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This study explores the development and characterization of lyophilized chondroitin sulfate (CHON)-loaded solid lipid nanoparticles (SLN) as an innovative platform for advanced drug delivery. Background/Objectives: Solid lipid nanoparticles are increasingly recognized for their biocompatibility, their ability to encapsulate diverse compounds, their capacity to enhance drug stability, their bioavailability, and their therapeutic efficacy. Methods: CHON, a naturally occurring glycosaminoglycan with anti-inflammatory and regenerative properties, was integrated into SLN formulations using the hot microemulsion technique. Two formulations (SLN-1 and SLN-2) were produced and optimized by evaluating critical physicochemical properties such as particle size, zeta potential, encapsulation efficiency (EE%), and stability. The lyophilization process, with the addition of various cryoprotectants, revealed trehalose to be the most effective agent in maintaining nanoparticle integrity and functional properties. Results: Morphological analyses using transmission electron microscopy (TEM) and atomic force microscopy (AFM) confirmed the dimensions of the nanoscales and their structural uniformity. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) revealed minimal excipient interaction with CHON, ensuring formulation stability. Stability studies under different environmental conditions highlighted that SLN-2 is the most stable formulation, maintaining superior encapsulation efficiency (≥88%) and particle size consistency over time. Conclusions: These findings underscore the potential of CHON-loaded SLNs as promising candidates for targeted, sustained-release therapies in the treatment of inflammatory and degenerative diseases. [ABSTRACT FROM AUTHOR]

Curcumin is utilized extensively as Chinese medicine in Asia due to its antioxidant, antimicrobial, and inflammatory activities. However, its use has the challenges of low oral bioavailability and high heat sensitivity. The aim of this research was to produce flexible nano-liposomes containing curcumin using an innovative approach of ethanol injection and Tween 80 to enhance the stability and preservation of curcumin. The mean particle size, encapsulation efficiency, thermal degradation, storage stability, and curcumin release in flexible nano-liposomes were also investigated. We found that the mean particle size of curcumin-loaded flexible nano-liposome decreased from 278 nm to 27.6 nm. At the same time, the Tween 80 concentration increased from 0 to 0.15 wt%, which corresponded with the results of transmission electron microscopy (TEM) morphology analyses, and particle size decreased with an enhancement in Tween 80 concentration. Further, pure curcumin was quickly released within one hour at 37 °C, and first-order kinetics matched with its release curve. However, curcumin encapsulated in flexible nano-liposomes showed a slow release of 71.24% within 12 h, and a slower release pattern matched with the Higuchi model over 24 h, ultimately reaching 84.63% release. Hence, flexible nano-liposomes of curcumin made by a combination of ethanol injection and Tween 80 addition prevented the thermal degradation of curcumin, and enhanced its storage stability and preservation for future drug delivery applications. [ABSTRACT FROM AUTHOR]

Fertilizers that release nutrients slowly can provide crops with consistent nutrients, while soils with good water-holding capacity can alleviate the impact of droughts on crops. Sodium alginate/carboxymethyl starch sodium/polydopamine/urea (SCPU) is a new kind of slow-release fertilizer with water absorption property. In this study, the Box–Behnken response surface methodology (RSM) was used to reveal the effects of concentrations of sodium alginate, carboxymethyl starch sodium, urea, calcium chloride and dopamine on the encapsulation efficiency and water absorption of SCPU. The results show that the optimum preparation conditions to obtain the highest level of encapsulation efficiency (89.27%) and water absorption (167.05%) are 2.2% sodium alginate, 5% carboxymethyl starch sodium, 30% urea, 1.9% calcium chloride and 0.52% dopamine. [ABSTRACT FROM AUTHOR]

The current work is devoted to the development of probiotic microencapsulation systems with the co-encapsulation of a plant extract, which can increase the survival of beneficial bacteria and are suitable for potential applications in the enrichment of fermented beverages based on acid whey. The encapsulation process exhibited a high level of effectiveness, achieving 83.0% for Bifidobacterium (BB), 89.2% for Stevia leaf extract (SE), and 91.3% for their combination (BB + SE). The FTIR analysis verified substantial interactions between the encapsulated agents and the polymer matrix, which enhanced the stability of the microcapsules. The BB + SE microcapsules exhibited reduced swelling and moisture content, indicating a denser structure compared to separately encapsulated BB and SE. Comparison of release kinetics of BB, SE and BB + SE loaded microcapsules showed that the combination of active agents has a quicker initial release, reaching 60% release within the first 2 h, and this value increased to 70% after 4 h. The release kinetics studies demonstrated a controlled release of active substances over 24 h. A morphology analysis shows that the surfaces of the dry microcapsules containing BB, SE, and their combination BB + SE have a porous structure. For encapsulated agents, the size of the capsules produced with BB and SE are smaller than those produced with two components (BB + SE), the sizes of which are between 760 µm and 1.1 mm. Modeling of the behavior of microcapsules in a simulated gastrointestinal tract provides information on swelling and active agents release rates as a function of pH in real biological environments. Thus, the new formulations of microcapsules with microorganisms and plant extracts have great potential for the development of fermented whey-based beverages. [ABSTRACT FROM AUTHOR]

The excessive use of biocides has considerable environmental and economic impacts; this is why new technologies have been sought to decrease the concentration levels applied in an effort to reduce the use of these substances. Microencapsulation using cyclodextrins has been widely used in the food and pharmaceutical industries as a way of reducing the concentrations of the active substance necessary to achieve a biological effect and/or eliminate its irritating or toxicological effects. In this study, the inclusion complexation behavior and binding ability of benzothiazolinone (BIT) with different β-cyclodextrins (β-CD, HP-β-CD, and Me-β-CD) was investigated. The intermolecular interactions were examined through UV and FTIR spectroscopy, DSC, 1D 1H NMR, and 2D ROESY. The highest stability constant was observed for the BIT/Me-β-CD inclusion complex (299.5 ± 2.9 M−1). Antibacterial activity was investigated against Staphylococcus aureus and Escherichia coli, and the results revealed that the BIT/Me-β-CD inclusion complex displays a higher antibacterial activity than BIT. The acute toxicity of the biocide and inclusion complex was also examined using the photobacterium Aliivibrio fischeri. Although BIT exhibited higher toxicity than the inclusion complex, further investigation is needed due to the quorum quenching effect of β-CDs. The data found suggest that BIT microencapsulation can increase its aqueous solubility and can be used as an effective tool to improve its chemical, biological, and ecotoxicological properties. [ABSTRACT FROM AUTHOR]

The aim of the study was to compare two kinds of soluble dietary fibres in a mixture with OSA-starch as wall components of linseed oil capsules. Comparison was made based on emulsion (droplet size, polydispersity index, and viscosity) and powder properties (outer structure, colour, surface oil content, and encapsulation efficiency). Additionally, linseed oil powders were applied to the food model (apple juice) and the colour, physical stability, and volatile compound profile of fortified juice were determined. Although the obtained linseed oil emulsions with different compositions of polysaccharide components showed some variation in droplet size, polydisperse index and viscosity, their encapsulation efficiency by spray-drying was very high (>98%). The powders produced had a similar structure and low surface oil content, and their 2% addition to apple juice did not change its stability and only slightly decreased its colour lightness and yellowness. However, greater differences in the volatile compounds of obtained juices were observed. Overall, the added powders reduced the volatility of aroma compounds typical of apple juice but introduced propanal and hexanal, especially the powders with the highest OSA-starch share. [ABSTRACT FROM AUTHOR]

RNA-based therapeutics, including siRNA, have obtained recognition in recent years due to their potential to treat various chronic and rare diseases. However, there are still limitations to lipid-based drug delivery systems in the clinical use of RNA therapeutics due to the need for optimization in the design and the preparation process. In this study, we propose adaptive focused ultrasound (AFU) as a drug loading technique to protect RNA from degradation by encapsulating small RNA in nanoliposomes, which we term nanoplexes. The AFU method is non-invasive and isothermal, as nanoplexes are produced without direct contact with any external materials while maintaining precise temperature control according to the desired settings. The controllability of sample treatments can be effectively modulated, allowing for a wide range of ultrasound intensities to be applied. Importantly, the absence of co-solvents in the process eliminates the need for additional substances, thereby minimizing the potential for cross-contaminations. Since AFU is a non-invasive method, the entire process can be conducted under sterile conditions. A minimal volume (300 μL) is required for this process, and the treatment is speedy (10 min in this study). Our in vitro experiments with silencer CD44 siRNA, which performs as a model therapeutic drug in different mammalian cell lines, showed encouraging results (knockdown > 80%). To quantify gene silencing efficacy, we employed quantitative polymerase chain reaction (qPCR). Additionally, cryo-electron microscopy (cryo-EM) and atomic force microscopy (AFM) techniques were employed to capture images of nanoplexes. These images revealed the presence of individual nanoparticles measuring approximately 100–200 nm in contrast with the random distribution of clustered complexes observed in ultrasound-untreated samples of liposome nanoparticles and siRNA. AFU holds great potential as a standardized liposome processing and loading method because its process is fast, sterile, and does not require additional solvents. [ABSTRACT FROM AUTHOR]

Multiple emulsions can dissolve some substances with different properties, such as hydrophilicity and lipophilicity, into different phases. They play an important role in protection, controlled release and targeted release of the encapsulated substances. However, it's poor stability has always been one of the main problems restricting its application in the food industry. For this reason, a heat-induced aggregate (HIA) of Maillard graft product of isomalto-oligosaccharides (IMO), as well as egg white protein (EWP), was used as hydrophilic emulsifier to improve the stability of W1/O/W2 emulsions. Moreover, gelatin was added into the internal aqueous phase (W1) to construct W1/O/W2 emulsion-gels system. The encapsulation efficiency of HIA-stabilized W1/O/W2 emulsions remained nearly unaltered, dropping by only 0.86%, significantly outperforming the conjugates and physical mixture of IMO and EWP in terms of encapsulation stability. The emulsion-gels system was constructed by adding 5% gelatin in the W1, and had the highest EE% and good salt and heat stability after 30 days of storage. This experiment provides guidance for improving the stability of W1/O/W2 emulsions system and its application in the package delivery of functional substances in the food field. [ABSTRACT FROM AUTHOR]

Nanoemulsions are gaining interest in a variety of products as a means of integrating easily degradable bioactive compounds, preserving them from oxidation, and increasing their bioavailability. However, preparing stable emulsion compositions with the desired characteristics is a difficult task. The aim of this study was to encapsulate the Tinospora cordifolia aqueous extract (TCAE) into a water in oil (W/O) nanoemulsion and identify its critical process and formulation variables, like oil (27–29.4 mL), the surfactant concentration (0.6–3 mL), and sonication amplitude (40% to 100%), using response surface methodology (RSM). The responses of this formulation were studied with an analysis of the particle size (PS), free fatty acids (FFAs), and encapsulation efficiency (EE). In between, we have studied a fishbone diagram that was used to measure risk and preliminary research. The optimized condition for the formation of a stable nanoemulsion using quality by design was surfactant (2.43 mL), oil concentration (27.61 mL), and sonication amplitude (88.6%), providing a PS of 171.62 nm, FFA content of 0.86 meq/kg oil and viscosity of 0.597 Pa.s for the blank sample compared to the enriched TCAE nanoemulsion with a PS of 243.60 nm, FFA content of 0.27 meq/kg oil and viscosity of 0.22 Pa.s. The EE increases with increasing concentrations of TCAE, from 56.88% to 85.45%. The RSM response demonstrated that both composition variables had a considerable impact on the properties of the W/O nanoemulsion. Furthermore, after the storage time, the enriched TCAE nanoemulsion showed better stability over the blank nanoemulsion, specially the FFAs, and the blank increased from 0.142 to 1.22 meq/kg oil, while TCAE showed 0.266 to 0.82 meq/kg. [ABSTRACT FROM AUTHOR]

Curcumin is an antioxidant that can effectively eliminate free radicals. However, as its oral bioavailability is low, an effective delivery method is required. Phospholipid-based liposomes can encapsulate lipophilic drugs, such as curcumin, while liposome, cholesterol, and gum Arabic (GA) can enhance the internal and external stability of drug membranes. This present study used concentrations of cholesterol (Cchol) and GA (CGA), ranging from 0 to 10, 20, 30, and 40% as well as 0 to 5, 10, 15, 20, 30, and 40%, respectively, to encapsulate curcumin in a GA–cocoliposome (CCL/GA) matrix and test its efficacy in simulated intestinal fluid (SIF) and simulated gastric fluid (SGF). The absence of new characteristic peaks in the Fourier transform infrared (FTIR) spectra results indicate the presence of non-covalent interactions in the CCL/GA encapsulation. Furthermore, increasing the Cchol decreased the encapsulation efficiency (EE), loading capacity (LC), and antioxidant activity (IR) of the CCL/GA encapsulation but increased its release rate (RR). Conversely, increasing CGA increased its EE and IR but decreased its LC and RR. The two conditions applied confirmed this. Liposomal curcumin had the highest IR in SIF (84.081%) and the highest RR in SGF (0.657 ppm/day). Furthermore, liposomes loaded with 10% Cchol and 20% CGA performed best in SIF, while those loaded with 10% Cchol and 30% CGA performed best in SGF. Lastly, the CCL/GA performed better in SIF than SGF. [ABSTRACT FROM AUTHOR]

In response to environmental issues, upcycling has become a growing trend in the food industry. Aquasoya is a promising method to upcycle by-product from soybean processing due to its high protein contents and excellent emulsifying ability. In the present research, Aquasoya powder was used an emulsifier to incorporate the antioxidant compounds from perilla skin extract (PSE), namely rosmarinic acid, into oil-in-water (O/W) emulsion system and its physochemical stability was assessed. As a result, droplet size of the emulsion was smaller in PSE-incorporated emulsion (PO, 350.57 ± 9.60 b nm) than the emulsion without PSE (PX, 1045.37 ± 142.63 a nm). Centrifugal photosedimentometry analysis also revealed that the physical stability was significantly improved in PO, and the stability was maintained over 30 d of storage. Furthermore, as PO had a higher ABTS radical scavenging ability and showed slower initial lipid oxidation, it was concluded that PO has a higher antioxidant ability than PX. Conclusively, Aquasoya can be considered as an emulsifier in O/W emulsion with PSE because it can effectively integrate and stabilize the antioxidant substance derived from perilla skin. [ABSTRACT FROM AUTHOR]

In this study, protein-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres were prepared via supercritical fluid extraction of emulsion (SFEE) technology. To understand the correlation between process parameters and the main quality characteristics of PLGA microspheres, a comprehensive prior study on the influence of process variables on encapsulation efficiency (EE), initial drug burst release (IBR), morphology, surface property, and particle size distribution (PSD) was conducted within a wide process condition range of each unit process step, from the double-emulsion preparation step to the extraction step. Bovine serum albumin (BSA), a high-molecular weight-protein that is difficult to control the IBR and EE of PLGA microspheres with, was used as a model material. As double-emulsion manufacturing process parameters, the primary (W/O) and secondary emulsion (W/O/W) homogenization speed and secondary emulsification time were evaluated. In addition, the effect of the SFEE process parameters, including the pressure (70–160 bar), temperature (35–65 °C), stirring rate (50–1000 rpm), and flow rate of supercritical carbon dioxide, SC-CO2 (1–40 mL/min), on PLGA microsphere quality properties were also evaluated. An increase in the homogenization speed of the primary emulsion resulted in an increase in EE and a decrease in IBR. In contrast, increasing the secondary emulsification speed resulted in a decrease in EE and an increase in IBR along with a decrease in microsphere size. The insufficient secondary emulsification time resulted in excessive increases in particle size, and excessive durations resulted in decreased EE and increased IBR. Increasing the temperature and pressure of SFEE resulted in an overall increase in particle size, a decrease in EE, and an increase in IBR. It was observed that, at low stirring rates or SC-CO2 flow rates, there was an increase in particle size and SPAN value, while the EE decreased. Overall, when the EE of the prepared microspheres is low, a higher proportion of drugs is distributed on the external surface of the microspheres, resulting in a larger IBR. In conclusion, this study contributes to the scientific understanding of the influence of SFEE process variables on PLGA microspheres. [ABSTRACT FROM AUTHOR]

Lactic acid bacteria (LAB) constitute the microbial group most used as probiotics; however, many strains reduce their viability during their transit through the body. The objective of this study was to evaluate the effect of two microencapsulation techniques, as well as the incorporation of lactulose as a prebiotic and the use of chitosan coating on the microcapsules, on the viability of the Lactobacillus sp. strain FM4.C1.2. LAB were microencapsulated by extrusion or emulsion, using 2% sodium alginate as encapsulating matrix and lactulose (2 or 4%) as the prebiotic. The encapsulation efficiency was evaluated, and the capsules were measured for moisture and size. The encapsulation efficiency ranged between 80.64 and 99.32% for both techniques, with capsule sizes between 140.64 and 1465.65 µm and moisture contents from 88.23 to 98.04%. The microcapsules of some selected treatments (five) were later coated with chitosan and LAB survival was evaluated both in coated and uncoated microcapsules, through tolerance to pH 2.5, bile salts and storage for 15 days at 4 °C. The highest survival of the probiotic strain under the conditions of pH 2.5 (96.78–99.2%), bile salts (95.54%) and storage for 15 days (84.26%), was found in the microcapsules obtained by emulsion containing 4% lactulose and coated with chitosan. These results demonstrate the possible interaction of lactulose with alginate to form better encapsulating networks, beyond its sole probiotic effect. Additional research may shed more light on this hypothesis. [ABSTRACT FROM AUTHOR]

This study reports the interfacial phenomenon of cefotaxime in combination with nonionic surfactants, Triton X-100 (TX-100) and Tween-80 (TW-80), and their mixed micellar formulations. Cefotaxime was enclosed in a micellar system to improve its solubility and effectiveness. TX-100 and TW-80 were used in an amphiphilic self-assembly process to create the micellar formulation. The effect of the addition of TX-100, a nonionic surfactant, on the ability of TW-80 to solubilize the drug was examined. The values of the critical micelle concentration (CMC) were determined via UV-Visible spectroscopy. Gibbs free energies (ΔGp and ΔGb), the partition coefficient (Kx), and the binding constant (Kb) were also computed. In a single micellar system, the partition coefficient (Kx) was found to be 33.78 × 106 and 2.78 × 106 in the presence of TX-100 and TW-80, respectively. In a mixed micellar system, the value of the partition coefficient for the CEF/TW-80 system is maximum (5.48 × 106) in the presence of 0.0019 mM of TX-100, which shows that TX-100 significantly enhances the solubilizing power of micelles. It has been demonstrated that these surfactants are effective in enhancing the solubility and bioavailability of therapeutic compounds. This study elaborates on the physicochemical characteristics and solubilization of reactive drugs in single and mixed micellar media. This investigation, conducted in the presence of surfactants, shows a large contribution to the binding process via both hydrogen bonding and hydrophobic interactions. [ABSTRACT FROM AUTHOR]

Liposomes are self-assembled spherical systems composed of amphiphilic phospholipids. They can be used as carriers of both hydrophobic and hydrophilic substances, such as the anti-aging and wound-healing copper-binding peptide, GHK-Cu (glycyl-L-histidyl-L-lysine). Anionic (AL) and cationic (CL) hydrogenated lecithin-based liposomes were obtained as GHK-Cu skin delivery systems using the thin-film hydration method combined with freeze–thaw cycles and the extrusion process. The influence of total lipid content, lipid composition and GHK-Cu concentration on the physicochemical properties of liposomes was studied. The lipid bilayer fluidity and the peptide encapsulation efficiency (EE) were also determined. Moreover, in vitro assays of tyrosinase and elastase inhibition were performed. Stable GHK-Cu-loaded liposome systems of small sizes (approx. 100 nm) were obtained. The bilayer fluidity was higher in the case of cationic liposomes. As the best carriers, 25 mg/cm3 CL and AL hydrated with 0.5 mg/cm3 GHK-Cu were selected with EE of 31.7 ± 0.9% and 20.0 ± 2.8%, respectively. The obtained results confirmed that the liposomes can be used as carriers for biomimetic peptides such as copper-binding peptide and that the GHK-Cu did not significantly affect the tyrosinase activity but led to 48.90 ± 2.50% elastase inhibition, thus reducing the rate of elastin degeneration and supporting the structural integrity of the skin. [ABSTRACT FROM AUTHOR]

Background: The use of conventional astaxanthin extraction methods, typically involving organic solvents, leads to a heightened environmental impact. The aim of this study was to explore the potential use of environmentally friendly extraction solvents, such as vegetable oils, for recovering the shrimp by-product astaxanthin. Methods: Ultrasound-assisted extraction (UAE) in vegetable oils, including olive oil (OO), sunflower oil (SO), and flaxseed oil (FO), was employed to extract astaxanthin. The astaxanthin antioxidant activity was evaluated using an ABTS assay, and a mixture of gum Arabic and soy lecithin was used to form coacervates to produce astaxanthin encapsulation. Results: A by-product–vegetable oil ratio of 1:60, extraction time of 210 min, 60% amplitude of the extraction process, and the use of OO as the extracting medium resulted in an astaxanthin yield of 235 ± 4.07 μg astaxanthin/g by-products. The astaxanthin encapsulation efficiency on day 0 and astaxanthin recovery on day 1 were recorded at 66.6 ± 2.7% and 94.4 ± 4.6%, respectively. Conclusions: The utilization of OO as an extraction solvent for astaxanthin from shrimp by-products in UAE represents a novel and promising approach to reducing the environmental impact of shrimp by-products. The effective astaxanthin encapsulation efficiency highlights its potential application in food industries. [ABSTRACT FROM AUTHOR]

The use of the appropriate emulsifier is essential for forming a stable nanoemulsion delivery system that can maintain the sustained release of its contents. Health concerns have prompted the search for natural biopolymers to replace traditional synthetic substances as emulsifiers. In this study, an oregano essential oil (OEO) nanoemulsion-embedding system was created using soybean protein isolate (SPI), tea saponin (TS), and soy lecithin (SL) as natural emulsifiers and then compared to a system created using a synthetic emulsifier (Tween 80). The results showed that 4% Tween 80, 1% SPI, 2% TS, and 4% SL were the optimal conditions. Subsequently, the influence of emulsifier type on nanoemulsion stability was evaluated. The results revealed that among all the nanoemulsions, the TS nanoemulsion exhibited excellent centrifugal stability, storage stability, and oxidative stability and maintained high stability and encapsulation efficiency, even under relatively extreme environmental conditions. The good stability of the TS nanoemulsion may be due to the strong electrostatic repulsion generated by TS molecules, which contain hydroxyl groups, sapogenins, and saccharides in their structures. Overall, the natural emulsifiers used in our study can form homogeneous nanoemulsions, but their effectiveness and stability differ considerably. [ABSTRACT FROM AUTHOR]

The marketed drug Doxorubicin (DOX) and the promising anti-cancer agent 9-(N-piperazinyl)-5-methyl-12(H)-quino[3,4-b][1,4]benzothiazinium chloride (9-PBThACl) were used to prepare and compare a range of liposomal delivery systems based on dipalmitoylphosphatidylcholine (DPPC). Liposome-assisted drug release was examined using the spectrophotometric method. In order to provide in vitro release characteristics of liposomal conjugates (LDPPC/drug vs. LDPPC/drug/drug) as well as to evaluate the impact of temperature and pH buffering on the conformation/polarity of the phospholipid bilayer, the encapsulation efficiency of the liposomes entrapping 9-PBThACl and DOX was calculated. In fact, some competition between the investigated molecules was noticed during the entrapment process because relatively high values of the encapsulation efficiency were observed only for the liposomal complexes containing one trapped drug molecule. An averaged absorbance value enabled us to indicate the pH value of the environment (pH ≈ 6.8), at which the physicochemical property profiles of the liposomal complexes were noticeably changed. Moreover, the operational factors limiting the drug release kinetics from the produced liposomes were mathematically modeled. First-order and Bhaskas models ensured satisfactory compliance with the experimental data for the liposomal complexes buffered at pH values of 5.50, 6.00, and 7.40, respectively. [ABSTRACT FROM AUTHOR]

Curcumin (Cur) is a beneficial phytochemical with numerous health advantages. However, its limited solubility in oil and poor stability hinder its potential for biomedical applications. In this study, we employed a mixture of food-grade Tween 60, a polymeric surfactant, and Span 60 to adjust the hydrophilic lipophilic balance number (HLBt) and prepared nanoemulsions (NEs) of coconut oil (Cc oil) as carriers for Cur. The effects of HLBt values, surfactant-to-oil ratio, and oil ratio on the physicochemical characteristics of the food-grade oil-NEs were investigated using dynamic light scattering, transmission electron microscopy, differential scanning calorimetry, fluorescence polarization spectroscopy, and viscometry. Increasing the addition ratio of Tween 60 in the NEs, thereby increasing the HLBt, resulted in a reduction in NE size and an improvement in their storage stability. The temperature and size of the phase transition region of the NEs decreased with increasing HLBt. NEs with higher HLBt exhibited a disordering effect on the intra-NE molecular packing of Cc oil. NEs with high HLBt displayed low viscosity and demonstrated nearly Newtonian fluid behavior, while those with lower HLBt exhibited pseudoplastic fluid behavior. Cur was effectively encapsulated into the Cc oil-NEs, with higher encapsulation efficiency observed in NEs with higher HLBt values. Furthermore, the Cur remaining activity was significantly enhanced through encapsulation within stable NEs. The biocompatibility of the Cc oil-NEs was also demonstrated in vitro. In summary, this study highlights the preparation of stable NEs of Cc oil by adjusting the HLBt using Tween 60, facilitating effective encapsulation of Cur. These findings provide valuable insights for the development of Cur carriers with improved solubility, stability, and bioavailability. [ABSTRACT FROM AUTHOR]

Spray-drying is a continuous encapsulation method that effectively preserves, stabilizes, and retards the degradation of bioactive compounds by encapsulating them within a wall material. The resulting capsules exhibit diverse characteristics influenced by factors such as operating conditions (e.g., air temperature and feed rate) and the interactions between the bioactive compounds and the wall material. This review aims to compile recent research (within the past 5 years) on spray-drying for bioactive compound encapsulation, emphasizing the significance of wall materials in spray-drying and their impact on encapsulation yield, efficiency, and capsule morphology. [ABSTRACT FROM AUTHOR]

Novel lipid-based nanosystems have been of interest in improving conventional drug release methods. Liposomes are the most studied nanostructures, consisting of lipid bilayers ideal for drug delivery, thanks to their resemblance to the cell plasma membrane. Asymmetric liposomes are vesicles with different lipids in their inner and outer layers; because of this, they can be configured to be compatible with the therapeutic drug while achieving biocompatibility and stability. Throughout this review, topics such as the applications, advantages, and synthesis techniques of asymmetric liposomes will be discussed. Further, an in silico analysis by computational tools will be examined as a helpful tool for designing and understanding asymmetric liposome mechanisms in pharmaceutical applications. The dual-engineered design of asymmetric liposomes makes them an ideal alternative for transdermal drug delivery because of the improved protection of pharmaceuticals without lowering adsorption rates and system biocompatibility. [ABSTRACT FROM AUTHOR]

Background: The Box–Behnken design of experiments (BBD) is a statistical modelling technique that allows the determination of the significant factors in developing nanoparticles (NPs) using a limited number of runs. It also allows the prediction of the best levels of variables to obtain the desired characteristics (size, charge, and encapsulation efficiency) of the NPs. The aim of this study was to examine the effect of the independent variables (amount of polymer and drug, and surfactant concentration) and their interaction on the characteristics of the irinotecan hydrochloride (IRH)-loaded polycaprolactone (PCL) NPs and to determine the most optimum conditions for producing the desired NPs. Methods: The development of the NPs was carried out by a double emulsion solvent evaporation technique with yield enhancement. The NPs data were fitted in Minitab software to obtain the best fit model. Results: By using BBD, the most optimum conditions for producing the smallest size, highest magnitude of charge, and highest EE% of PCL NPs were predicted to be achieved by using 61.02 mg PCL, 9 mg IRH, and 4.82% PVA, which would yield 203.01 nm, −15.81 mV, and 82.35% EE. Conclusion: The analysis by BBD highlighted that the model was a good fit to the data, confirming the suitability of the design of the experiments. [ABSTRACT FROM AUTHOR]

The impacts of liposomal encapsulation on the bitterness of salmon frame protein hydrolysate (SFPH) and salmon frame protein plastein (SFPP) with the aid of ultrasound (20% amplitude, 750 W) for different time intervals (30, 60 and 120 s) were investigated. Liposomes loaded with 1% protein hydrolysate (L-PH1) and 1% plastein (L-PT1) showed the highest encapsulation efficiency and the least bitterness (p < 0.05). Ultrasonication for longer times reduced encapsulation efficiency (EE) and increased bitterness of both L-PH1 and L-PT1 along with a reduction in particle size. When comparing between L-PH1 and L-PT1, the latter showed less bitterness due to the lower bitterness in nature and higher entrapment of plastein in the liposomes. In vitro release studies also showed the delayed release of peptides from L-PT1 in comparison to the control plastein hydrolysate. Therefore, encapsulation of liposomes with 1% plastein could be an efficient delivery system for improving the sensory characteristics by lowering the bitterness of protein hydrolysates. [ABSTRACT FROM AUTHOR]

Featured Application: Novel spray-dried casein micelles microcapsules were developed to extend the stability and bioavailability of anthraquinones extracted from Aloe vera. These microcapsules can be used commercially in food formulations (yoghurt, bakery products and health drinks) while developing functional foods and nutraceuticals to use as laxative, antibacterial, antiviral and anti-inflammatory. The encapsulation efficiency (EE%) and structural changes within the Anthraquinones-encapsulated casein micelles (CM) powders were evaluated in this study. For this purpose, the anthraquinone powder extracted from Aloevera, its freeze-dried powder (FDP) and whole leaf Aloe vera gel (WLAG) has been encapsulated in CM through ultrasonication prior to spray dying to produce nanocapsules: CM encapsulated anthraquinone powder (CMAQP), CM encapsulated freeze-dried powder (CMFDP) and CM encapsulated Whole leaf aloe vera gel (CMWLAG). Based on the pH of the solution before drying, CMAQP had the highest EE% following spray drying. However, due to air-interface-related dehydration stresses, SD resulted in a slight decrease in the EE% of anthraquinones (aloin, aloe-emodin, and rhein) in CMAQP. Meanwhile, a significant increase in EE% of CMFDP was observed compared to the aqueous state. According to SEM findings, the particle size of CMAQP was 2.39 µm and ξ-potential of ~−17mV. The CMFDP had a rough fractal surface with large particle sizes and potential of 3.49 µm and ~−11mV respectively. CM deformed, having the least EE% and lowest ξ-potential (−4.5 mV). Spray drying enhances melanoidin formation in CMWLAG, as evidenced by the highest chroma values. The results suggested that EE%, stability, and degree of Maillard reaction are closely linked to the type of anthraquinone encapsulated, the pH of the solution, and the nanostructure of casein micelles during spray drying. [ABSTRACT FROM AUTHOR]

The development of fish oral vaccines is of great interest to the aquaculture industry due to the possibility of rapid vaccination of a large number of animals at reduced cost. In a previous study, we evaluated the effect of alginate-encapsulated Piscirickettsia salmonis antigens (AEPSA) incorporated in feed, effectively enhancing the immune response in Atlantic salmon (Salmo salar). In this study, we seek to characterize AEPSA produced by ionic gelation using an aerodynamically assisted jetting (AAJ) system, to optimize microencapsulation efficiency (EE%), to assess microparticle stability against environmental (pH, salinity and temperature) and gastrointestinal conditions, and to evaluate microparticle incorporation in fish feed pellets through micro-CT-scanning. The AAJ system was effective in obtaining small microparticles (d < 20 μm) with a high EE% (97.92%). Environmental conditions (pH, salinity and temperature) generated instability in the microparticles, triggering protein release. 62.42% of the protein content was delivered at the intestinal level after in vitro digestion. Finally, micro-CT-scanning images confirmed microparticle incorporation in fish feed pellets. In conclusion, the AAJ system is effective at encapsulating P. salmonis antigens in alginate with a high EE% and a size small enough to be incorporated in fish feed and produce an oral vaccine. [ABSTRACT FROM AUTHOR]

This review presents an updated scenario of findings and evolutions of encapsulation of bioactive compounds for food and agricultural applications. Many polymers have been reported as encapsulated agents, such as sodium alginate, gum Arabic, chitosan, cellulose and carboxymethylcellulose, pectin, Shellac, xanthan gum, zein, pullulan, maltodextrin, whey protein, galactomannan, modified starch, polycaprolactone, and sodium caseinate. The main encapsulation methods investigated in the study include both physical and chemical ones, such as freeze-drying, spray-drying, extrusion, coacervation, complexation, and supercritical anti-solvent drying. Consequently, in the food area, bioactive peptides, vitamins, essential oils, caffeine, plant extracts, fatty acids, flavonoids, carotenoids, and terpenes are the main compounds encapsulated. In the agricultural area, essential oils, lipids, phytotoxins, medicines, vaccines, hemoglobin, and microbial metabolites are the main compounds encapsulated. Most scientific investigations have one or more objectives, such as to improve the stability of formulated systems, increase the release time, retain and protect active properties, reduce lipid oxidation, maintain organoleptic properties, and present bioactivities even in extreme thermal, radiation, and pH conditions. Considering the increasing worldwide interest for biomolecules in modern and sustainable agriculture, encapsulation can be efficient for the formulation of biofungicides, biopesticides, bioherbicides, and biofertilizers. With this review, it is inferred that the current scenario indicates evolutions in the production methods by increasing the scales and the techno-economic feasibilities. The Technology Readiness Level (TRL) for most of the encapsulation methods is going beyond TRL 6, in which the knowledge gathered allows for having a functional prototype or a representative model of the encapsulation technologies presented in this review. [ABSTRACT FROM AUTHOR]

Rapid release and diminished stability are two of the limitations associated with the growth factors that are essentially used in dental applications. These growth factors are employed to enhance the quality and quantity of tissue or bone matter during regeneration. Therefore, drug delivery devices and systems have been developed to address these limitations. In this study, bovine serum albumin (BSA), as a representative growth factor, was successfully sustained by encapsulation with the medium-absorbable copolymer, poly(L-lactide-co-glycolide) (PLG) 70:30% mol, via the multiple emulsion method. Different PLG, PVA, and BSA concentrations were used to investigate their effects on the BSA encapsulation efficiency. The suitable ratios leading to a better characterization of microparticles and a higher encapsulation efficiency in producing encapsulated PLG microparticles were 8% (w/v) of PLG, 0.25% (w/v) of PVA, and 8% (w/v) of BSA. Furthermore, an in vitro release study revealed a bursting release of BSA from the encapsulated PLG microsphere in the early phase of development. Subsequently, a gradual release was observed over a period of eight weeks. Furthermore, to encapsulate LL-37, different proteins were used in conjunction with PLG under identical conditions with regard to the loading efficiency and morphology, thereby indicating high variations and poor reproducibility. In conclusion, the encapsulated PLG microparticles could effectively protect the protein during encapsulation and could facilitate sustainable protein release over a period of 60 days. Importantly, an optimal method must be employed in order to achieve a high degree of encapsulation efficiency for all of the protein or growth factors. Accordingly, the outcomes of this study will be useful in the manufacture of drug delivery devices that require medium-sustained release growth factors, particularly in dental treatments. [ABSTRACT FROM AUTHOR]

The main aim of this study was to optimize the formulation and process variables for the preparation of ibrutinib nanoliposomes and to evaluate the stability of nanoliposomes. The influence of four formulations and process parameters, namely, the phosphatidylcholine-to-cholesterol ratio (A), conc. of ibrutinib (B), sonication time (C), and stirring time (D) on the drug encapsulation efficiency (Y1) and particle size (Y2) of ibrutinib nanoliposomes were investigated by using response surface methodology. Reverse-phase evaporation was used to prepare ibrutinib nanoliposomes. Twenty-nine trial experiments were performed as per the design and the response parameters were noted. Multiple linear regression analysis was used to assess each response parameter. The effect of each factor on the response parameters was depicted using perturbation, response surface, and contour plots. A numerical optimization technique was used to estimate the optimum process parameters to obtain the desired responses. Ibrutinib nanoliposomes prepared under optimal conditions were evaluated for stability at a different temperature, pH, and sonication time. It is evident from the results that the phosphatidylcholine-to-cholesterol ratio (A) was the major factor influencing the encapsulation efficiency. All the factors were found to have noteworthy influences on particle size. A statistical evaluation provided the information about the individual and interactive effects of independent factors on the response parameters in order to obtain optimum experimental conditions that lead to preparing nanoliposomes with improved characteristics. The optimum level of the independent variables was phosphatidylcholine:cholesterol (6.76:1), ibrutinib concentration (2 mg/mL), sonication time (15.13 min), and stirring time (45 min). At optimal conditions, Y1 and Y2 were found to be 90.76 ± 1.56% and 208.24 ± 3.16 nm, respectively. The ibrutinib nanoliposomes were found to be stable both in simulated gastric and intestinal fluids at 37 °C for 6 h. At elevated conditions of temperature and pH, the prepared nanoliposomes were found to be unstable. Sonication for shorter periods resulted in decreased particle size, whereas longer periods can be helpful for ultrasound-assisted drug delivery. The closeness between the obtained results and predicted results indicates the reliability of the optimization technique for the preparation of ibrutinib nanoliposomes. [ABSTRACT FROM AUTHOR]

Biopolymers, especially polysaccharides (e.g., gum Arabic), are widely applied as drug carriers in drug delivery systems due to their advantages. Curcumin, with high antioxidant ability but limited solubility and bioavailability in the body, can be encapsulated in gum Arabic to improve its solubility and bioavailability. When curcumin is encapsulated in gum Arabic, it is essential to understand how it works in various conditions. As a result, in Simulated Intestinal Fluid and Simulated Gastric Fluid conditions, we investigated the potential of gum Arabic as the drug carrier of curcumin. This study was conducted by varying the gum Arabic concentrations, i.e., 5, 10, 15, 20, 30, and 40%, to encapsulate 0.1 mg/mL of curcumin. Under both conditions, the greater the gum Arabic concentration, the greater the encapsulation efficiency and antioxidant activity of curcumin, but the worse the gum Arabic loading capacity. To achieve excellent encapsulation efficiency, loading capacity, and antioxidant activity, the data advises that 10% is the best feasible gum Arabic concentration. Regarding the antioxidant activity of curcumin, the findings imply that a high concentration of gum Arabic was effective, and the Simulated Intestinal Fluid brought an excellent surrounding compared to the Simulated Gastric Fluid solution. Moreover, the gum Arabic releases curcumin faster in the Simulated Gastric Fluid condition. [ABSTRACT FROM AUTHOR]

A medium-chain triglyceride (MCT) oil microcapsule was prepared by spray drying. The effects of the wall-material parameters of wall-to-oil ratio (1:1 to 3:1) and type of wall material (gum arabic (GA), whey protein isolate (WPI), and octenyl succinic anhydride (OSA) starch) on the microcapsules were evaluated. The droplet size, size distribution, viscosity, zeta potential, and stability of the emulsions were measured. The spray-dried powder was characterized by its morphology, yield, encapsulation efficiency, and moisture content. The wall material influenced the characteristics of the emulsions and microcapsules. The formulation with a 2:1 wall-to-oil ratio and OSA starch/maltodextrin as the wall material resulted in a small droplet size (0.177 ± 0.002 µm) with high encapsulation efficiency (98.38 ± 0.01%). This formulation had good physical stability over three months under accelerated conditions. Thus, OSA starch/maltodextrin is an appropriate wall material for encapsulating MCT oil. [ABSTRACT FROM AUTHOR]

The aim of the study is to compare selected carbohydrates that differed in the glycaemic index: maltodextrin, three native starches (wheat, rice, maize), and two disaccharides (trehalose and lactose) used to encapsulation of model oil (in this case cold-pressed pumpkin oil). Encapsulation efficiency of pumpkin oil by spray drying, size of obtained capsules, oxidative stability of encapsulated oil, and retention of tocopherols, squalene, and sterols in surface and core material of capsules were determined. It was found that encapsulation efficiency varied from 35% for rice starch to 68–71% for wheat starch, maltodextrin, and lactose. The bulk density of capsules was independent of the used carbohydrate type (189–198 kg/m3), while their size was significantly lower for samples of pumpkin oil encapsulated in native starches (over 2 times compared to capsules with trehalose). Of the best lipid capturing agents (native wheat starch, maltodextrin, and lactose), wheat starch mainly bound tocopherols, squalene, and sterols to the capsule surface, while lactose to the core material of the capsules (35.5–81.2%). Among tested carbohydrates, native wheat starch acted as the best antioxidant agent (oxidative stability was 15.1 h vs. 9.4 h for pure pumpkin oil). [ABSTRACT FROM AUTHOR]

In recent years, starch nanoparticles (SNPs) have attracted growing attention due to their unique properties as a sustainable alternative to common nanomaterials since they are natural, renewable and biodegradable. SNPs can be obtained by the breakdown of starch granules through different techniques which include both physical and chemical methods. The final properties of the SNPs are strongly influenced by the synthesis method used as well as the operational conditions, where a controlled and monodispersed size is crucial for certain bioapplications. SNPs are considered to be a good vehicle to improve the controlled release of many bioactive compounds in different research fields due to their high biocompatibility, potential functionalization, and high surface/volume ratio. Their applications are frequently found in medicine, cosmetics, biotechnology, or the food industry, among others. Both the encapsulation properties as well as the releasing processes of the bioactive compounds are highly influenced by the size of the SNPs. In this review, a general description of the different types of SNPs (whole and hollow) synthesis methods is provided as well as on different techniques for encapsulating bioactive compounds, including direct and indirect methods, with application in several fields. Starches from different botanical sources and different bioactive compounds are compared with respect to the efficacy in vitro and in vivo. Applications and future research trends on SNPs synthesis have been included and discussed. [ABSTRACT FROM AUTHOR]

Anthocyanins are value-added food ingredients that have health-promoting impacts and biological functionalities. Nevertheless, there are technological barriers to their application in the food industry, mainly because of their poor stability and susceptibility to harsh environmental conditions, such as oxygen, temperature, pH, and light, which could profoundly influence the final food product′s physicochemical properties. Microencapsulation technology is extensively investigated to enhance stability, bioaccessibility, and impart controlled release properties. There are many varieties of microencapsulation methods and diverse types of wall materials. However, choosing a proper approach involves considering the processing parameters, equipment availability, and application purposes. The present review thoroughly scrutinizes anthocyanins′ chemical structure, principles, benefits, and drawbacks of different microencapsulation methods, including spray drying, freeze drying, electrospinning/electrospraying, inclusion complexes, emulsification, liposomal systems, ionic gelation, and coacervation. Furthermore, wall materials applied in different techniques plus parameters that affect the powders′ encapsulation efficiency and physicochemical properties are discussed. Future studies should focus on various processing parameters and the combination of different techniques and applications regarding microencapsulated anthocyanins in functional foods to assess their stability, efficiency, and commercialization potentials. [ABSTRACT FROM AUTHOR]

Recent findings have proved the benefits of Pioglitazone (PGZ) against atherosclerosis and type 2 diabetes. Since the systematic and controllable release of this drug is of significant importance, encapsulation of this drug in nanoparticles (NPs) can minimize uncontrolled issues. In this context, drug delivery approaches based on several poly(lactic-co-glycolic acid) (PLGA) nanoparticles have been rising in popularity due to their promising capabilities. However, a fully reliable and reproducible synthetic methodology is still lacking. In this work, we present a rational optimization of the most critical formulation parameters for the production of PGZ-loaded PLGA NPs by the single emulsification-solvent evaporation or nanoprecipitation methods. We examined the influence of several variables (e.g., component concentrations, phases ratio, injection flux rate) on the synthesis of the PGZ-NPs. In addition, a comparison of these synthetic methodologies in terms of nanoparticle size, polydispersity index (PDI), zeta potential (ζp), drug loading (DL%), entrapment efficiency (EE%), and stability is offered. According to the higher entrapment efficiency content, enhanced storage time and suitable particle size, the nanoprecipitation approach appears to be the simplest, most rapid and most reliable synthetic pathway for these drug nanocarriers, and we demonstrated a very slow drug release in PBS for the best formulation obtained by this synthesis. [ABSTRACT FROM AUTHOR]

Edible nanoparticles containing antibacterial agents are one of the effective strategies to control foodborne diseases. Herein, novel ternary nanoparticles (TNP) were prepared from rosemary essential oil (REO), nisin and Lycium barbarum polysaccharides (LBP) through hydrophobic and electrostatic interaction. The average particle size of TNP was 211.5 nm, and its encapsulation efficiency reached 86.6%. After the addition of LBP, the physical stability, thermal stability and storage stability of TNP were significantly improved. In vitro, compared with the control group, the population of S. aureus and E. coli O157:H7 in the TNP-treated group was reduced by 2.386 log CFU/mL and 1.966 log CFU/mL, respectively, on the fifth day. The free radical scavenging rate of TNP was 63.15%. The application of TNP on beef presented favorable preservation effects without affecting its color and texture. Therefore, the synthesis strategy of TNP has important reference significance for the research and development of new food antibacterial agents. [ABSTRACT FROM AUTHOR]

Numerous attempts to overcome the poor water solubility of cam ptothecin (CPT) by various nano drug delivery systems are described in various sources in the literature. However, the results of these approaches may be hampered by the incomplete separation of free CPT from the formulations, and this issue has not been investigated in detail. This study aimed to promote the solubility and continuous delivery of CPT by developing long-lasting liposomes using various weights (M.W. 2000 and 5000 Daltons) of the hydrophilic polymer polyethylene glycol (PEG). Conventional and PEGylated liposomes containing CPT were formulated via the lipid film hydration method (solvent evaporation) using a rotary flash evaporator after optimising various formulation parameters. The following physicochemical characteristics were investigated: surface morphology, particle size, encapsulation efficiency, in vitro release, and formulation stability. Different molecular weights of PEG were used to improve the encapsulation efficiency and particle size. The stealth liposomes prepared with PEG5000 were discrete in shape and with a higher encapsulation efficiency (83 ± 0.4%) and a prolonged rate of drug release (32.2% in 9 h) compared with conventional liposomes (64.8 ± 0.8% and 52.4%, respectively) and stealth liposomes containing PEG2000 (79.00 ± 0.4% and 45.3%, respectively). Furthermore, the stealth liposomes prepared with PEG5000 were highly stable at refrigeration temperature. Significant changes were observed using various pharmacokinetic parameters (mean residence time (MRT), half-life, elimination rate, volume of distribution, clearance, and area under the curve) of stealth liposomes containing PEG2000 and PEG5000 compared with conventional liposomes. The stealth liposomes prepared with PEG5000 showed promising results with a slow rate of release over a long period compared with conventional liposomes and liposomes prepared with PEG2000, with altered tissue distribution and pharmacokinetic parameters. [ABSTRACT FROM AUTHOR]

This paper discusses the development and validation of a rapid method for the reversed phase HPLC-UV quantification of biodegradable poly(D,L-lactic-co-glycolic) acid (PLGA) microspheres co-loaded with two neuroprotective agents (dexamethasone and melatonin) (DX-MEL-MSs) to be intravitreally administered as a promising glaucoma treatment. The study was performed to validate two procedures that quantify the content of the two active substances entrapped into the polymer matrix during an encapsulation efficiency assay and the amount of drugs liberated over time during the in vitro release assay. The reversed-phase method allowed for the simultaneous determination of dexamethasone and melatonin, which were respectively detected at 240.5 and 222.7 nm. Chromatographic separation was performed using an Ascentis® C18 HPLC Column (25 cm × 4.6 mm, 5 µm) with an isocratic mobile phase composed of methanol-water (70:30, v/v) with 1.0 mL min−1 flow rate. The two procedures were validated analytically in terms of system suitability testing, specificity, linearity, precision, accuracy, sensitivity, and robustness. Both the validated procedures were applied to characterize DX-MEL-MSs and were found appropriate to quantify the drug quantities encapsulated and estimate their release profile over 10 days. The validation study designed in this work can be helpful for planning any other protocols that refer to the quantification of PLGA based drug delivery systems. [ABSTRACT FROM AUTHOR]

Curcumin has been demonstrated to have biological activities and its fortification in food products is an important strategy to deliver bioactive ingredients at target sites. However, studies have documented a curcumin low bioavailability and low intake. Hence, combining functional ingredients with food should be needed to prevent widespread nutrient intake shortfalls and associated deficiencies. Thus, curcumin was encapsulated in calcium-alginate and their characteristics as well as in vitro release behavior of curcumin hydrogel beads (CHBs) was studied. Moreover, CHBs were fortified in development of functional Kulfi and their quality characteristics were studied. The encapsulation efficiency was up to 95.04%, indicating that most of the curcumin was entrapped. FTIR shifts in the bands were due to the replacement of sodium ions to the calcium ions. In vitro release (%) for CHBs was found to be 67.15% after 2 h, which increased slightly up to 67.88% after 4 h. The average swelling index of CHBs was found to be 10.21 to 37.92 from 2 to 12 h in PBS (pH 7.40). Control and Kulfi fortified with CHBs showed no significant difference (p > 0.05) in colour (L = 73.03 and 75.88) and the melting rate (0.88 mL/min and 0.63 mL/min), respectively. Standard plate count was reduced in the Kulfi fortified with CHBs (13.77 × 104 CFU/mL) with high sensory score for overall acceptability (8.56) compared to the control (154.70 × 104 CFU/mL). These findings suggested the feasibility of developing CHBs to mask the bitterness, enhance the solubility, and increase the bioavailability in gastrointestinal conditions. Additionally, Kulfi could be a suitable dairy delivery system for curcumin bioactive compounds. [ABSTRACT FROM AUTHOR]

Saffron extract was encapsulated into a gelatin matrix by means of electrospinning and freeze drying techniques and the degradation kinetics of bioactive compounds were evaluated during their storage at 4, 24, and 35 °C as compared to non-encapsulated control. The encapsulation efficiency, thermal properties, storage stability, morphology, and diameter distribution of the encapsulated saffron extract were evaluated as output parameters. In general, both encapsulation techniques demonstrated superior retention of bioactive compounds compared to samples without encapsulation during the entire storage period. Electrospinning and freeze drying techniques were able to retain at least 96.2 and 93.7% of crocin, respectively, after 42 days of storage at 35 °C with the 15% saffron extract. The half-life (t1/2) time parameter for the control sample (with 15% saffron extract without encapsulation) was 22 days at 4 °C temperature, while that encapsulated by electrospinning was 138 days and that obtained for freeze drying was 77 days, The half-lives were longer at lower temperatures. The encapsulation efficiency of crocin, picrocrocin, and safranal associated with the electro-spun gelatin fibers were 76.3, 86.0, and 74.2%, respectively, and in comparison, the freeze drying encapsulation efficiencies were relatively lower, at 69.0, 74.7, and 65.8%, respectively. Electro-spun gelatin fibers also had higher melting and denaturation temperatures of 78.3 °C and 108.1 °C, respectively, as compared to 65.4 °C and 93.2 °C, respectively, for freeze-dried samples. Thus, from all respects, it was concluded that electrospinning was a better and more effective technique than freeze drying in terms of preserving saffron bioactive compounds. [ABSTRACT FROM AUTHOR]

Drug carrier nanoparticles (NPs) were prepared by the polyelectrolyte method, with chitosan sulfate, with different substituents and quaternary ammonium chitosan, including C236-HACC NPs, C36-HACC NPs, and C6-HACC NPs. To evaluate whether the NPs are suitable for loading different antigens, we chose bovine serum albumin (BSA), ovalbumin (OVA), and myoglobin (Mb) as model antigens to investigate the encapsulation effect of the NPs. The characteristics (size, potential, and encapsulation efficiency) of the NPs were measured. Moreover, the NPs with higher encapsulation efficiency were selected for the immunological activity research. The results showed that chitosan derivative NPs with different substitution sites had different loading effects on the three antigens, and the encapsulation rate of BSA and OVA was significantly better than that of Mb. Moreover, the NPs encapsulated with different antigens have different immune stimulating abilities to DCS cells, the immune effect of OVA-coated NPs was significantly better than that of BSA-coated NPs and blank NPs, especially C236-HACC-OVA NPs. Furthermore, we found that C236-HACC-OVA NPs could increase the phosphorylation level of intracellular proteins to activate cell pathways. Therefore, C236-HACC NPs are more suitable for the loading of antigens similar to the OVA structure. [ABSTRACT FROM AUTHOR]

In this study, we chemically modified the short linear glucan (SLG) using the 3-chloro-2-hydroxypropyl trimethylammonium chloride to introduce a positive surface charge via cationization (CSLG). We then prepared CSLG-based binary nanocomplex particles through electrostatic interactions with low and high methoxyl pectin. The two new types of binary nanocomplex were comprehensively characterized. It was found that the nanocomplex particles showed a spherical shape with the particle size of <700 nm, smooth surface, homogeneous distribution, and negative surface charge. Fourier transform infrared spectroscopy (FTIR) revealed that the driving forces to form nanocomplex were primarily electrostatic interactions and hydrogen bonding. In addition, increasing the CSLG concentration in the nanocomplex significantly enhanced both thermal stability and digestive stability. By comparing the two complex nanoparticles, the HMP-CSLG has a larger particle size and better stability under the GI condition due to the high content of the methoxy group. Additionally, the HMP-CSLG nanoparticle has a higher encapsulation efficiency and slower release rate under simulated gastrointestinal fluid for tangeretin compared with the LMP-CSLG. These results provide new insights into designing the CSLG-based nanocomplex as a potential oral delivery system for nutraceuticals or active ingredients. [ABSTRACT FROM AUTHOR]

Refined cobia liver oil is a nutritional supplement (CBLO) that is rich in polyunsaturated fatty acids (PUFAs), such as DHA and EPA; however, PUFAs are prone to oxidation. In this study, the fabrication of chitosan-TPP-encapsulated CBLO nanoparticles (CS@CBLO NPs) was achieved by a two-step method, including emulsification and the ionic gelation of chitosan with sodium tripolyphosphate (TPP). The obtained nanoparticles were inspected by dynamic light scattering (DLS) and showed a positively charged surface with a z-average diameter of between 174 and 456 nm. Thermogravimetric analysis (TGA) results showed the three-stage weight loss trends contributing to the water evaporation, chitosan decomposition, and CBLO decomposition. The loading capacity (LC) and encapsulation efficiency (EE) of the CBLO loading in CS@CBLO NPs were 17.77–33.43% and 25.93–50.27%, respectively. The successful encapsulation of CBLO in CS@CBLO NPs was also confirmed by the Fourier transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) techniques. The oxidative stability of CBLO and CS@CBLO NPs was monitored by FTIR. As compared to CBLO, CS@CBLO NPs showed less oxidation with a lower generation of hydroperoxides and secondary oxidation products after four weeks of storage. CS@CBLO NPs are composed of two ingredients that are beneficial for health, chitosan and fish oil in a nano powdered fish oil form, with an excellent oxidative stability that will enhance its usage in the functional food and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

Dual centrifugation (DC) is a novel in-vial homogenization technique for the preparation of liposomes in small batch sizes under gentle and sterile conditions which allows encapsulation efficiencies ( EE ) for water soluble compounds of >50%. Since liposome size, size distribution (PDI), and EE depend on the lipid concentration used in the DC process, a screening method to find optimal lipid concentrations for a defined lipid composition was developed. Four lipid mixtures consisting of cholesterol, hydrogenated or non-hydrogenated egg PC, and/or PEG-DSPE were screened and suitable concentration ranges could be identified for optimal DC homogenization. In addition to the very fast and parallel liposome preparation of up to 40 samples, the screening process was further accelerated by the finding that DC generates homogeneously mixed liposomes from a macroscopic lipid mixture without the need to initially prepare a molecularly mixed lipid film from an organic solution of all components. This much simpler procedure even works for cholesterol containing lipid blends, which could be explained by a nano-milling of the cholesterol crystals during DC homogenization. Furthermore, EE determination was performed by time-resolved fluorescence measurements of calcein-loaded liposomes without removing the non-entrapped calcein. The new strategy allows the rapid characterization of a certain lipid composition for the preparation of liposomes within a working day.

Two multi-functional powders, in terms of anthocyanins from black rice (Oryza sativa L.) and lactic acid bacteria (Lactobacillus paracasei, L. casei 431®) were obtained through co-microencapsulation into a biopolymer matrix composed of milk proteins and inulin. Two extracts were obtained using black rice flour as a raw material and hot water and ethanol as solvents. Both powders (called P1 for aqueous extract and P2 for ethanolic extract) proved to be rich sources of valuable bioactives, with microencapsulation efficiency up to 80%, both for anthocyanins and lactic acid bacteria. A higher content of anthocyanins was found in P1, of 102.91 ± 1.83 mg cyanindin-3-O-glucoside (C3G)/g dry weight (DW) when compared with only 27.60 ± 17.36 mg C3G/g DW in P2. The morphological analysis revealed the presence of large, thin, and fragile structures, with different sizes. A different pattern of gastric digestion was observed, with a highly protective effect of the matrix in P1 and a maximum decrease in anthocyanins of approximatively 44% in P2. In intestinal juice, the anthocyanins decreased significantly in P2, reaching a maximum of 97% at the end of digestion; whereas in P1, more than 45% from the initial anthocyanins content remained in the microparticles. Overall, the short-term storage stability test revealed a release of bioactive from P2 and a decrease in P1. The viable cells of lactic acid bacteria after 21 days of storage reached 7 log colony forming units (CFU)/g DW. [ABSTRACT FROM AUTHOR]

This research highlights the capacity of a newly introduced centrifugation process to form liposomes from water-in-fluorocarbon nano-emulsions stabilized with phospholipids to incorporate macromolecular and sensitive active pharmaceutical ingredients (API). The encapsulation efficiency of the produced liposomes, incorporating fluorescein-sodium, bovine serum albumin and fluorecein isothiocyanate dextran as model APIs, is determined by applying Vivaspin® centrifugation filtration and quantified by UV-Vis spectroscopy. It was found that higher densities of the fluorocarbons used as the hydrophobic phase enable a higher encapsulation efficiency and that an efficiency of up to 98% is possible depending on the used phospholipid. Among the engineering aspects of the process, a comparison between different membrane substances was performed. Efficiency increases with a higher phospholipid concentration but decreases with the addition of cholesterol. Due to the higher bending modulus, liposome formation is slowed down by cholesterol during liposome closure leading to a greater leakage of the model API. The encapsulation of bovine serum albumin and dextran, both investigated under different osmotic conditions, shows that an efflux negatively affects the encapsulation efficiency while an influx increases the stability. Overall, the process shows the potential for a very high encapsulation efficiency for macromolecules and future pharmaceutical applications. [ABSTRACT FROM AUTHOR]

Liposomes are consolidated and attractive biomimetic nanocarriers widely used in the field of drug delivery. The structural versatility of liposomes has been exploited for the development of various carriers for the topical or systemic delivery of drugs and bioactive molecules, with the possibility of increasing their bioavailability and stability, and modulating and directing their release, while limiting the side effects at the same time. Nevertheless, first-generation vesicles suffer from some limitations including physical instability, short in vivo circulation lifetime, reduced payload, uncontrolled release properties, and low targeting abilities. Therefore, liposome preparation technology soon took advantage of the possibility of improving vesicle performance using both natural and synthetic polymers. Polymers can easily be synthesized in a controlled manner over a wide range of molecular weights and in a low dispersity range. Their properties are widely tunable and therefore allow the low chemical versatility typical of lipids to be overcome. Moreover, depending on their structure, polymers can be used to create a simple covering on the liposome surface or to intercalate in the phospholipid bilayer to give rise to real hybrid structures. This review illustrates the main strategies implemented in the field of polymer/liposome assembly for drug delivery, with a look at the most recent publications without neglecting basic concepts for a simple and complete understanding by the reader. [ABSTRACT FROM AUTHOR]