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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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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 1 H 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.

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.

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.

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.

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.

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.

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 W 1 /O/W 2 emulsions. Moreover, gelatin was added into the internal aqueous phase (W 1 ) to construct W 1 /O/W 2 emulsion-gels system. The encapsulation efficiency of HIA-stabilized W 1 /O/W 2 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 W 1 , 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 W 1 /O/W 2 emulsions system and its application in the package delivery of functional substances in the food field.

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.

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.

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.

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).

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.

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

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.

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.

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.

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.

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.

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.

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.

Since its discovery, evidence that siRNA was able to act as an RNA interference effector, led to its acceptation as a novel medicine. The siRNA approach is very effective, due to its catalytic mechanism, but still the limitations of its cellular delivery should be addressed. One promising form of non-viral gene delivery system is liposomes. The variable and versatile nature of the lipids keeps the possibility to upgrade the liposomal structure, which makes them suitable for encapsulation and delivery of drugs. However, to avoid the limitation of fast release for the hydrophilic drug, we previously designed viscous core liposomes. We aimed in this work to evaluate if these viscous core liposomes (NvcLs) could be of interest for siRNA encapsulation. Then, we sought to add a limited amount of positive charges to provide cell interaction and transfection. Cationic lipid dimyristoylaminopropylaminopropyl or the polymer poly(ethylenimine) were incorporated in NvcL to produce positively charged viscous core liposomes (PvcL) by a customized microfluidic device. We found that NvcLs increased the encapsulation efficiency and loading content with regards to the neutral liposome. Both PvcLPEI and PvcLDMAPAP exhibited transfection and GFP knock-down (≈40%) in both 2D and 3D cell cultures. Finally, the addition of slight positive charges did not induce cell toxicity.

Onion-type multi-lamellar liposomes (MLLs), composed of a mixture of phosphatidylcholine and Tween 80, were analyzed for their ability to encapsulate ε-Viniferin (εVin), a resveratrol dimer. Their encapsulation efficiency (EE) was measured by UV-VIS spectroscopy using three different separation methods—ultracentrifugation, size exclusion chromatography, and a more original and advantageous one, based on adsorption filtration. The adsorption filtration method consists indeed of using syringe filters to retain the molecule of interest, and not the liposomes as usually performed. The process is rapid (less than 10 min), easy to handle, and inexpensive in terms of sample amount (around 2 mg of liposomes) and equipment (one syringe filter is required). Whatever the separation method, a similar EE value was determined, validating the proposed method. A total of 80% ± 4% of εVin was found to be encapsulated leading to a 6.1% payload, roughly twice those reported for resveratrol-loaded liposomes. Finally, the release kinetics of εVin from MLLs was followed for a 77 day period, demonstrating a slow release of the polyphenol.

In the present study, nanoliposomes composed of rapeseed lecithin were used for the encapsulation of anthocyanin compounds (AC). The nanoliposomes were prepared using hydration and ultrasound combined method, and the effect of AC concentration (4.5, 6.75, 9% w/w) on the characteristics of nanoliposomes including particle size, polydispersity index (PDI), zeta potential, and the encapsulation efficiency (EE) of nanoliposomes with and without AC were studied. The results suggested the fabricated nanoliposomes had a size range of 141–196 nm, negative zeta potential and narrow particle size distribution. Further, the samples containing 9% extract had the maximum EE (43%). The results showed elevation of AC concentration resulted in increased particle size, PDI, EE, and surface charge of nanoparticles. The presence of AC extract led to diminished membrane fluidity through the hydrophobic interactions with the hydrocarbon chain of fatty acids. TEM images suggested that the nanoliposomes were nearly spherical and the AC caused their improved sphericity. Further, in vitro biocompatibility tests for human mesenchymal (MSC) and fibroblast (FBL) cells indicated nanoparticles were not toxic. Specifically, the best formulations with the maximum compatibility and bioavailability for MSC and FBL cells were AC-loaded nanoliposomes with concentrations of 0.5 mL/mg and 10.3 mL/µg and, respectively.

Vesicular nanocarriers have an important role in drug delivery and dietary supplements. Size control and optimization of encapsulation efficiency (EE) should be optimized for those applications. In this work, we report on the identification of the crucial step (injection, evaporation, or sonication) innanovesicles (transfersomes and niosomes) preparation by theethanol injection method (EI). The identification of each production step on the final vesicle size was analyzed in order to optimize further scale-up process. Results indicated that the final size of transfersomeswas clearly influenced by the sonication step while the final size of niosomes was mainly governed by the injection step. Measurements of final surface tension of the different vesicular systems prepared indicate a linear positive tendency with the vesicle size formed. This relation could help to better understand the process and design a vesicular size prediction model for EI. Vitamin D3 (VitD3) was encapsulated in the systems formulated with encapsulation efficiencies larger than 90%. Interaction between the encapsulated compound and the membrane layer components is crucial for vesicle stability. This work has an impact on the scaling-up production of vesicles for further food science applications.

Nowadays, pharmaceutical companies are facing several challenges with the development and approval of new biological products. The unique properties of several fluorinated ionic liquids (FILs), such as their high surfactant power in aqueous solutions, their chemical and biological stability, and low toxicity, favor their application in the pharmaceutical industry. Furthermore, the numerous combinations between cations and anions, in the FILs design, enlarge the possibilities to construct a successful delivery system. Several FILs also proved to not affect the activity, stability, and secondary structure of the therapeutic protein lysozyme. This work aims to study the aggregation behavior of distinct FILs in the protein suitable medium, in the presence or absence of lysozyme. Besides, different incubation conditions were tested to guarantee the optimal enzymatic activity of the protein at more stable delivery systems. Following the optimization of the incubation conditions, the quantification of the encapsulated lysozyme was performed to evaluate the encapsulation efficiency of each FIL-based system. The release of the protein was tested applying variables such as time, temperature, and ultrasound frequency. The experimental results suggest that the aggregation behavior of FILs is not significantly influenced by the protein and/or protein buffer and supports their application for the design of delivery systems with high encapsulation efficiencies, maintaining the biological activity of either encapsulated and released protein.

Droplet-based microfluidics offers significant advantages, such as high throughput and scalability, making platforms based on this technology ideal candidates for point-of-care (POC) testing and clinical diagnosis. However, the efficiency of co-encapsulation in droplets is suboptimal, limiting the applicability of such platforms for the biosensing applications. The homogeneity of the bioanalytes in the droplets is an unsolved problem. While there is extensive literature on the experimental setups and active methods used to increase the efficiency of such platforms, passive techniques have received less attention, and their fundamentals have not been fully explored. Here, we develop a novel passive technique for investigating cell encapsulation using the finite element method (FEM). The level set method was used to track the interfaces of forming droplets. The effects of walls and the droplet interfaces on relatively large cells were calculated to track them more accurately during encapsulation. The static surface tension force was used to account for the effects of the interfaces on cells. The results revealed that the pairing efficiency is highly sensitive to the standard deviation (SD) of the distance between the cells in the entrance channel. The pairing efficiency prediction error of our model differed by less than 5% from previous experiments. The proposed model can be used to evaluate the performance of droplet-based microfluidic devices to ensure higher precision for co-encapsulation of cells.

This study aims to improve the production efficiency of β-carotene suspensions using a naturally occurring Z-isomerization-accelerating catalyst, allyl isothiocyanate (AITC), via supercritical CO2 (SC-CO2). Namely, utilizing solubility improvement of β-carotene with the Z-isomerization by adding AITC in the SC-CO2-used dispersion process, the encapsulation efficiency of β-carotene was enhanced. The dispersion of β-carotene was conducted by ultrasonic treatment, and there was no involvement of organic solvents in the whole process. When 100 mg of AITC was added in the dispersion process, the encapsulation efficiency (β-carotene content in resulting suspension) was approximately 3.5 times higher than that without addition of the catalyst. Moreover, the Z-isomer ratio of β-carotene in the suspensions significantly improved, that is, it was approximately 12 times higher than the raw β-carotene material. Since Z-isomers of β-carotene are known to have higher antiatherosclerotic and antiatherogenic activities compared to the all-E-isomer, this one-step method not only efficiently produces β-carotene suspensions without organic solvents but also enhances the bioactivities of them.

The evaluation of encapsulation efficiency is a regulatory requirement for the characterization of drug delivery systems. However, the difficulties in efficiently separating nanomedicines from the free drug may compromise the achievement of accurate determinations. Herein, ultrafiltration was exploited as a separative strategy towards the evaluation of methotrexate (MTX) encapsulation efficiency in nanostructured lipid carriers and polymeric nanoparticles. The effect of experimental conditions such as pH and the amount of surfactant present in the ultrafiltration media was addressed aiming at the selection of suitable conditions for the effective purification of nanocarriers. MTX-loaded nanoparticles were then submitted to ultrafiltration and the portions remaining in the upper compartment of the filtering device and in the ultrafiltrate were collected and analyzed by HPLC-UV using a reversed-phase (C18) monolithic column. A short centrifugation time (5 min) was suitable for establishing the amount of encapsulated MTX in nanostructured lipid carriers, based on the assumption that the free MTX concentration was the same in the upper compartment and in the ultrafiltrate. The defined conditions allowed the efficient separation of nanocarriers from the free drug, with recoveries of >85% even when nanoparticles were present in cell culture media and in pig skin surrogate from permeation assays.

Thymol and the corresponding brominated derivatives constitute important biological active molecules as antibacterial, antioxidant, antifungal, and antiparasitic agents. However, their application is often limited, because their pronounced fragrance, their poor solubility in water, and their high volatility. The encapsulation of different thymol derivatives into biocompatible lignin-microcapsules is presented as a synergy-delivering remedy. The adoption of lignosulfonate as an encapsulating material possessing relevant antioxidant activity, as well as general biocompatibility allows for the development of new materials that are suitable for the application in various fields, especially cosmesis. To this purpose, lignin microcapsules containing thymol, 4-bromothymol, 2,4-dibromothymol, and the corresponding O-methylated derivatives have been efficiently prepared through a sustainable ultrasonication procedure. Actives could be efficiently encapsulated with efficiencies of up to 50%. To evaluate the applicability of such systems for topical purposes, controlled release experiments have been performed in acetate buffer at pH 5.4, to simulate skin pH: all of the capsules show a slow release of actives, which is strongly determined by their inherent lipophilicity.

Purple flesh cultivated potato (PP) is a foodstuff scarcely cultivated in the world but with high potential because of its anthocyanin content. Moreover, it has been little explored as a source of anthocyanins (AT) for further applications in formulated food products. The main goal of this research was to study the effect of maltodextrin (MD) and spray drying conditions on the encapsulation efficiency (EE) and bioaccesibility of AT from purple flesh cultivated potato extract (PPE). The anthocyanin-rich extract was obtained from PP and microencapsulated by spray-drying, using MD as the encapsulating agent. A statistical optimization approach was used to obtain optimal microencapsulation conditions. The PPE microparticles obtained under optimal conditions showed 86% of EE. The protector effect of microencapsulation on AT was observed to be stable during storage and in vitro digestion. The AT degradation rate constant was significantly lower for the PPE-MD than for the PPE. The assessed bioaccesibility of AT from the PPE-MD was 20% higher than that of the PPE, which could be explained by the protective effect of encapsulation against environmental conditions. In conclusion, microencapsulation is an effective strategy to protect AT from PP, suggesting that AT may be an alternative as a stable colorant for use in the food industry.

Double emulsions are very promising for various applications in pharmaceutics, cosmetics, and food. Despite lots of published research, only a few products have successfully been marketed due to immense stability problems. This review describes approaches on how to characterize the stability of double emulsions. The measurement methods are used to investigate the influence of the ingredients or the process on the stability, as well as of the environmental conditions during storage. The described techniques are applied either to double emulsions themselves or to model systems. The presented analysis methods are based on microscopy, rheology, light scattering, marker detection, and differential scanning calorimetry. Many methods for the characterization of double emulsions focus only on the release of the inner water phase or of a marker encapsulated therein. Analysis methods for a specific application rarely give information on the actual mechanism, leading to double emulsion breakage. In contrast, model systems such as simple emulsions, microfluidic emulsions, or single-drop experiments allow for a systematic investigation of diffusion and coalescence between the individual phases. They also give information on the order of magnitude in which they contribute to the failure of the overall system. This review gives an overview of various methods for the characterization of double emulsion stability, describing the underlying assumptions and the information gained. With this review, we intend to assist in the development of stable double emulsion-based products.

Single-cell analysis is of critical importance in revealing cell-to-cell heterogeneity by characterizing individual cells and identifying minority sub-populations of interest. Droplet-based microfluidics has been widely used in the past decade to achieve high-throughput single-cell analysis. However, to maximize the proportion of single-cell emulsification is challenging due to cell sedimentation and aggregation. The purpose of this study was to investigate the influence of single-cell encapsulation and incubation through the use of neutral buoyancy. As a proof of concept, OptiPrep™ was used to create neutrally buoyant cell suspensions of THP-1, a human monocytic leukemia cell line, for single-cell encapsulation and incubation. We found that using a neutrally buoyant suspension greatly increased the efficiency of single-cell encapsulation in microdroplets and eliminated unnecessary cell loss. Moreover, the presence of OptiPrep™ was shown to not affect cellular viability. This method significantly improved the effectiveness of single-cell study in a non-toxic environment and is expected to broadly facilitate single-cell analysis.

Since the first use of liposomes as carriers for antigens, much work has been done to elucidate the mechanisms involved in the encapsulation of vaccine-relevant biomolecules. However, only a few studies have specifically investigated the encapsulation of hydrophilic, non-conformational peptide epitopes. We performed comprehensive and systematic screening studies, in order to identify conditions that favor the electrostatic interaction of such peptides with lipid membranes. Moreover, we have explored bi-terminal sequence extension as an approach to modify the isoelectric point of peptides, in order to modulate their membrane binding behavior and eventually shift/expand the working range under which they can be efficiently encapsulated in an electrostatically driven manner. The findings of our membrane interaction studies were then applied to preparing peptide-loaded liposomes. Our results show that the magnitude of membrane binding observed in our exploratory in situ setup translates to corresponding levels of encapsulation efficiency in both of the two most commonly employed methods for the preparation of liposomes, i.e., thin-film hydration and microfluidic mixing. We believe that the methods and findings described in the present studies will be of use to a wide audience and can be applied to address the ongoing relevant issue of the efficient encapsulation of hydrophilic biomolecules.

The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.

Persimmon (Diospyros kaki L.), a fruit rich in phenolic compounds (PCs), has been considered effective in mitigating oxidative damage induced by an excess of reactive oxygen species. Due to large molecular weight and intrinsic instability in some physiological fluids, PCs’ passage through biological membranes is very limited. Carriers like phytosomes are promising systems to optimize oral absorption of encapsulated extracts. This work prepared and fully characterized phytosomes containing bioactive phenolic extracts from persimmon in terms of size, surface charge, encapsulation efficiency and stability over six months. These phytosomes were orally dosed to Wistar rats during a 15-day period. Afterwards, haematological and biochemical analyses were performed. Monodisperse phytosomes were successfully prepared, with size less than 300nm (PI < 0.3) and high encapsulation efficiency (97.4%) of PCs. In contrast to free extract, extract-loaded phytosomes had higher antioxidant activity after 6 months storage. Oral administration of extract-loaded phytosomes and free extract did not lead to lipidic profile changes and were within referenced normal ranges, as well as glycaemia levels and urine parameters. The results highlighted the potential of persimmon PCs as food supplements or pharmacological tools, suggesting a promising and safe phytosomal formulation containing bioactive agents of persimmon that could lead to health benefits.