Search Results (75)

Antarctic krill protein (AKP) was conjugated with three reducing monosaccharides (ribose, glucose, fructose) and five polysaccharides (xanthan gum, konjac glucomannan, inulin, κ-carrageenan, and pectin) via a controlled Maillard-type glycation process (pH 7.0, 90 °C, 24 h). We comparatively evaluated glycation reactivity (color change and degree of glycation), structural responses (particle size, FTIR, intrinsic fluorescence, surface hydrophobicity, and microstructure), and key techno-functional properties (solubility, water- and oil-holding capacities, and emulsifying performance). Monosaccharide-conjugated AKP exhibited stronger browning and higher apparent glycation activity, consistent with the higher reactivity of small-molecule sugars. In contrast, polysaccharide-conjugated AKP showed more pronounced improvements in dispersion-related and interfacial functions, reflecting enhanced steric stabilization and hydration after polysaccharide grafting. Notably, κ-carrageenan conjugation delivered the strongest overall functional enhancement (water-holding capacity ≈ 22.1 g/g; oil-holding capacity ≈ 10 g/g) and the most stable emulsions. These findings clarify how glycosylating-agent size and architecture steer AKP glycation outcomes, providing a practical basis for tailoring AKP ingredients for aqueous and emulsion-based foods. Full article

The therapeutic potential of prodigiosin as a hydrophobic anticancer agent can be enhanced by various approaches, one of which is the loading of PG into extracellular vesicles. Drug distribution and stability in aqueous media play a crucial role in targeting and accumulation, thereby enabling the attainment of therapeutically effective drug concentrations. Extracellular vesicles are nano-sized, cell-derived vesicles with a lipid bilayer membrane. Extracellular vesicles can be utilized as drug carriers for both water-soluble and non-water-soluble therapeutic agents. We hypothesized that microvesicles could effectively address the current challenges of prodigiosin delivery. Several different techniques have been developed for fabricating extracellular vesicles. These include microvesicles induction by cytochalasin B treatment as well as cell cultivation in serum depleted media. In our study, prodigiosin, like cytochalasin B, demonstrated efficacy in microvesicles formation based on protein quantification and Nanoparticle Tracking Analysis. In addition, Nanoparticle Tracking Analysis showed that vesicles from mesenchymal stem cells are more stable under ultrasound exposure. Microvesicles encapsulating prodigiosin, compared to unmodified naïve ones, demonstrated slightly increased zeta potentials and hydrodynamic diameters, which probably contributed to better stability. We demonstrated that ultrasonic treatment for the loading of prodigiosin does not significantly increase the proportion of prodigiosin-positive microvesicles in comparison with microvesicles induced with prodigiosin; moreover, this method cannot be considered as optimal due to its disadvantages, such as particle aggregation. Prodigiosin-induced and prodigiosin-loaded microvesicles from mesenchymal stem cells were significantly smaller and less polydisperse in size. Overall, prodigiosin encapsulated in extracellular vesicles might be more suitable for medical and clinical applications compared to pure forms of PG due to their cell membrane compatibility. Full article

The cosmetic industry is constantly evolving to create new formulations that offer controlled and specific release of active ingredients, as well as greater penetration, duration and stability of the resulting products. To fulfil all these objectives, the use of cyclodextrins in different cosmetic formulations is being considered. CDs are cyclic oligosaccharides with a hydrophilic outer surface and an inner cavity able to encapsulate hydrophobic molecules. This property can be used to form complexes with hydrophobic molecules and solubilise them in aqueous matrices, such as creams or gels. This review analyses the main advantages that these agents provide in cosmetic products, such as protection, administration and controlled release of bioactive ingredients, improved water solubility, reduced fragrance volatility, masking off unpleasant odours, modification of the physicochemical properties of formulations or prevention of ingredient side effects, among others. Formulations of lotions, sunscreens, deodorants, gels or perfumes containing CDs are already on the market, and new ones are being developed. Moreover, the regulations concerning their use, the types of cyclodextrins allowed and the mechanism required to produce CD-guest inclusion complexes are reviewed. Likewise, the use of CDs alone or encapsulating other compounds makes them an extremely versatile nanomaterial for dermofacial and cosmetic formulations. Full article

Background/Objectives: Pharmaceutical preparation technologies can enhance the bioavailability of poorly water-soluble drugs. Ursolic acid (UA) has been found to possess anti-cancer and hepatoprotective properties, demonstrating its potential as a therapeutic agent; however, its hydrophobicity and low solubility present challenges in the development of drug formulations. This study investigates the preparation of a nano-UA suspension by wet grinding, researches the influence of process parameters on particle size, and explores the rules of particle breakage and agglomeration by combining model fitting. Methods: Wet grinding experiments were conducted using a laboratory-scale grinding machine. The particle size distributions (PSDs) of UA suspensions under different grinding conditions were measured using a laser particle size analyzer. A single-factor experimental design was employed to optimize operational conditions. Model parameters for a population balance model considering both breakage and agglomeration were determined by an evolutionary algorithm optimization method. By measuring the degree to which UA inhibits the colorimetric reaction between salicylic acid and hydroxyl radicals, its antioxidant capacity in scavenging hydroxyl radicals was indirectly evaluated. Results: Wet grinding process conditions for nano-UA particles were established, yielding a UA suspension with a D50 particle size of 122 nm. The scavenging rate of the final grinding product was improved to three times higher than that of the UA raw material (D50 = 14.2 μm). Conclusions: Preparing nano-UA suspensions via wet grinding technology can significantly enhance their antioxidant properties. Model regression analysis of PSD data reveals that increasing the grinding mill’s stirring speed leads to more uniform particle size distribution, indicating that grinding speed (power) is a critical factor in producing nanosuspensions. Full article

The extensive use of submicron emulsion systems, particularly those stabilized by nonionic surfactants, with their proven effectiveness and safety profile, provides a reassuring foundation for our research. Consequently, we designed and engineered new submicron emulsion formulations stabilized with a biocompatible surfactant polyoxyethylated cocoamine, whose nonionic character is due to a high degree of polyoxyethylation. We chose oleic acid as the oil phase, a fatty acid known for its beneficial properties. This led to novel biocompatible nanoemulsions with high stability and cosurfactant-free microemulsions. The dynamic light scattering studies confirmed that both formulations have a nanometric size and low polydispersity index values. Moreover, transmission electron microscopy verified the nanodroplets’ morphological homogeneity and spherical shape. The resulting nanoplatforms can be applied to carry bioactive agents in the pharmaceutical and cosmetic fields. For this reason, we solubilized newly synthesized 5-dimethylamino-5′-nitro-2,2′-bithiophene as a model hydrophobic cargo for delivering poorly water-soluble compounds. This dye was chosen due to its strong solvatochromic behavior and suitability for micropolarity analysis via UV–Vis spectroscopy. We also present a simple method for rapid micropolarity screening to assess the type of nanodispersion via solvatochromic shift as an alternative procedure for evaluating of the oils used to fabricate nanoformulations for pharmaceutical and cosmetic purposes. Full article

A pyrimidine-based compound (PP) was recently found to be a promising anticancer agent for colorectal and breast cancers. However, this compound exhibited low selectivity and poor water solubility. To address these challenges, albumin gel nanoparticles were used, where the gel matrix is formed by cross-linking of BSA molecules, allowing for a high concentration of this hydrophobic drug to be carried with no cytotoxicity to non-tumor cells. Functionalization with hyaluronic acid (HA) was employed to target CD44-overexpressing cancer cells, specifically triple-negative breast cancer (MDA-MB-231) and colorectal cancer cell lines (HCT 116). The gel nanoparticles present mean sizes below 250 nm, very low polydispersity, small aggregation tendency, and excellent colloidal stability in PBS buffer for a storage period of 30 days. Moreover, the drug-loaded particles showed high encapsulation efficiencies (above 85%) and sustained release profiles. Drug-loaded BSA/HA particles (PP-HA-BSA-NPs) revealed advantageous activity, presenting around 55% and 23% cell viability at a IC₅₀ drug concentration for triple-negative breast cancer (the most aggressive breast cancer subtype) and colorectal cancer (second leading cause of cancer-related deaths), respectively. In conclusion, these nanoparticles outperform the ones without HA, demonstrating target capabilities, while retaining the drug’s anticancer activity and reducing the drug’s toxicity. These results are promising for future in vivo assays and clinical translational applications. Full article

The interfacial and foam properties of proteins can be enhanced by altering the interactions between polyphenols and proteins. The aim of this study was to determine the influence of gallic acid (GA) on the structural properties of whey protein isolate (WPI), specifically focusing on particle size, potential, and surface hydrophobicity, as well as the subsequent alterations in its interfacial and foam properties when utilized as a foaming agent. An increase in turbidity and a decrease in particle size suggested the formation of a soluble complex between GA and WPI at a pH of 6. The results from fluorescence spectroscopy and surface hydrophobicity analyses indicated that the primary interactions between GA and WPI are characterized by hydrogen bonding and hydrophobic interactions. The reduction in particle size enhances the capacity of WPI/GA complexes to lower the surface pressure, thereby demonstrating significant efficacy at the macroscopic scale. Furthermore, the structural connectivity of GA facilitates the formation of a stable interfacial film at the air–water interface by WPI/GA, resulting in high foam stability at a macroscopic level. This research contributes to a deeper understanding of the application of protein–polyphenol complexes as surfactants and provides theoretical support for their use in food applications. Full article

Delivering of hydrophobic drugs by polymeric nanoparticles is an intensively investigated research and development field worldwide due to the insufficient solubility of many existing and potential new drugs in aqueous media. Among polymeric nanoparticles, micelles of biocompatible amphiphilic block copolymers are among the most promising candidates for solubilization, encapsulation, and delivery of hydrophobic drugs to improve the water solubility and thus the bioavailability of such drugs. In this study, amphiphilic ABA triblock copolymers containing biocompatible hydrophilic hyperbranched (dendritic) polyglycerol (HbPG) outer and hydrophobic poly(tetrahydrofuran) (PTHF) inner segments were synthesized using amine-telechelic PTHF as a macroinitiator for glycidol polymerization. These hyperbranched–linear–hyperbranched block copolymers form nanosized micelles with 15–20 nm diameter above the critical micelle concentration. Coagulation experiments proved high colloidal stability of the aqueous micellar solutions of these block copolymers against temperature changes. The applicability of block copolymers as drug delivery systems was investigated using curcumin, a highly hydrophobic, water-insoluble, natural anti-cancer agent. High and efficient drug solubilization up to more than 3 orders of magnitude to that of the water solubility of curcumin (>1500-fold) is achieved with the HbPG-PTHF-HbPG block copolymer nanomicelles, locating the drug in amorphous form in the inner PTHF core. Outstanding stability of and sustained curcumin release from the drug-loaded block copolymer micelles were observed. The in vitro bioactivity of the curcumin-loaded nanomicelles was investigated on U-87 glioblastoma cell line, and an optimal triblock copolymer composition was found, which showed highly effective cellular uptake and no toxicity. These findings indicate that the HbPG-PTHF-HbPG triblock copolymers are promising candidates for advanced drug solubilization and delivery systems. Full article

This review examines the pharmaceutical applications of essential oils (EOs) and terpenes, highlighting their dual role as therapeutic agents and natural penetration enhancers. These volatile, hydrophobic compounds have well-documented antimicrobial, antioxidant, and anti-inflammatory properties. However, their clinical potential is limited by poor water solubility, high volatility, and sensitivity to environmental factors, including light, heat, and oxygen. To address these challenges, various advanced delivery systems have been developed to enhance stability, bioavailability, and controlled release. These systems not only protect chemical integrity but also exploit these compounds’ abilities to interact with lipid membranes, facilitating the transport of active compounds across biological barriers. Additionally, their inherent antimicrobial properties can contribute to the overall stability of formulations. The review critically examines the incorporation of terpenes and major essential oil (EO) components, such as limonene, linalool, eugenol, α-pinene, and menthol, into delivery systems, assessing their performance in enhancing drug permeability and targeting specific tissues. Current challenges and future directions in terpenes and EO-based delivery strategies are discussed, highlighting their promising role in developing multifunctional and efficient pharmaceutical formulations. Full article

Background: Nutraceuticals represent a strategy for maintaining health and constitute a brilliant market in Italy and across Europe. However, the absence of strict regulations regarding formulation requirements highlights a critical issue: their poor bioavailability. An example is coenzyme Q10 (CoQ10), a quinone known for its potential as a mitochondrial protective agent but characterized by low intestinal absorption. CoQ10 is a hydrophobic molecule with high molecular weight and poor water solubility, factors that significantly limit its intestinal bioaccessibility and, consequently, its oral bioavailability. Objectives: In this context, the present study describes a novel formulation designed to enhance CoQ10 bioaccessibility through in situ emulsification upon contact with gastroenteric fluids. This technology, termed Lipid-Based Auto-Emulsifying Drug Delivery System (LiBADDS), is unique because it combines a medium-chain triglyceride (MCT), a long-chain fatty acid, conjugated linoleic acid (CLA) with a high HLB solubilizer, Polysorbate 80 (PS80), and a sodium octenyl succinate starch derivative (SOS), which can create a nanometric emulsion simply by aqueous dispersion and upon contact with gastrointestinal fluids. This phenomenon promotes the prompt dispersion of CoQ10 and its rapid translocation into the serosal compartment of the intestinal epithelium. Methods: Its efficacy was evaluated in vitro through the Caco-2 cellular model and in vivo through a crossover study on healthy volunteers, measuring pharmacokinetic parameters such as AUC, C_max, T_max, ΔAUC, and ΔC_max. Results: Overall, LiBADDS demonstrated a significant improvement in both the bioaccessibility and bioavailability of CoQ10 compared to the unformulated substance. Conclusions: LiBADDS showed to be a promising tool to improve CoQ10 bioavailability by enhancing its bioaccessibility. Full article

This study explores an innovative topical formulation to treat alopecia by encapsulating cannabidiol (CBD) in chitosan nanoparticles. CBD, widely known for its anti-inflammatory, antioxidant, and endocannabinoid-modulating effects, shows significant potential for treating alopecia, a condition characterized by hair loss influenced by genetic, hormonal, or environmental factors. However, its low water solubility presents a significant challenge for topical applications. To address this issue, chitosan nanoparticles were synthesized using chitosan of reduced molecular mass (270 kDa) with an acetylation level of 12%, β-glycerophosphate as a crosslinking agent, and 1% glycerol to improve CBD encapsulation efficiency. Physicochemical characterization using scanning electron microscopy (SEM), zeta potential measurement, and Fourier transform infrared spectroscopy (FTIR) revealed that the β-glycerophosphate concentration impacted nanoparticle size and the electrostatic interactions between chitosan’s primary amines and phosphate groups of β-glycerophosphate. Among the tested concentrations (0.05, 0.1, 0.2, and 0.25 mol/L), 0.20 mol/L produced the smallest nanoparticles (390 nm), which were further optimized to encapsulate CBD, reaching a particle size of 227 nm. This optimized formulation may improve the solubility of CBD and enable targeted and sustained delivery to hair follicles. These findings highlight chitosan nanoparticles as a cutting-edge and scalable platform for transdermal delivery of hydrophobic bioactive compounds, presenting a promising approach for the effective management of alopecia. Full article

The aim of this research was to examine the effect of water-based hydrophobic impregnations on concrete in order to improve its durability, chemical resistance, and physical–mechanical parameters. The purpose of this research was to prevent as much water evaporation as possible during concrete hydration, which resulted in the improvement in concrete properties including strength, durability, resistance of concrete in high-pressure water, water tightness, etc. Water-based hydrophobic impregnations based on silane and siloxane, epoxy resin, and oil were chosen to achieve improvements in concrete parameters. The comparison of water-based hydrophobic impregnations with solvent-based hydrophobic impregnations was also performed using the determination of absorbency, water pressure penetration depth, watertightness, concrete penetration depth, and resistance to aggressive environment. The concrete microstructure was observed using a digital microscope and a scanning electron microscope (SEM). Samples with hydrophobic agents exhibited a higher contact angle, lower absorbency, and higher resistance to aggressive environment, when compared to the untreated surfaces, confirming the water repellency of the water-soluble hydrophobic impregnations. The positive effect of hydrophobic agents in the compressive strength was also recorded. Furthermore, the benefit of the addition of 0.1 wt.% of nanocellulose into the hydrophobic impregnations was observed. Based on the obtained results, it was found that the addition of nanocellulose to water-soluble hydrophobic impregnations reduced the depth of pressurized water seepage and increased the compressive strength of the concrete after 28 days by 2 MPa. Full article

Whey protein isolate (WPI) has functional properties such as gelation and emulsification. Emulsion gels combine the benefits of both emulsions and hydrogels. In this study, WPI hydrogels and emulsion gels were developed with goji oil (GO) as the oil phase by the inclusion of blueberry extract (BE) in the protein matrix. Heat-denatured WPI (hWPI) particles and emulsions were characterized in terms of size distribution, ζ-potential, interfacial protein, and anthocyanin partition. The inclusion of anthocyanins-rich blueberry extract led to the aggregation of hWPI particles, but it also increased the interfacial protein of 10% goji oil emulsions to 20% and decreased their size distribution to 120 and 325 nm. WPI hydrogels and emulsion gels were analyzed in terms of their water-holding capacity, which decreased from 98% to 82% with the addition of blueberry extract and goji oil. Syneresis, rheological, and morphological characteristics were also analyzed. The gelation time of hWPI particles and emulsions was shortened from 24 h to 12 h when incorporating blueberry extract to form a dense network. The network was the most homogeneous and densest in the presence of 3% blueberry extract and 5% goji oil. The co-inclusion of blueberry extract and goji oil increased the syneresis during the freeze–thaw cycles, with the values rising from 13% to 36% for 5% BE hydrogel and BE-containing emulsion gels after the first cycle. All WPI hydrogels and emulsion gels exhibit predominantly elastic behavior. Moreover, anthocyanin release, antioxidant activity, and the fatty acid composition profile were also analyzed during in vitro digestion. Soluble and free anthocyanins in the digested medium were reduced with the goji oil content but increased with the blueberry extract content. The stability of polyunsaturated fatty acids in the digested medium was improved by the addition of blueberry extract. The antioxidant activity of the digested medium increased with the content of blueberry extract but decreased with the content of goji oil. The ABTS^∙+ scavenging capacities decreased from 63% to 49% by increasing the content of GO from 0% to 10% and they increased from 48% to 57% for 5% BE and 10% GO emulsion gels as the BE content increased from 0% to 5% after 6 h of digestion. The data gathered should provide valuable insights for future efforts to co-encapsulate hydrophilic and hydrophobic agents, thereby enhancing their stability, bioavailability, and functional properties for potential applications in food industries. Full article

In this study, the use of surfactant-free water-in-oil gelled emulsions containing benzyl alcohol (BAl/w) is proposed as an alternative to the more traditional use of organic solvents for removing varnishes. To mitigate the strong swelling and solvent action of benzyl alcohol and protect the paint and the underlying layers, temporary hydrophobization with cyclomethicone D5 has been proposed. The aim of this study was to evaluate the application of BAl/w surfactant-free, constructed with three different gelling agents of the aqueous dispersing phase (xanthan gum, agar-agar, and polyacrylate) on the surface of an oil painting varnished with and without preliminary saturation with D5. The role of pH, which can influence the ionization, and therefore the water solubility of terpene molecules and all other acid species present on the surface, was also studied. Fourier transform infrared (FT-IR) and Raman spectroscopies were used to characterize the pigments and the surface before and after varnish removal. Elemental analysis and any morphological changes were evaluated using scanning electron microscopy coupled with energy-dispersive X-ray spectroscopy (SEM-EDS). The leaching efficiency of each surfactant-free emulsion applied on the paint surface was evaluated using a gas chromatography/mass spectroscopy (GC/MS) analysis: the fatty acid content was established in each sample before and after the treatments. Full article

As a promising polymer for the production of biomaterials and drug delivery systems, poly(lactic acid) (PLA) is characterized by its relative hydrophobicity, as well as its chemical and biological inertness. Here, we aimed to improve the biological properties of PLA-based materials via the covalent attachment of a hydrophilic biocompatible glycopolymer, namely poly(2-deoxy-N-methacrylamido-D-glucose) (PMAG) on their surface. PMAG is a water-soluble polymer that contains glucose units in its side chains, which are responsible for good biocompatibility and the ability to attach bioactive molecules. In the developed protocol, PMAG was synthesized by controlled radical polymerization in the presence of a reversible addition–fragmentation chain transfer (RAFT) agent, followed by the conversion of glycopolymer terminal dithiobenzoate functionality into a primary amino group (PMAG-NH₂). PLA-based films served as model aliphatic polyester materials for developing the surface biofunctionalization protocol. According to that, PMAG-NH₂ covalent immobilization was carried out after alkali treatment, allowing the generation of the surface-located carboxyl groups and their activation. The developed modification method provided a one-point attachment of hydrophilic PMAG to the hydrophobic PLA surface. PMAG samples, which differed by the degree of polymerization, and the variation of polymer concentration in the reaction medium were applied to investigate the modification efficacy and grafting density. The developed single-point polymer grafting approach provided the efficient functionalization with a grafting density in the range of 5–23 nmol/cm². The neat and modified polymer films were characterized by a number of methods, namely atomic force microscopy, thermogravimetric analysis, ellipsometry, and contact angle measurements. In addition, an ArgGlyAsp-containing peptide (RGD peptide) was conjugated to the PMAG macromolecules grafted on the surface of PLA films. It was shown that both surface modification with PMAG and with PMAG-RGD peptide enhanced the adhesion and growth of mesenchymal stem cells as compared to a neat PLA surface. Full article