoretic Mobility, Fourier Transform Infrared Spectroscopy and X-ray Diffraction. Isotropic and anisotropic silver nanoparticles were obtained, presenting hydrodinamic diameters ranging 90 - 180 nm, polydispersity (PdI > 0.2) and moderate stability (zeta potential values around - 20 mV)

The impact of the physical form of torularhodin on its metabolic fate in the gastrointestinal tract.

Torularhodin is a fungal carotenoid with multiple health benefits. However, the relationship between its physical form and metabolic fate in the gastrointestinal tract (GIT), which is essential to its bioavailability and health efficacy, has rarely been studied. Thus, physical forms of torularhodin including nanoemulsion powder (T-EP), capsules of the T-EP by alginate (T-EPA), and solution in MCT oil (T-oil) were used in the study. T-EP was produced through OSA-starch-mediated torularhodin emulsification and spray drying whereas the T-EPA was alginate-based capsules of the T-EP particles that were entrapped in the network structure of the alginate matrix as observed by scanning electron microscopy (SEM). The oil digestibility in the simulated small intestine was decreased from T-EP (100%), T-oil (60%) to T-EPA (40%), and the bioaccessibilities were 27%, 15% and 12%, respectively. The in vivo study using mice revealed that the content of torularhodin gradually decreased along with the digestion time in both the stomach and small intestine while a significantly higher colonic accumulation was observed in T-EPA compared to T-oil and T-EP. In vitro fecal fermentation showed that propionate (32 mM) was the predominant metabolite produced by torularhodin in the physical form of T-EPA. Thus, the physical form of torularhodin is a significant contributing factor to its GIT metabolic fate, and a health outcome-oriented design of the physical form of torularhodin or other nutraceuticals is beneficial for the development of functional foods with enhanced health benefits.

Preparation, characterization, and evaluation of HP-ß-CD inclusion complex with alcohol extractives from star anise.

The active compounds in star anise alcohol extractives (SAAE) have potent bioactivity. However, their poor solubility and stability limit their applications. In this study, SAAE/hydroxypropyl-ß-cyclodextrin (HP-ß-CD) inclusion complexes were prepared as a strategy to overcome the abovementioned disadvantages. The phase solubility results indicated that the solubility of the inclusion complex was enhanced. Complexation was confirmed by complementary methods, including Fourier-transform infrared spectroscopy, nuclear magnetic resonance spectroscopy, scanning electron microscopy, and transmission electron microscopy, which proved to be extremely insightful for studying the inclusion formation phenomenon between SAAE and HP-ß-CD. Despite there being no apparent improvements in the antioxidant capacity and antimicrobial activity, the results of the stability studies presented higher thermal, volatile, and photostability after encapsulation. Further, molecular modeling was used to investigate the factors influencing complex formation and provide the most stable molecular conformation. Thus, based on the obtained results, this study strongly demonstrates the potential of the SAAE/HP-ß-CD inclusion complex in the food industry.

Effect of cellulose and starch fatty acid esters addition on microstructure and physical properties of arabinoxylan films.

Arabinoxylan (AX) and cellulose were extracted from wheat straw, whereas starch was extracted from potato peel. Thereafter, cellulose and starch were esterified with lauric, myristic, palmitic and stearic acids to prepare corresponding cellulose (CFAs) and starch fatty acid esters (SFAs) with DS 2.1-2.8. XRD study revealed remarkable loss of crystallinity in cellulose and starch due to fatty acid esterification. The addition of palmitate and stearate esters of cellulose and starch to AX formed laminar film microstructures which limited water vapor permeability whereas films prepared by blending AX with laurate and myristate esters of starch and cellulose were less effective as water vapor barrier due to their non-layer microstructures. The laminar structures also resulted significant reduction in mechanical strength of the composite films. Furthermore, all AX-CFAs and AX-SFAs films were thermally more stable than native composite films. These films might be used to produce industrially useful coating material for food products.

In-situ fermentation with gellan gum adding to produce bacterial cellulose from traditional Chinese medicinal herb residues hydrolysate.

In this study, bacterial cellulose was synthesized by Taonella mepensis from traditional Chinese medicinal herb residues hydrolysate. To overcome the inhibitory effect of fermentation environment, in-situ fermentation with gellan gum adding was carried out for the first time. After 10 days' static fermentation, both high-acyl gellan gum and low-acyl gellan gum adding showed certain beneficial effects for bacterial cellulose production that the highest bacterial cellulose yield (0.866 and 0.798 g/L, respectively) was 59% and 47% higher than that (0.543 g/L) without gellan gum adding. Besides, gellan gum based bacterial cellulose showed some better texture characteristics. Gellan gum was loaded in the nano network of bacterial cellulose, and gellan gum adding had some influence on the crystal structure and thermal degradation behaviors of bacterial cellulose but affected little on its functional groups. Overall, this in-situ fermentation technology is attractive for bacterial cellulose production from low-cost but inhibitory substrates.

Anchor and bridge functions of APTES layer on interface between hydrophilic starch films and hydrophobic soyabean oil coating.

One of the well-recognized weaknesses of starch-based materials is their sensitivity to moisture, which limits their expanding applications. Natural materials, soyabean oils have been used as a coating for starch film, but the poor interface between hydrophilic starch and hydrophobic soyabean oil needs to be improved. In this work, (3-Aminopropyl) triethoxysilane (APTES) was used to reinforce the bonding between starch matrix and the coating of bio-based acrylated epoxidized soyabean oil (AESO). Study results show that APTES interacted effectively with both starch films via hydrogen bonding, and chemical bonds with AESO through the Michael addition reaction. Pull adhesion and cross-cutting tests demonstrated that the interfacial adhesion was significantly improved after treating their surface with APTES. The interfacial adhesion strength increased over 4 times after treating with 1.6 wt% APTES. The starch films treated with APTES and AESO coating were intact after soaking in water for more than 2 h.

Chitosan-silica with hops ß-acids added films as prospective food packaging materials: Preparation, characterization, and properties.

In this study, silica (SiO2) and ß-acids were added to the chitosan films in order to improve the film's properties. Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction analysis (XRD) were used to explore the structure of film. The results of mechanical test indicated that the film containing SiO2 (0.3%) and ß-acids (0.3%) could obtain a significant tensile strength (10.04 MPa). The complex films possessed a good inhibitory effect on three types of bacteria, and good antioxidant activity (>56%, DPPH). The release mechanism of ß-acids from the films exhibited Fickian diffusion (n < 0.45). During the storage of soybean oil, the films could well control the changes of the peroxide value, acid value and thiobarbituric acid reactant content. Overall, the biofilms not only possess good physical and chemical properties, but also prolongs the time of food storage.

Facile Synthesis of Bio-Antimicrobials with "Smart" Triiodides.

Multi-drug resistant pathogens are a rising danger for the future of mankind. Iodine (I2) is a centuries-old microbicide, but leads to skin discoloration, irritation, and uncontrolled iodine release. Plants rich in phytochemicals have a long history in basic health care. Aloe Vera Barbadensis Miller (AV) and Salvia officinalis L. (Sage) are effectively utilized against different ailments. Previously, we investigated the antimicrobial activities of smart triiodides and iodinated AV hybrids. In this work, we combined iodine with Sage extracts and pure AV gel with polyvinylpyrrolidone (PVP) as an encapsulating and stabilizing agent. Fourier transform infrared spectroscopy (FT-IR), Ultraviolet-visible spectroscopy (UV-Vis), Surface-Enhanced Raman Spectroscopy (SERS), microstructural analysis by scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), and X-Ray-Diffraction (XRD) analysis verified the composition of AV-PVP-Sage-I2. Antimicrobial properties were investigated by disc diffusion method against 10 reference microbial strains in comparison to gentamicin and nystatin. We impregnated surgical sutures with our biohybrid and tested their inhibitory effects. AV-PVP-Sage-I2 showed excellent to intermediate antimicrobial activity in discs and sutures. The iodine within the polymeric biomaterial AV-PVP-Sage-I2 and the synergistic action of the two plant extracts enhanced the microbial inhibition. Our compound has potential for use as an antifungal agent, disinfectant and coating material on sutures to prevent surgical site infections.

Experimental and Theoretical Studies on Extract of Date Palm Seed as a Green Anti-Corrosion Agent in Hydrochloric Acid Solution.

Extracts from plant materials have great potential as alternatives to inorganic corrosion inhibitors, which typically have harmful consequences. Experimental and theoretical methodologies studied the effectiveness of agricultural waste, namely, date palm seed extract as a green anti-corrosive agent in 0.5 M hydrochloric acid. Experimental results showed that immersion time and temperature are closely related to the effectivity of date palm seed as a corrosion inhibitor. The inhibition efficiency reduced from 95% to 91% at 1400 ppm when the immersion time was increased from 72 h to 168 h. The experimental results also indicated that the inhibition efficiency decreased as the temperature increased. The presence of a protective layer of organic matter was corroborated by scanning electron microscopy. The adsorption studies indicated that date palm seed obeyed Langmuir adsorption isotherm on the carbon steel surface, and Gibbs free energy values were in the range of -33.45 to -38.41 kJ·mol-1. These results suggested that the date palm seed molecules interacted with the carbon steel surface through mixture adsorption. Theoretical calculations using density functional theory showed that the capability to donate and accept electrons between the alloy surface and the date palm seed inhibitor molecules is critical for adsorption effectiveness. The HOMO and LUMO result indicated that the carboxyl (COOH) group and C=C bond were the most active sites for the electron donation-acceptance type of interaction and most auxiliary to the adsorption process over the Fe surface.

Structural evidence for extracellular silica formation by diatoms.

The silica cell wall of diatoms, a widespread group of unicellular microalgae, is an exquisite example for the ability of organisms to finely sculpt minerals under strict biological control. The prevailing paradigm for diatom silicification is that this is invariably an intracellular process, occurring inside specialized silica deposition vesicles that are responsible for silica precipitation and morphogenesis. Here, we study the formation of long silicified extensions that characterize many diatom species. We use cryo-electron tomography to image silica formation in situ, in 3D, and at a nanometer-scale resolution. Remarkably, our data suggest that, contradictory to the ruling paradigm, these intricate structures form outside the cytoplasm. In addition, the formation of these silica extensions is halted at low silicon concentrations that still support the formation of other cell wall elements, further alluding to a different silicification mechanism. The identification of this unconventional strategy expands the suite of mechanisms that diatoms use for silicification.

Structural characterization and osteogenic activity in vitro of novel polysaccharides from the rhizome of Polygonatum sibiricum.

Polygonatum sibiricum Red., a kind of edible and medicinal plant, has a long history of use in traditional Chinese medicine and as a nutritional food additive. Water-soluble crude polysaccharide (PS50) was obtained from P. sibiricum rhizome. After deproteinization and dialysis, PS50 was isolated and purified via DEAE-52 cellulose and Sephadex G-75 gel filtration chromatography to obtain two novel polysaccharides (PSP50-2-1 and PSP50-2-2). Chemical analysis and nuclear magnetic resonance (NMR) studies indicated that PSP50-2-1 was composed of ß-d-Glcp-(1→, →2)-ß-d-Galp-(1→, →2,6)-ß-d-Galp-(1→, ß-d-Fruf-(2→, and PSP50-2-2 was composed of ß-d-Glcp-(1→, ß-d-Galp-(1→, →2)-ß-d-Galp-(1→, →6)-ß-d-Galp-(1→, →2,6)-ß-d-Galp-(1→, ß-d-Fruf-(2→. The morphological analysis suggested that PSP50-2-1 and PSP50-2-2 both had a rough surface with cracks. Pharmacological studies showed that PSP50-2-2 at concentrations of 2.59 and 5.19 µM significantly promoted the differentiation and mineralization of MC3T3-E1 cells in vitro, which indicated that PSP50-2-2 had a function of osteogenic activity. Above all, this study provides evidence that PSP50-2-2 may be used as an anti-osteoporotic agent, with applications in health-care and pharmaceutical industries.

Nutritional targeting modification of silkworm pupae oil catalyzed by a smart hydrogel immobilized lipase.

To prepare a nutritional supplement using silkworm pupae oil (SPO) as a feedstock, a microfluidic reactor with a smart hydrogel immobilized lipase was first constructed to reduce the relative content of palmitic acid at sn-1,3 and improve the nutritional function. The effects of flow rate, reaction temperature, and substrate molar ratio were investigated. In vitro digestion and pH-stat models were employed to analyze the digestion feature after the modification of SPO, while HPLC-ELSD, zeta potential, DSC, and TGA were used to evaluate the nutritional function. The relative content of "OOO" and "OPO" type triglycerides was increased by 49.48% and 107.67%, and that of palmitic acid at sn-1,3 was decreased by 49.61% in 10 s. After the verification of the in vitro digestion model, the fatty acid release rate of the modified SPO was significantly improved by 22.07%, indicating the nutritional function improvement of SPO. Therefore, the nutritional function of SPO has been improved successfully by the application of a microchannel reactor with photo-immobilized lipase, which could set a reference for the utilization of insect oil resources.

Biosystematic studies of some Egyptian species of Cestrum (Solanaceae).

Cestrum is the second largest genus of family Solanaceae, after Solanum, distributed in warm to subtropical regions. Species of genus Cestrum are one of the most ethnopharmacological relevant plants, for their broad biological and pharmacological properties. There is a scarcity to taxonomical studies and identification of these plants in Egypt, thus, the objective of this study was to implement various morphological features, chemical markers and molecular tools to emphasize the taxonomical features of the different Cestrum species. Morphologically, the epidermal cells of C. diurnum, C. elegans and C. parqui were irregular with sinuate anticlinal wall patterns for both surfaces, while, C. nocturnum has anticlinal walls, sinuolate with polygonal to irregular epidermal cells on the abaxial surface. The species of Cestrum have hypostomatic leaves, except C. parqui that has amphistomatic leaves. The experimented species of Cestrum have Anomocytic and anisocytic stomata, while, C. elegans has a diacytic stomata. The morphologically identified Cestrum spp were molecular confirmed based on their ITS sequences, the sequences of C. diurnum, C. nocturnum, C. elegans and C. parqui were deposited on genbank with accession # MT742788.1, MT749390.1, MW091481.1 and MW023744.1, respectively. From the SCOT analyses, the four species of Cestrum were grouped into 2 clusters (I, II), cluster I contains C. elegans, C. nocturnum and C. parqui, while cluster II contains only C. diurnum with 100% polymorphism for all primers. From the GC-MS profile, the C. diurnum exhibited a diverse metabolic paradigm, ensuring their richness with different metabolites comparing to other experimented Cestrum species. Among the total resolved metabolites, 15-methyltricyclo 6.5.2-pentadeca-1,3,5,7,9, 11,13-heptene was the highly incident compound in C. elegans (35.89%) followed by C. parqui (21.81%) and C. diurnum (11.28%), while it absent on C. nocturnum. The compound, 2,2',6,6'-tetra-tert-butyl-4,4'-methylenediphenol was highly detected in C. elegans and C. dirunum with minor amounts in the other Cestrum species. Cypermethrin and 3-butynyl-2,2,5-trimethyl-1,3-dioxane-5-methanol were pivotally reported in C. nocturnum. Taken together, from molecular and metabolic markers, C. diurnum, C. parqui and C. elegans have higher proximity unlike to C. nocturnum.

Hydrothermal synthesis of hydroxyapatite powders using Response Surface Methodology (RSM).

Hydroxyapatite (HAp)-[Ca10 (PO4)6(OH) 2] has a similar chemical composition to bone material, making it the main mineral supplement in bone-making. Due to its high biocompatibility, hydroxyapatite is widely used in the repair of bone deficiencies and in the production of dental or orthopedic implants. In this research, hydroxyapatite nanopowder was synthesized using a hydrothermal technique. Fourier Transform Infrared Spectroscopy (FTIR) and transmission electron microscopy (TEM) were used to investigate the chemical structure and morphology of the synthesized hydroxyapatite powder. X-ray diffraction (XRD) was used to evaluate the phase analysis of HAp nanopowder. In addition, bioactivity HAp assessment was conducted by scanning electron microscopy (SEM) attached with Energy Dispersive X-Ray Spectroscopy (EDX) analysis. Response Surface Methodology (RSM) with central composite design (CCD) was used in order to determine the optimal conditions for yield, size, and crystallinity. Three independent variables (pH, temperature, and hydrothermal treatment time) were investigated. The yield was observed to increase in alkaline conditions; pH showed the greatest influence on the yield, size, and crystallinity of the synthesized hydroxyapatite, based on Analysis of Variance. The results of bioactivity evaluation are showed high bioactivity due to the formation of apatite on the surface of the synthesized nanopowder.

A competitive nature-derived multilayered scaffold based on chitosan and alginate, for full-thickness wound healing.

The aim of this study was to evaluate a bioactive multilayer wound dressing, based on chitosan and alginate. To enhance healing potential, Dracaena Cinnabari and Aloe Vera were loaded as separate layers into the scaffold. The bare and bioactive multilayered scaffolds were fabricated by an iterative layering freeze-drying technique. Following of topographical, chemical, and physical assessment, the performance of the scaffolds was evaluated in vitro and in vivo. The results revealed adequate attachment, and proliferation of human foreskin fibroblasts, indicating excellent biocompatibility of the bioactive scaffold. In vivo, the performance of the multi-layered scaffold loaded with the bioactive materials was comparable with Comfeel plus®. The wounds treated with the bioactive scaffold exhibited superior hypergranulation, fibroblast maturation, epithelization, and collagen deposition, with minimal inflammation, and crust formation. It is concluded that the synergism of extracellular matrix-mimicking multi-layered scaffolding with Aloe Vera and Dracaena Cinnabari could be considered as a supportive wound dressing.

Formation and structural evolution of starch nanocrystals from waxy maize starch and waxy potato starch.

The formation and structural evolution of starch nanocrystals from waxy maize starch (WMS) and waxy potato starch (WPS) by acid hydrolysis were studied. The relative crystallinity, the short-range molecular order, and the double-helix content of WMS and WPS increased significantly during the initial stage of acid hydrolysis, indicating that acid preferentially eroded the amorphous regions of starch granules. With time, there was increased destruction of lamellar structures, causing the granules to completely disintegrate to form nanocrystals. WMS and WPS displayed different hydrolysis mechanisms. WPS was more susceptible to acid hydrolysis than WMS, and WMS exhibited an endo-corrosion pattern and WPS showed an exo-corrosion pattern. WMS nanocrystals had a parallelepiped shape, and WPS nanocrystals were round. This difference in shape is likely due to the different packing configuration of double helices in native starches.