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Messenger RNA (mRNA) is the template for protein biosynthesis and is emerging as an essential active molecule to combat various diseases, including viral infection and cancer. Especially, mRNA-based vaccines, as a new type of vaccine, have played a leading role in fighting against the current global pandemic of COVID-19. However, the inherent drawbacks, including large size, negative charge, and instability, hinder its use as a therapeutic agent. Lipid carriers are distinguishable and promising vehicles for mRNA delivery, owning the capacity to encapsulate and deliver negatively charged drugs to the targeted tissues and release cargoes at the desired time. Here, we first summarized the structure and properties of different lipid carriers, such as liposomes, liposome-like nanoparticles, solid lipid nanoparticles, lipid-polymer hybrid nanoparticles, nanoemulsions, exosomes and lipoprotein particles, and their applications in delivering mRNA. Then, the development of lipid-based formulations as vaccine delivery systems was discussed and highlighted. Recent advancements in the mRNA vaccine of COVID-19 were emphasized. Finally, we described our future vision and perspectives in this field. Lipid carriers with high biocompatibility have excellent mRNA encapsulation and delivery efficacy. Meanwhile, the emergence of lipid carriers provides an effective solution for delivering mRNA vaccines. [Display omitted] [ABSTRACT FROM AUTHOR]

Microencapsulation is utilized to protect probiotics, such as Geotrichum candidum , ensuring their survival, stability, and targeted release. The encapsulation efficiency depends on factors such as the type and concentration of the polymers and the encapsulation method. In this study, G. candidum was encapsulated using alginate (Alg) combined with starch (Alg S) or xanthan (Alg-X) and coated with chitosan aand chitosan nanoparticles (Alg C, Alg-S-C, Alg-X-C, Alg-CN, Alg-S-CN, and Alg-X-CN) using a simple extrusion technique. The structural characteristics and surface morphology of the microcapsules were analyzed using Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). Encapsulation efficiency (EE) and pH and temperature tolerances were assessed using in vitro assays. SEM results showed that the Alg-CN microcapsules were notably spherical and smooth, in contrast to the irregular and rough textures of the uncoated forms. Notably, Alg-CN exhibited the highest EE (99.3 %), followed by Alg-C (96.6 %) and Alg-X-CN (96.03 %). Moreover, chitosan-coated microcapsules, particularly Alg-CN, demonstrated superior viability at various pH levels and after exposure to 60 °C, along with extended shelf life at room temperature and 4 °C. These findings suggest that a 2 % alginate and 0.4 % chitosan combination is optimal for preserving G. candidum 's viability in various applications. [ABSTRACT FROM AUTHOR]

[Display omitted] To quantify concentration and encapsulation efficiency (EE) of mRNA in lipid nanoparticles (LNPs) the RiboGreen assay is extensively used. As part of this assay, a surfactant is used to release mRNA from LNPs for detection with the RiboGreen dye. So far, the surfactant of choice has been Triton X-100, which is harmful to human health and the environment. Alternatives to Triton X-100 are therefore needed, but surprisingly no such effort has yet been described in the literature. Here we show how three, less harmful, surfactants (Brij 93, Zwittergent 3–14 and Tween 20) compare to Triton X-100 for releasing mRNA from LNPs for detection with the RiboGreen assay. We found that Zwittergent 3–14 and Tween 20 at high concentrations (0.5 %) are at the minimum as effective as Triton X-100 at high concentration (0.5 %) across three different mRNA-LNP formulations. Interestingly, Tween 20 was the most effective at releasing mRNA from LNPs, across all concentration ranges explored (0.0025 %, 0.01 %, 0.1 % and to 0.5 % (v/v)) highlighting its potency at solubilizing the three different LNP formulations. Our results show that Tween 20 can be used as an alternative to Triton X-100 in the RiboGreen assay, resulting in more accurate quantification of the total mRNA concentration and EE%, as well as making the assay more environmentally friendly. Such improvement could potentially increase the likelihood of identifying therapeutically attractive hard-to-solubilize LNP-mRNA formulations that would be discharged when using Triton X-100 due to their apparent low EE values, as well as ensure more accurate mRNA dosing in both in vitro and in vivo studies. [ABSTRACT FROM AUTHOR]

In this work, different ratios of α/β-Cyclodextrin and carbonyldiimidazole as a cross linker were employed for formulation of α/β-Cyclodextrin Nanosponges wherein 1:6 M ratio was finalized for preparation of Cinnamon Extract/ trans -Cinnamaldehyde loaded Cyclodextrin Nanosponges via freeze drying. β-Cyclodextrin Nanosponges were found to have greater encapsulation efficiency for trans -Cinnamaldehyde (93.30% ± 1.94%) and Cinnamon Extract (35.64% ± 2.08%) compared to α-Cyclodextrin Nanosponges. FTIR spectra of loaded Cyclodextrin Nanosponges did not display any representative peaks of the Cinnamon Extract/ trans -Cinnamaldehyde, confirming inclusion complexation. X-ray Diffraction and Differential Scanning Calorimetry results disclosed the amorphous nature of blank and loaded Cyclodextrin Nanosponges. Cinnamon Extract loaded α/β- Cyclodextrin Nanosponges displayed relatively smaller particle size (447–580 nm) compared to trans -Cinnamaldehyde loaded α/β-Cyclodextrin Nanosponges (630–651 nm). SEM illustrated the porous nature of Cyclodextrin Nanosponges, while TEM depicted the spherical outline of Cinnamon extract-loaded-β-Cyclodextrin Nanosponges with an average diameter of 495 nm. Cinnamon Extract loaded Cyclodextrin Nanosponges displayed greater antioxidant activity while trans -Cinnamaldehyde loaded Cyclodextrin Nanosponges exhibited superior antimicrobial activity. Trans -Cinnamaldehyde loaded β Cyclodextrin Nanosponges demonstrated significant inhibition (47.66 ± 0.51 mm) against Pseudomonas aeruginosa while Cinnamon Extract loaded β Cyclodextrin Nanosponges exerted maximum inhibition zone against Staphylococcus aureus (27.66 ± 0.51 mm). The current research is important as it compares the efficacy of a pure, isolated bioactive compound with a mixture of bioactive compounds available in the Cinnamon extract. Further, combining bioactive loaded Cyclodextrin Nanosponges with a suitable biopolymer can aid in developing active packaging solutions in the form of film/coating/sachet for preserving highly perishable foods which can significantly benefit the food packaging industry. [Display omitted] • Cyclodextrin (CD): Crosslinker was fixed in Cyclodextrin Nanosponges (CD-NS). • α/βCD-NS encapsulated Cinnamon bark extract (CE) and trans -Cinnamaldehyde (t -CMA). • βCD-NS exhibited higher encapsulation efficiency for CE and t -CMA than αCD-NS. • The loaded CD-NSs were amorphous in nature with particle size between 440 and 660 nm. • βCD-NS-CE/ t -CMA exhibited significant antioxidant and antibacterial activity. [ABSTRACT FROM AUTHOR]

The encapsulation efficiency (EE%) reflects the amount of bioactive components that can be loaded into nanoliposomes. Obtaining a suitable nanoliposome stabiliser may be the key to improving their EE%. In this study, three polyphenols were screened as stabilisers of nanoliposomes with high nisin EE%, with curcumin nanoliposomes (Cu-NLs) exhibiting the best performance (EE% = 95.94%). Characterizations of particle size, PDI and zeta potential indicate that the Cu-NLs had good uniformity and stability. TEM found that nisin accumulated at the edges of the Cu-NLs' phospholipid layer. DSC and FT-IR revealed that curcumin was involved in the formation of the phospholipid layer and altered its structure. FT-IR and molecular docking simulations indicate that the interactions between curcumin and nisin are mainly hydrogen bonding and hydrophobic. In whole milk, Cu-NLs effectively protected nisin activity. This study provides an effective strategy for improving the EE% of nanoliposomes loaded with nisin and other bacteriocins. [Display omitted] • Curcumin used as a stabiliser improved the EE% (95.94%) of nisin nanoliposomes. • Curcumin interacts with both phospholipids and nisin. • Nisin aggregates at the edges between the phospholipid layer and aqueous layer • Hydrogen bonding and hydrophobic interactions between nisin and curcumin result in a high EE%. [ABSTRACT FROM AUTHOR]

[Display omitted] The removal of organic solvents during the preparation of biodegradable poly(D,L-lactide-co-glycolide) (PLGA) microparticles by an O/W- solvent extraction/evaporation process was investigated and controlled by diafiltration. Emulsification and steady replacement of the aqueous phase were performed in parallel in a single-vessel setup. During the process, the solidification of the dispersed phase (drug:PLGA:solvent droplets) into microparticles was monitored with video-microscopy and focused beam reflectance measurement (FBRM) and the residual solvent content was analyzed with headspace gas chromatography (organic solvent) and coulometric Karl-Fischer titration (water). Microparticles containing dexamethasone or risperidone were characterized with regard to particle size, morphology, encapsulation efficiency and in-vitro release. Diafiltration-accelerated solvent extraction shortened the process time by accelerating solidification of dispersed phase but reduced the residual dichloromethane content only in combination with increased temperature. Increasing the diafiltration rate increased particle size, porosity, and the encapsulation efficiency of risperidone. The latter effect was particularly evident with increasing lipophilicity of PLGA. A slower and more uniform solidification of end-capped and increased lactide content PLGA grade was identified as the reason for an increased drug leaching. Accelerated solvent extraction by diafiltration did not affect the in-vitro release of risperidone from different PLGA grades. The initial burst release of dexamethasone was increased by diafiltration when encapsulated in concentrations above the percolation threshold. Both porosity and burst release could be reduced by increasing the process temperature during diafiltration. Residual water content was established as an indicator for porosity and correlated with the burst release of dexamethasone. [ABSTRACT FROM AUTHOR]

This study investigated the effects of oil phases on the encapsulation rate, storage stability, and bioavailability of astaxanthin (ASTA) in Pickering emulsions (PEs). Results showed PEs of mixed oils (olive oil/edible tea oil) had excellent encapsulation efficiency (about 96.0%) and storage stability of ASTA. In vitro simulated gastrointestinal digestion results showed the mixed oil PE with a smaller interfacial area and higher monounsaturated fatty acid content may play a better role in improving ASTA retention and bioaccessibility. In vivo absorption results confirmed the mixed oil PE with an olive oil/edible tea oil of 7:3 was more favorable for ASTA absorption. Molecular dynamics simulation showed ASTA bound more strongly and stably to fatty acid molecules in the system of olive oil/edible tea oil of 7:3; and van der Waals force was the main binding force. NMR further proved there really were interactions between ASTA and four main fatty acids. [Display omitted] • Mixed oil PE markedly improved the entrapment efficiency & oral absorption of ASTA. • PE with olive oil/edible tea oil (7:3) was the most effective for ASTA absorption. • Interaction mechanisms between fatty acids and ASTA were unveiled by MD simulation. • The van der Waals force and hydrogen bond were the main interaction forces. [ABSTRACT FROM AUTHOR]

Pomegranate peel polyphenols (PPPs) are recognized as promising food additives due to their diverse bioactivities; however, their application is limited by poor stability. To address this critical issue, three types of PPPs microcapsules were prepared using β-cyclodextrin (CD), whey protein isolate (WPI), and a composite material of CD-WPI through ultrasound treatment (US). Results revealed that ultrasound treatment can enhance the PPPs-wall material interaction, as evidenced by MD simulations. The encapsulation efficiency of CD-WPI-PPPs was 93.73 %, which was significantly higher than that of CD-PPPs and WPI-PPPs (p < 0.05). The degradation rate constant of CD-WPI-PPPs was reduced by 95.83 %, and its t 1/2 was extended by 23-fold compared to that of unencapsulated PPPs. Furthermore, CD-WPI-PPPs exhibited greater DPPH scavenging activity and inhibited polyphenol release during oral and gastric digestion while promoting release during intestinal digestion. These outcomes were attributed to enhanced integrity and interactions between PPPs and composite materials in the microcapsules formed through ultrasound treatment, as supported by SEM images and FT-IR spectra. Consequently, the application of US in the preparation of PPPs microcapsules presents a promising strategy for developing natural nutrient additives for food applications, thereby enhancing the functional properties of food products. • Composite wall materials of CD-WPI can obtain highest encapsulation effect of PPPs. • Ultrasound treatment can enhance the interaction between wall materials and PPPs. • The half-life of CD-WPI-PPPs was extended by 23-fold compared to PPPs. • CD-WPI-PPPs showed higher DPPH scavenging activity after 16 days of storage. • CD-WPI-PPPs can reduce the release of polyphenols in vitro simulated digestion. [ABSTRACT FROM AUTHOR]

Iron is an important micronutrient that cannot be added directly into food products due to potential reactions with the food matrix, impact on color, and taste. Complexed biopolymeric nanocarriers can overcome these challenges particularly for oral delivery of iron, but selecting appropriate biopolymers, their ratio and pH of complexation is very important. In this study, whey protein concentrate (WPC)-pectin nanocomplexes were prepared at different concentrations (WPC 4, 6 and 8%; pectin 0.5, 0.75 and 1%), and pH (3, 6 and 9) to encapsulate iron. The smallest carriers were observed at pH 3; higher pH led to higher zeta potential (zero to −32.5 mV). Encapsulation efficiency of iron in nanocarriers formulated at pH = 3, 6 and 9 were 87.83, 75.92 and 20%, respectively. Scanning electron microscopy revealed the spherical particles at pH 3. To conclude, a WPC to pectin ratio of 4: 1 at pH 3 was the best conditions for loading iron. [Display omitted] • WPC to pectin ratio of 4: 1 at pH 3 was the best complexation conditions. • Encapsulation efficiency (EE) of iron in complexed carriers decreased at higher pH. • An inverse correlation was found between EE and surface color of carriers. [ABSTRACT FROM AUTHOR]

This study focuses on the optimization of Hydrastis canadensis -based nanocarriers in environmental and microbial applications like antibacterial and dye degradation. Hydrastis canadensis (H. canadensis) is loaded into the nanocarrier using a gelation method. Characterization involves pH analysis, UV-VIS spectrophotometry, scanning electron microscopy, Fourier-transform infrared spectroscopy, dynamic light scattering, high-performance liquid chromatography, encapsulation efficiency. Further antimicrobial activity against Staphylococcus aureus and Escherichia coli were tested. Dye degradation was evaluated at concentrations of 1 % of high molecular (HM) and 1.5 % of low molecular (LM) chitosan nanoparticles with both 3C and 1000C concentrations of the drug. The obtained results confirm the presence of chitosan nanocarrier alongside the pure drug in 1 % HM and 1.5 % LM chitosan particles with a notable encapsulation efficiency activity in both 3C and 1000C concentrations. Antimicrobial studies were carried out using the agar well diffusion method and revealed a significant zone of inhibition of 20 mm and 25 mm for E. coli and S. aureus , respectively in chitosan nanocarrier-loaded samples compared to pure drug and chitosan nanocarriers samples. The dye degradation studies of four dyes methylene blue, methylene orange, methylene red, and safranin using both pure drugs and chitosan nanocarrier-loaded drugs showed the highest percentage of degradation (76 %) against methylene blue in the chitosan nanocarrier-drug loaded formulation. These findings cumulatively underscore chitosan nanoparticles can be used as an effective carrier for Hydrastis Canadensis , with enhanced antimicrobial and dye degradation capabilities. Varied concentrations and molecular weights highlight the versatility of the ionotropic gelation method in optimizing drug delivery. Enhanced efficacy of the nanocarrier was evident in the observed zone of inhibition in antimicrobial testing. The substantial degradation percentage in methylene blue emphasizes the formulation's applicability in environmental dye removal processes, with potential avenues for improvement explored through interactions between the chitosan nanocarrier and H. canadensis characteristics. Future investigations may focus on scaling up the optimized formulation for large-scale applications and exploring release kinetics and comprehensive toxicity assessments for a holistic understanding of potential environmental and biomedical implications. [ABSTRACT FROM AUTHOR]

The phytochemical-rich extract obtained from black jamun pulp were encapsulated using vibrating dripping extrusion technique. The utilisation of alginate (AL) with four variations of core-shell material comprising gum Arabic (AL-GA), guar gum (AL-GG), pectin (AL-P) and xanthan gum (AL-X) was engaged to form calcium-alginate based lyophilised jamun extract encapsulated beads. It resulted that among four variations, lyophilised alginate with AL-GG based encapsulated jamun extract filled beads have better physicochemical characteristics and 95% encapsulation efficiency. The results revealed the morphological comparison of each variation. The release behaviour of AL-GG based beads has a higher release of total phenolics (TPC) and total anthocyanin content (TAC). The release kinetics model involving Ritger-Peppas and Higuchi model were applied for release TPC and TAC of all variations of beads. The Ritger-Peppas model was found best suitable in terms of average R2 (0.965) and lowest χ2 (0.0039). The release kinetics study showed that AL-GA based beads followed by AL-GG could also be the best suitable in release behaviour using simulated gastrointestinal fluids at 140–160 min. Overall, results shown the encapsulated Jamun beads have the best agro-industrial efficacy in form of phytochemical compounds based microparticles, holding decent antioxidant potential. [Display omitted] [ABSTRACT FROM AUTHOR]

[Display omitted] • Rhamnolipid can increase the loading ratio of luteolin in SPI nanocomplexes. • Rhamnolipid made the SPI complexes more compact by hydrophobic interactions. • SSPS can cooperate with rhamnolipid to improve the stability of nanocomplexes. Luteolin has anti-inflammatory, antioxidant, and anti-tumor functions, but its poor water solubility and stability limit its applications in foods as a functional component. In this study, the nanocomposites loading luteolin (Lut) with soybean protein isolate (SPI), soluble soybean polysaccharide (SSPS) and/or rhamnolipid (Rha) were prepared by layer-by-layer shelf assembly method, and their properties were also evaluated. The results showed that Rha/SPI/Lut had the smallest particle size (206.24 nm) and highest loading ratio (8.03 μg/mg) while Rha/SSPS/SPI/Lut had the highest encapsulation efficiency (82.45 %). Rha interacted with SPI through hydrophobic interactions as the main driving force, while SSPS attached to SPI with only hydrogen bonding. Furthermore, the synergistic effect between Rha and SSPS was observed in Rha/SSPS/SPI/Lut complex, in consequence, it had the best thermal and storage stability, and the slowest release in gastrointestinal digestion. Thus, this approach provided an alternative way for the application of luteolin in functional foods. [ABSTRACT FROM AUTHOR]

[Display omitted] • The critical pH of structure unfolding of 7S and 11S were pH 10.5 and pH 10.3. • The electrostatic, hydrogen bond and hydrophobic interaction operated in unfolding. • The encapsulation efficiency of protein at critical pH was significantly improved. The pH-shifting process is an effective encapsulation method, and it is typically performed at extreme alkaline pH, which severely limits the application. In this study, we found that there were critical pH for the unfolding proteins during pH-shifting from 7 to 12, and upon the critical pH, physiochemical characteristics of protein greatly changed, leading to a sharp increase of encapsulation of hydrophobic actives. Firstly, the critical pH for β-conglycinin (7S) or Glycinin (11S) unfolding was determined by multispectral technology. The critical pH for 7S and 11S were 10.5 and 10.3, respectively. The encapsulation efficiency (EE) obtained by β-conglycinin-curcumin nanocomposite (7S-Cur) (88.80 %) and Glycinin-curcumin nanocomposite (11S-Cur) (88.38 %) at critical pH was significantly higher than that obtained by pH 7 (7S-Cur = 16.66 % and 11S-Cur = 15.78 %), and both values were close to EE obtained by at 12 (7S-Cur = 95.16 % and 11S-Cur = 94.63 %). The large-scale application of hydrophobic functional compounds will be enhanced by the experimental results. [ABSTRACT FROM AUTHOR]

• Stable Tyr-LPs were prepared by pH-driven method. • Liposome has good encapsulation performance for tyrosol and the EE was up to 94.8 ± 2.5 %. • Tyr-LP has good physical stability. • The bioavailability of tyrosol was improved by liposomes encapsulation. To improve the poor water solubility and oral bioavailability of tyrosol, novel tyrosol liposomes (Tyr-LPs) were prepared by pH-driven method. Fourier transform infrared (FTIR) absorption spectra and X-ray diffraction (XRD) analysis indicated that Tyr-LPs were successfully encapsulated and tyrosol was in an amorphous state in liposomes. When tyrosol content in Tyr-LP was 1.33 mg/ml and the Tyr:LP (mass ratio) = 1:2, favorable dispersibility of Tyr-LP was exhibited, with an instability index of 0.049 ± 0.004, PDI of 0.274 ± 0.003, and the EE of 94.8 ± 2.5 %. In vivo pharmacokinetic studies showed that after oral administration of tyrosol or Tyr-LP (Tyr:LP = 1:2), concentration-versus-time curve (AUC 0–720mins) and maximum concentration (C max) values of Tyr-LP was respectively 1.5-fold (P < 0.01) and 2.25-fold (P < 0.01) higher than tyrosol, which indicated that the oral bioavailability of tyrosol was effectively improved in Tyr-LPs. Our study thereby provides theoretical support for the application of Tyr-LP for optimal delivery of tryosol. [ABSTRACT FROM AUTHOR]

• RSM was used to optimize prepration for evening primrose oil nanoemulsions (EPO NEs). • The properties of EPO NEs were dependent on the type of surfactants used. • EPO NEs exhibited nearly Newtonian fluid behavior. • EPO NEs showed high encapsulation efficiency and negligible cytotoxicity. In this study, evening primrose oil (EPO), recognized for its bioactivity and safety, played a pivotal role as a primary component in the production of nanoemulsions (NEs) through a combination of homogenization and ultrasonic nano-emulsification technology. The significance of EPO NEs lies in their potential impact on various aspects of health and well-being. The research aimed to explore the physicochemical properties, encapsulation efficiency, and in vitro biocompatibility of the resulting EPO NEs by employing three distinct surfactants: dioctadecyl dimethylammonium bromide (D+), dihexadecyl phosphate (D−), and saponin (Sn) for stabilization. Response surface methodology (RSM) was used to optimize the preparation parameters of the NEs. The physicochemical properties of NEs were assessed using various techniques, including dynamic light scattering, transmission electron microscopy, differential scanning calorimetry, fluorescence polarization spectroscopy, and viscometer measurements. The encapsulation efficiency of the NEs was evaluated through the use of quercetin. Furthermore, the in vitro biocompatibility of the NEs was assessed via a cell viability assay. RSM effectively determined the optimal ultrasonication operation parameters, including time and amplitude, to achieve EPO NE with the desired size and distribution. The thermal phase change and intra-particle fluidity of NEs decreased as the oil/surfactant ratio increased and varied with the type of surfactant used. Furthermore, EPO NE exhibited nearly Newtonian fluid characteristics. Most importantly, all NEs demonstrated excellent in vitro biocompatibility and high encapsulation efficiency. In conclusion, the high potential of EPO NEs underscores their pivotal role in advancing drug delivery systems. [Display omitted] [ABSTRACT FROM AUTHOR]

• Cinnamaldehyde-nanostructured lipid carriers and nanoemulsion reduced nitrite in sausage. • Nanoemulsion and NE + nitrite indicated the lowest oxidative and microbial features. • CA/NLC/NE + nitrite indicated better color quality and higher oxymyoglobin content. • NE and NLC (+nitrite) were favored by the panelists in terms of color and flavor. This study aimed to produce cinnamaldehyde (CA)-loaded nanostructured lipid carriers (NLC) and nanoemulsion (NE) to replace nitrite in sausage. The NLC and NE droplet sizes were 132 and 116 nm with encapsulation efficiency of 98 and 96 %, respectively. In in vitro antimicrobial assessment, the free CA and NE showed higher microbial activity against S. aureus and E. coli than NLC. Meanwhile, NE showed a faster release profile for CA than NLC. Among the samples, NE and NE + nitrite indicated the lowest peroxide value (3.7 ± 0.1), TVBN amount (8.6 ± 0.2), acidity (0.3 ± 0.02), microbial quality (against E. coli , C. perfringens , lactic acid bacteria, psychrophilic bacteria, total mold and yeast, and total viable counts), and sensory attribute, while the NE + nitrite sample exhibited better color properties and higher oxymyoglobin content (5–10 % higher). Therefore, NE + nitrite can be the best choice due to supporting the different quality parameters of sausage. [ABSTRACT FROM AUTHOR]

• SPI and OKGM with high oxidation degree facilitated encapsulating walnut oil. • Physicochemical properties of microcapsules were enhanced with increasing oxidation degree of OKGM. • Fatty acids released from microcapsules with SPI and highly OKGM was the highest. • The binding energy of system decreased with increasing oxidation degree of OKGM. This study investigated the effect of the oxidation degrees of oxidized konjac glucomannan (OKGM) on the encapsulation efficiency (EE), physicochemical and in vitro digestive properties of soy protein isolate (SPI)-based microcapsules walnut oil using experimental and computational approaches. Microcapsules had the highest EE when the ratio of OKGM and SPI to oil was 2.5:1. With increasing the oxidation degree of OKGM, the EE of microcapsules was increased and the hygroscopicity was decreased. Molecular dynamics simulation results showed that SPI/oil/highly OKGM had relatively low binding energy (−4.03 × 106 kJ/mol) and strong electrostatic interactions, which may contribute to a higher EE and lower hygroscopicity of microcapsules, respectively. The oxidative stability of the oil was markedly improved by SPI and OKGM, and microcapsules prepared with SPI and highly OKGM had the highest in vitro digestion. This study provided theoretical support for broadening the application of microcapsules prepared with SPI and OKGM. [ABSTRACT FROM AUTHOR]

[Display omitted] • ω-3 MLCTs microcapsules were synthesized using diverse homogenization method. • Encapsulation efficiency of soy protein-based MLCTs microcapsules was 94.56%. • Microcapsules showed excellent water solubility contributed to further application. • Microcapsules exhibited a spherical shape with the smooth surface. Recently, MLCTs have attracted considerable attention as a potential alternative to traditional oils due to their suppressive effect on fat accumulation and insulin sensitivity. In this study, the microcapsules of MLCTs with superior performance were fabricated through different homogenization processes to overcome the limitations of ω-3 medium- and long- chain triacylglycerols (MLCTs), including poor stability and prone oxidation. Additionally, the impact of various homogenization techniques, namely, high-pressure, ultrasound, and cavitation jet, on the particle structure, encapsulation efficiency, and oxidation stability of microcapsules (MLCTs) was investigated. The MLCTs microcapsules fabricated through high-pressure homogenization had a smaller particle size of 295.12 nm, lower PDI of 0.24, and a higher zeta-potential absolute value of 32.65, which significantly improved their dispersion and encapsulation efficiency, reaching 94.56 % after the spray-drying process. Furthermore, the low moisture content and superior storage stability of MLCTs microcapsules have the potential to serve as carriers of liposoluble actives. [ABSTRACT FROM AUTHOR]

Ionotropic gelation is a low-cost, easy and green microencapsulation technique. However, the encapsulation of highly soluble compounds is challenging because of the wide loss of material into the external water phase by passive diffusion and the consequent low encapsulation efficiency. In this work an important increase of encapsulation efficiency for Thymus vulgaris L. aqueous extract in alginate-based microparticles has been obtained. A formulation with the proper thyme extract/alginate ratio (30:70) was used as reference and then optimized by adding different co-carrier excipients. Microparticles obtained by dropping a solution containing thyme extract and alginate into a chitosan/calcium-chloride/acid acetic solution lead to a high encapsulation efficiency (70.43 ± 5.28 %). After drying, microparticles had a particle size of 1096 ± 72 μm, 20.087 ± 1.487 % of extract content, 6.2 % of residual water, and showed a complete release of thyme extract within one hour. Combining alginate and chitosan as polymeric co-carrier was a valuable option for efficiently encapsulating an aqueous extract by ionotropic gelation. [ABSTRACT FROM AUTHOR]

Enzyme encapsulation has emerged as a promising strategy for protecting enzymes against denaturation under harsh conditions. Alginate encapsulation using a dripping and gelation method is a common technique for encapsulating enzymes, however, the encapsulation efficiency is often limited due to the quick diffusion of water-soluble enzymes into the gelation bath. Herein, we report a novel post-loading enzyme encapsulation method with a 100% encapsulation efficiency and a high enzyme loading. We demonstrate a 20-fold enzyme thermal stability improvement upon encapsulation. Furthermore, we investigate the effects of alginate pore size, enzyme concentration, and enzyme distribution on the thermal stability of encapsulated enzyme using both experimental and computational methods, elucidating the mechanism underlying the stability improvement of the encapsulated enzyme. Additionally, the encapsulated enzyme demonstrates successful release under simulated gastric conditions. This highly efficient enzyme encapsulation system, utilizing food-grade encapsulation materials and an environmentally friendly synthesis approach, holds great promise for various applications in the food industry. A two-step post-loading enzyme encapsulation approach using alginate crosslinking achieves 100% enzyme encapsulation efficiency and over 90% enzyme thermal stability. [Display omitted] • Phytase thermal stability was improved by encapsulation using alginate beads. • A 20-fold enzyme thermal stability improvement was observed after encapsulation. • The major protection mechanism of enzyme thermal stabilization is confinement. • The encapsulation efficiency was optimized to 100% using a post-loading method. [ABSTRACT FROM AUTHOR]

In order to load fish oil for potential encapsulation of fat-soluble functional active substances, fish oil-loaded multicore submillimeter-sized capsules were prepared with a combination method of three strategies (monoaxial electrospraying, chitosan-tripolyphosphate ionotropic gelation, and Tween blending). The chitosan-tripolyphosphate/Tween (20, 40, 60, and 80) capsules had smaller and evener fish oil cores than the chitosan-tripolyphosphate capsules, which resulted from that Tween addition induced smaller and evener fish oil droplets in the emulsions. Tween addition decreased the water contents from 56.6 % to 35.0 %–43.4 %, increased the loading capacities from 10.4 % to 12.7 %–17.2 %, and increased encapsulation efficiencies from 97.4 % to 97.8 %–99.1 %. In addition, Tween addition also decreased the highest peroxide values from 417 meq/kg oil to 173–262 meq/kg oil. These properties' changes might result from the structural differences between the chitosan-tripolyphosphate and chitosan-tripolyphosphate/Tween capsules. All the results suggested that the obtained chitosan-tripolyphosphate/Tween capsules are promising carriers for fish oil encapsulation. This work also provided useful knowledge to understand the preparation, structural, and physicochemical properties of the chitosan-tripolyphosphate capsules. [ABSTRACT FROM AUTHOR]

Effects of coating materials on emulsion, physical (moisture content, water activity, particle density, bulk properties, wettability and product yield) and chemical (total and surface phenolic content and encapsulation efficiency) properties of encapsulated propolis, rich in bioactive substances, were investigated with two different methods (spray and freeze drying). Emulsion properties have an effect on physical and chemical properties of the final product, which varied according to the encapsulation method used and the differences in coating materials combination. These variations resulted from the differences in the heat and mass transfer mechanism of the processes. The product yield of the freeze dryer experiments was generally higher than the spray dryer experiments; since the product loss in the freeze dryer method was only due to the adhesion of the emulsions to the equipment's glass plate surface. Encapsulation efficiency varied in a narrow range for both drying methods and these results were above 95%. High microencapsulation efficiency values of powders proved that the encapsulation processes are carried out effectively. [Display omitted] • Propolis was encapsulated by spray and freeze drying method. • The effects of emulsion properties on propolis powders properties were investigated. • The propolis powder properties was highly affected by encapsulation process. • The effect of coating material combination related with product properties. • The behavior of different coating materials in the emulsion was evaluated. [ABSTRACT FROM AUTHOR]

Different treatments of autoclaving, pullulanase debranching and/or ultrasound were applied to prepare debranched lentil starch (DBLS). Their fine structures can affect the retrogradation patterns of DBLSs, which consequently could affect their potential use as delivery carrier of sensitive bioactive compounds. An attempt was made to use these DBLSs as wall materials to encapsulate rutin, aiming to improve the bioaccessibility, meanwhile to enhance the aqueous solubility and stability of rutin molecules. Their encapsulation efficiency, structural characteristics, thermal stability, morphological features, antioxidant activity and in vitro release behavior under simulated upper gastrointestinal tract environment were evaluated. The results suggested that rutin was dispersed in the DBLS polymer matrix, showing the amorphous nature that further authenticates the encapsulation and entrapment of rutin. The structural analyses of microparticles revealed that rutin could interacted with DBLS biopolymer chains by hydrogen bonds, making the starch molecular chains less susceptible to interact with themselves for reordering. The encapsulation efficiency was found to be in an opposite trend with those values obtained for relative crystallinity, melting enthalpy, degree of order/double helices of DBLS wall materials before encapsulation. The release rate results indicated that DBLS carrier with lower M w , DP n and higher molecular order was beneficial for the slower release of rutin encapsulated in the microparticles. Unlabelled Image • Rutin was dispersed in DBLS polymer matrix, showing the amorphous nature. • The average crystallite size of microparticles ranged from 107.38 to 246.40 nm. • Encapsulation efficiency was in an opposite trend with relative crystallinity of DBLS. • DBLS carrier with higher molecular order was beneficial for slower release of rutin. [ABSTRACT FROM AUTHOR]

• Emulsion based delivery system was optimized with WPC80 & lactose. • Core (35%) had carotenoids extracted from carrot pomace in flaxseed oil. • 33 factorial experiment and 3-way ANOVA were robust tools for optimization. • Encapsulation efficiency of CREm was 92.745 ± 0.384%. • Microstructure revealed spherical emulsion with intact coat & no fissures/cracks. The juice expelled from carrot, a globally produced root vegetable, leaves behind carrot pomace (a bio- and horticultural waste) which is potentially rich source of micro-nutrients and carotenoids. However, it is discarded as waste or used as animal feed. It holds potential to be channelized to food chain by a couple of technological interventions. In this regard, present work was aimed at preparing stable emulsion based delivery system for 'green' carotenoids extracted from carrot-pomace in flaxseed oil (a green solvent), and at maximizing the amount of core material so that the resultant emulsion can potentially be used as a source of both carotenoids and omega-3 fatty acid of flaxseed oil origin. The study used natural emulsifier. Preparation of oil-in-water emulsion was optimized using 33 factorial experiment by varying levels of extract containing carotenoid (30–40%), whey protein concentrates (WPC-80) and lactose. The optimized emulsion (CREm) was selected on the basis of particle size, zeta potential, color values (L*, a*, b*) and viscosity statistically analyzed via three-way ANOVA using Proc GLM of SAS 9.3 (described in detail in this paper); the respective values of these parameters being 120.03 ± 8.20 nm, −16.57 ± 0.49 mV, 75.11 ± 0.04, 9.66 ± 0.32, 50.29 ± 0.62, and 0.124 ± 0.0115 Pa.s for CREm. CREm contained 35% flaxseed oil, 10% WPC-80 and 5% lactose and showed good centrifugal and gravitational stability (15 days). It was analyzed for total carotenoid content, antioxidant activities (ABTS (2,2-azinobis-(3-ethylbenzthiazoline-6sulfonic acid), DPPH (2,2-Diphenyl-1-picrylhydrazyl) and FRAP (Ferric reducing antioxidant power assay)) and microstructure. [ABSTRACT FROM AUTHOR]

Injectable, long-acting drug delivery systems provide effective drug concentrations in the blood for up to 6 months. Naltrexone-loaded poly(lactide- co -glycolide) (PLGA) microparticles were prepared using an in-line homogenization method. It allows the transition from a laboratory scale to scale-up production. This research was designed to understand how the processing parameters affect the properties of the microparticles, such as microparticle size distributions, surface and internal morphologies, drug loadings, and drug release kinetics, and thus, to control them. The in-line homogenization system was used at high flow rates for the oil- and water-phases, e.g. , 100 mL/min and 400 mL/min, respectively, to continuously generate microparticles. A high molecular weight (148 kDa) PLGA at various concentrations was used to generate oil-phases with a range of viscosities and also to compare with a 64 and 79 kDa at a single, high concentration. The uniformity of the microparticles was found to be related to the viscosity of the oil-phase. As the viscosity of the oil-phase increased from 52.6 mPa∙s to 4046 mPa∙s, the span value (a measure of uniformity) increased from 1.24 to 3.1 for the microparticles generated at the homogenization speed of 2000 RPM. Increasing the PLGA concentration from 5.58% to 16.85% showed a corresponding rise in the encapsulation efficiency from 74.0% to 85.8% and drug loading (DL) from 27.4% to 31.7% for the microparticles made with the homogenization speed of 2000 RPM. These increases may be due to a faster shell formulation, enabling PLGA microparticles to entrap more naltrexone into the structure. A higher DL, however, shortened the drug release duration from 56 to 42 days. The changes in morphology of the microparticles during different phases of the in vitro release study were also studied for three types of microparticles made with different PLGA concentrations and molecular weights. As PLGA microparticles went through structural changes, the surface showed raisin-like wrinkled morphologies within the first 10 days. Then, the microparticles swelled to form smooth surfaces. The in-line approach produced PLGA microparticles with a highly reproducible size distribution, DL, and naltrexone release rate. Unlabelled Image [ABSTRACT FROM AUTHOR]

The essential fatty acids (EFAs) are recognized as functional oils for humans as they possess nutritional and pharmaceutical benefits and can promote whole-body health in different ways. This review describes and classifies different types of EFAs, gives an overview of the spray drying process alongside its probable challenges for encapsulation of functional oils. Also, various used wall materials, and the effects of the process conditions on the encapsulation efficiency of functional oils have been discussed. Moreover, it focuses on the spray drying encapsulation of functional oils derived from marine and plant-based sources in recent years (2016-2019), and the fortification of different foods with encapsulated functional oils. Protecting EFAs through efficient methods such as spray drying encapsulation and enriching the various foods with encapsulated functional oils is an emerging field, which has drawn lots of attention these days. The wall materials (carriers) and spray drying conditions are two major influential factors that can easily affect the properties of final produced powders. Image 1 • Research Highlights: • The essential fatty acids (EFAs) are recognized as functional oils for humans. • Protecting EFAs through spray drying encapsulation is an emerging field. • There are some challenges for encapsulation of functional oils by spray drying. • Encapsulated functional oils can be applied for the fortification of different foods. [ABSTRACT FROM AUTHOR]

This work deals with assessing the efficient performance of sodium caseinate (SC) as protein-based drug delivery system of niacin (NA) than carboxymethyl cellulose (CMC). In this respect the hydrogels from complexation of chitosan with sodium caseinate (SC/Ch) or sodium carboxymethyl cellulose (CMC/Ch) were prepared. The Synthesized NA free and loaded hydrogels were characterized by many techniques for examining the interaction, morphology, swelling, encapsulation efficiency (EE) and loading (L) % of niacin, as well as cytotoxicity study. The finding data showed the promising behavior of SC/Ch hydrogel than CMC/Ch hydrogel, toward the amount of loaded NA (95.6%) and in vitro slow sustained release up to 24 h. Whereas, the entrapment efficiency of the CMC/Ch to nicotinic acid was reached 85.6%, and it possessed highly initial burst release followed by a slower release up to 24 h. At pH 7.4 (simulated intestinal fluid) both hydrogels provided higher level of releasing profile to NA than pH 2.1 (gastric fluid). The NA release from hydrogels followed Fickian and non-Fickian diffusion mechanism according to pH 7.4 and 2.1, respectively. It is interesting to note that, the data obtained are higher than those obtained from literature reported hydrogel, e.g., poly (2-hydroxyethyl methacrylate). Neutral red uptake and lactate dehydrogenase assays confirmed both hydrogels have good biocompatibility and could be used as nontoxic drug delivery system. So, we recommended SC/Ch hydrogel as an effective controlled niacin drug delivery system with reducing systemic side effects and improved intestinal targeting efficiency. • Assessment of protein- and cellulose-chitosan hydrogels as drug delivery systems • Effective of sodium caseinate–chitosan hydrogel for slow release of niacin drug • Mechanisms of diffusion and erosion coexisted for the release control of niacin. • The SC/Ch hydrogel possessed interesting feature for reducing systemic side effects. • The SC/Ch hydrogel provided improvement in intestinal targeting efficiency. [ABSTRACT FROM AUTHOR]

This research aims to optimize the parameters for the production of a stable nanoemulsion containing a mixture of essential oils (EOs) with a surfactant blend (Tween and Span 80) and assess its antimicrobial potency against spoilage bacteria and foodborne pathogens. The impact of a surfactant blend's hydrophilic-lipophilic balance (HLB) as well as surfactant:oil ratio was investigated based on the mean particle size (z-average) and polydispersity index (PDI). Results showed HLB value of 12 and a ratio of surfactant to oil at 0.75:1 exhibited an emulsion with the smallest z-average and PDI. Following this, a response surface methodology (RSM) employing central composite design (CCD) was utilized to formulate an optimal nanoemulsion using the microfluidization (MF) technique. The RSM revealed that the microfluidizer pressure of 15,000 psi and 5 cycles produces a z-average of 38.11 nm, PDI of 0.27, ζ-potential of 37.8 mV, and EE of 83.8%. The comparison between the experimental and anticipated results of the optimized nanoemulsion revealed no significant differences (p > 0.05). The optimal nanoemulsion displayed excellent stability during 30 days of storage at both 4 and 30 °C compared to 5 days for coarse emulsion. The nanoemulsion exhibited potent antimicrobial activity, showing minimum inhibitory concentration (MIC) values in the range of 0.019 to 0.156 µL/mL, surpassing the antimicrobial efficacy of the coarse emulsion, which had MIC values between 0.039 to 0.312 µL/mL. Thus, this study emphasized the efficacy of RSM design in developing an optimal nanoemulsion with enhanced antimicrobial properties using EOs, making it a promising natural food preservative. [Display omitted] [ABSTRACT FROM AUTHOR]

Tanshinone compounds are secondary metabolites which their application in food and pharmaceutical industry is limited due to the low solubility in water and sensitivity to heat. This study aimed to develop a novel biopolymer nanocarriers system based on pectin/zein for the encapsulation of tanshinone compounds using the anti-solvent precipitation method. The concentration of pectin and mass ratio of tanshinone/zein in the final formulation of nanoparticles were optimized. According to the results, a pectin concentration of 1 g/L and a tanshinone/zein ratio of 0.1:1 g/g were considered the optimal nanoparticle formulation. The resulting nanoparticles exhibited a spherical core-shell structure, with approximate values for size, zeta potential, TSI, and encapsulation efficiency of 132 ± 0.002 nm, −38.6 ± 0.019 mV, 0.600 ± 0.084, and 79.41 ± 0.62 %, respectively. The FTIR test confirmed the presence of hydrophobic, hydrogen, and electrostatic interactions among the constituents within the nanoparticles. Additionally, XRD and DSC tests verified the amorphous nature of the nanoparticles. Morphological examination conducted through TEM, and SEM revealed the characteristics of the resulting nanoparticles. Furthermore, this carrier system significantly enhanced the solubility of tanshinone compounds in water. • A novel tanshinone nanocarriers was fabricated using zein and pectin. • The hydrophobic and electrostatic interactions induced the formation of T/Z/P NPs. • The T/Z/P NPs had spherical morphology and uniform diameter about 132 nm. • T/Z/P NPs improved the solubility of tanshinone in the aqueous phase. • XRD and DSC analysis showed the amorphous structure of tanshinone in the T/Z/P NPs. [ABSTRACT FROM AUTHOR]

• Polyglycerol polyricinoleate affects stability by changing the viscosity and interfacial layer of emulsion. • The effects of different homogenization methods on the microstructure and stability of emulsion were analyzed. • The microscopic motion and diffusion of emulsion droplets were analyzed by the diffusing wave spectroscopy (DWS). • The droplet coalescence and Ostwald ripening curing behavior of water-in-oil emulsion during storage were analyzed. The aim of this study was to investigate the effect of the preparation methods and the concentration of polyglycerol polyricinoleate (PGPR) on the stability of the water-in-oil (W/O) emulsion. By comparing two different emulsions preparation methods, high-speed shear (16000 rpm) and high-pressure homogenization. We were found that high-speed shear treatment could reduce the particle size of the emulsion more effectively, thus significantly improving the stability of the emulsion. In addition, the effect of PGPR concentration on the stabilization mechanism of the emulsion was also discussed. The results showed that when the concentration of the PGPR was increased from 2 % to 6 %, it effectively prevented emulsion droplets polymerization and improved the stability of the emulsion. When the PGPR concentration was further increased to 10 %, the physical properties of the emulsion were mainly characterized by an increase in viscosity, which further enhanced the stability of the emulsion. In experiments involving the encapsulation of VB12, the encapsulation efficiency (EE) exceeded 95 %, and the retention efficiency (RE) exceeded 85 % even after 21 days of storage, demonstrating excellent stability. This study provided new insights into the preparation of stable water–oil emulsions, particularly regarding the efficient encapsulation and long-term stability of nutrients, and held significant application value for the food and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

The composite nanoparticles labeled as ZCP/C–CNC were synthesized by the combination of zein colloidal nanoparticles (ZCP) and carboxylated cellulose nanocrystals (C–CNC). The effects of the mass ratio of ZCP to C–CNC on the particle size, polydispersity index, ζ-potential, surface wettability and microstructure of ZCP/C–CNC were studied. The ZCP/C–CNC were used to stabilize cinnamon essential oil (CEO). The effects of ZCP/C–CNC on the properties of Pickering emulsions were investigated, including the interfacial tension, stability, encapsulation efficiency (EE), interfacial structure and antibacterial activity. With increasing of ZCP, the average particle size of ZCP/C–CNC firstly decreased and then increased, which was the smallest (196 nm) when the mass ratio of ZCP to C–CNC was 1. Scanning electron microscopy (SEM) showed that the structure of composite nanoparticles was featured that C–CNC layers wrapped ZCP. Confocal laser scanning microscope (CLSM) showed that CEO was effectively encapsulated by ZCP/C–CNC. When the mass ratio of ZCP to C–CNC was 1, the three-phase contact angle of the nanoparticle was 89.65°, showing the best surface wettability. And the CEO Pickering emulsion stabilized by this nanoparticle exhibited the smallest average particle size. It also showed the best stability and the best antibacterial activity against E. coli , S. aureus and S. putrefaciens. The EE of composite nanoparticles for CEO was significantly higher than that of pure ZCP or C–CNC particles, which all exceeded 91%. The Pickering emulsions stabilized by ZCP/C–CNC provided a promising alternative for the delivery of antimicrobial essential oils in the food, active packaging material and other related industries. [Display omitted] • The ZCP/C–CNC composite nanoparticles were synthesized by zein and C–CNC. • The structure of ZCP/C–CNC was featured that C–CNC wrapped zein nanoparticles. • The CEO Pickering emulsions were stabilized by ZCP/C–CNC composite nanoparticles. • The F1C1Zem showed the smallest average drop size and best storage stability. • The ZCP/C–CNC was beneficial to improve the encapsulation efficiency of CEO. [ABSTRACT FROM AUTHOR]

The focus of this study was on the development, physicochemical characterisation and evaluation of the antioxidant activity of cape gooseberry calyx extract loaded into nanoliposomal systems. Various nanoliposomes were prepared and optimised using the ethanol injection method and characterised based on particle size, polydispersity and zeta potential measurements. Subsequently, the encapsulation efficiency and in vitro release profile of the natural antioxidant extract (NAE) were evaluated, and its antioxidant activity was assessed using the oxygen radical absorbance capacity assay. The results revealed that NAE-loaded nanoliposomes described desired quality features (e.g., particle size of < 200 nm, polydispersity index of < 0.3, zeta potential of > −40 mV and encapsulation efficiency of ∼70%). Furthermore, it was found that NAE release is controlled by various stages, and its antioxidant activity improves by around 30% when loaded into the nanoliposomes, suggesting that it could be a promising antioxidant functional raw material. • The major antioxidant compound of the cape gooseberry extract is rutin flavone. • The optimized method allows developing nanoliposomes with desired quality characteristics. • Nanoliposomal systems encapsulate around 70% of the Natural Antioxidant Extract. • Natural antioxidant extract release is complex and given by a four-stage mechanism. • Nanoliposomes describe appropriate stability and remain the antioxidant effect over time. [ABSTRACT FROM AUTHOR]

In this study, it was aimed to prepare and characterize double (W 1 /O/W 2) emulsions for encapsulation of ferric chloride within the internal aqueous phase (W 1). The primary (W 1 /O) emulsion to be used in double emulsion was examined for oxidative stability and whey protein isolate was found effective in improving oxidation stability. The double emulsions were prepared with different primary emulsion:external water phase (W 1 /O:W 2) ratios as 40:60, 30:70 and 20:80; the emulsions were characterized in terms of droplet size, encapsulation efficiency, rheology, creaming stability and in vitro iron bioaccessibility. The emulsion with 40:60 ratio had the highest viscosity and encapsulation efficiency whereas it had the lowest creaming index and droplet size. It was also obtained that iron bioaccessibility increased as the ratio of W 2 phase increased and the double emulsion with 20:80 ratio showed the highest bioaccessibility (52.97 ± 0.89%). This study may enable the use of double emulsion encapsulation in the enrichment of food products with iron. • Ferric chloride was encapsulated in the internal phase of W/O/W emulsion. • Whey protein isolate was found as effective for improving oxidation stability. • Creaming stability and encapsulation efficiency were found to be highest for 40:60 ratio. • The highest iron bioaccessibility (52.97 ± 0.89%) was observed for 20:80 ratio. [ABSTRACT FROM AUTHOR]

Microspheres prepared by the modified HIP complex strategy highly improved peptide encapsulation within the PLGA matrix. With further pore healing, the initial burst of octreotide acetate from the microspheres was also greatly inhibited. • The HIP complex was formed between octreotide acetate and ion-pairing agent. • The HIP complex was encapsulated into the microspheres using the S/O/W method. • With self-healing, the pores within the microspheres were effectively healed. • A more satisfactory single phase release profile was observed in vitro and in vivo. Poor encapsulation and high initial burst were two major obstacles for the water-soluble peptide drug loaded microspheres preparation using the industrial emulsification method. In the present study, we hypothesized that the hydrophobic ion-pairing (HIP) complex strategy with a further healing of the pores within the microspheres may improve drug encapsulation and initial burst release. DSS was chosen as the most suitable one among the three test ion-pairing agents (SDS, DSS and STC) due to its high binding efficiency with drug and reversible dissociation capacity in presence of counter ions. The formation of HIP complex between octreotide acetate and DSS successfully reversed the highly water-soluble nature of the drug. A specific S/O/W method was adopted to encapsulate such drug containing HIP complex. The encapsulation efficiency of the drug was greatly improved compared with the conventional W1/O/W2 method (from 44% to 90%). Under the optimal healing conditions (the healing time 6 h, temperature 40 °C and 4% DEP content), the pores within the microspheres were effectively healed. Initial burst amount of octreotide acetate in S/O/W microspheres decreased to 3.56%. The pore healing effect was further confirmed by the scanning electron microscopy and fluorescence microscopy results. In the process of testing the drug release performance of such new strategy in vitro and in vivo, a more satisfactory single phase release profile with sustained and steady drug release was observed. These results suggested that the modified HIP strategy could be a promising platform for water-soluble peptide encapsulation with high encapsulation efficiency, low initial burst and stable drug release mechanism. [ABSTRACT FROM AUTHOR]

• Eugenol (E) was efficiently encapsulated by spray-drying using WP or LE. • Chitosan incorporation reduced the emulsion stability and encapsulation efficiency. • A fast release of E in different food simulants was observed for every encapsulant. • Antioxidant capacity was coherent with the E content inside the powder particles. • Antimicrobial effect (E. coli and L. innocua) was coherent with the powder E content. The encapsulation of eugenol (E) by spray-drying using whey protein (WP) or soy lecithin (LE) and maltodextrin in combination with oleic acid (OA) and chitosan (CH) was analysed in order to obtain antioxidant and antimicrobial powders for food applications. Formulations with only WP or LE showed higher encapsulation efficiencies (EE) (95–98%) and antibacterial effect against E. coli and L. innocua due to their greater E load. Incorporation of OA or CH promoted lower EE, which negatively affected the antimicrobial and antioxidant activities of the powders. Furthermore, the addition of CH implied less thermal protection against the E losses. The eugenol release was not notably affected by pH or polarity of the food simulant, but the release rate significantly decreased when incorporating OA and CH. The E-LE formulations better retained the eugenol than E-WP powders when heated above 200 °C, this being relevant for the powder inclusion in thermally treated products. [ABSTRACT FROM AUTHOR]

• α-Tocopherol nanocapsules loaded into carboxymethyl cellulose (CMC) film. • The levels of polycaprolactone, α-tocopherol and lecithin were selected as independent variables. • The encapsulation efficiency and release patterns of nanocapsules were determined. • The optimized levels were 75.33 mg of PCL, 200 mg of α-tocopherol, and 2 mg mL−1 of lecithin. • CMC films containing 70% nanocapsules showed the highest antioxidant attributes. The aim of the current study was to optimize vitamin E (α-tocopherol) loaded polycaprolactone (PCL) nanocapsules into the carboxymethyl cellulose (CMC) film. For this purpose, polycaprolactone concentration, α-tocopherol level, and lecithin concentration were selected as independent variables, and encapsulation efficiency and nanocapsule size designated as dependent variables. The organization of experiments was carried out using response surface methodology and Box-Behnken design. Afterwards, the α-tocopherol nanocapsule loaded CMC films subjected to antioxidant test, release test and release kinetics. From the results, the encapsulation efficiency of films containing 30–70% α-tocopherol nanocapsules was varied between 88.43 and 99.66%. The enlarged nanocapsules with the enhanced encapsulation efficiency were obtained by increasing in PCL concentration, while increase in α-tocopherol concentration caused a drop in encapsulation efficiency accompanied by distended particle size. The variation in lecithin concentration wasn't significantly (p < 0.05) impact on encapsulation efficiency and nanocapsule size. The desirability function suggested the following concentrations of variables: 75.33 mg of PCL, 200 mg of α-tocopherol, and 2 mg mL−1 of lecithin. Antioxidant potential of CMC films followed a linear pattern with the addition of more α-tocopherol nanocapsules, so that films containing 70% nanocapsules showed the highest radical scavenging activity of 68.85%. [ABSTRACT FROM AUTHOR]

The aim of this study was to investigate the influence of end group of poly(lactic- co -glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To this end, doxycycline hyclate (DOX) was selected as a model drug, and PLGA (molecular weight: 17 and 44 kDa) with either an acid or ester end group were electrosprayed with DOX. The processing parameters were optimized to obtain microspheres comparable in size. Drug loading efficiency and release profile were determined by the high-performance liquid chromatography-ultraviolet detection (HPLC-UV) method. PLGA polymers or drug-loaded microspheres were characterized before and after exposure to phosphate buffer saline at 37 °C regarding the wettability of polymers, pH changes of the buffer, molecular weight of PLGA and morphology of the microspheres. The acid end group of PLGA microspheres brought about lower encapsulation efficiency and faster DOX release rate in our study, indicating that different hydrophilicity of polymer and degradation speed were the main reasons causing a difference in encapsulation efficiency and release profile. In addition, DOX released from the PLGA microspheres was active by showing antibacterial effects against Porphyromonas gingivalis as measured using a zone of inhibition test, and varying the end groups showed no impact on the antibacterial efficacy. This study demonstrated that the end group of PLGA can be used as a new tool to regulate drug encapsulation efficiency and release rate to meet different clinical drug delivery requirements. [ABSTRACT FROM AUTHOR]

Abstract This study aimed to apply mixed drug–surfactant micelles to enhance the solubility and reduce the cytotoxicity of poorly water-soluble active pharmaceuticals. Nanosized drug–surfactant formulations were prepared using antihistaminic cationic drug diphenhydramine hydrochloride (DCP) with anionic sodium deoxycholate (SDC) and non-ionic transglycosylated stevia (Stevia-G) surfactants. Surface tension and fluorescence methods were used to evaluate mixed micellization in an aqueous medium. The negative interaction parameters (β m) values of the drug-surfactant mixed micelle showed the strong attractive interactions of DCP with SDC and Stevia-G. The applicability of the drug-surfactant mixed micelle for enhancing the binding constant (logK b), partition coefficient (logK m) and molar solubilization ration (MSR) of the non-steroidal anti-inflammatory drug, ethenzamide (ETZ) was evaluated. The %EE of ETZ in DCP at α DCP = 1.0 was higher than that of SDC and Stevia-G, reflecting the formation of a hydrogen bond between ETZ and DCP. The controlled released of ETZ in PBS at pH 7.4 was approximately 10% from both mixed micelles after 55 h. In addition, cell viabilities in the presence of ETZ and SDC were reduced to 48% and 40% at 0.5 and 3.0 mM, respectively, indicating their high cytotoxicity. By contrast, cell viability was >90% in the presence of mixed micelles of DCP–SDC and DCP–Stevia-G with α DCP = 0.9 at 3.0 mM, suggesting low cytotoxicity. These data show that nanosized mixed micelles facilitate the passage of these two drugs through the cell membranes, thereby leading to their improved uptake into the target cells. Graphical abstract Unlabelled Image Highlights • Developed formulation to form the nanosized mixed micelle of drug-surfactants. • Enhanced binding of ETZ using drug-surfactants mixed micelle. • Encapsulation efficiency and solubilization increased at a high mole fraction of α DCP 0.9. • Antihistamine drug could be used as a solubilized agent for poorly water-soluble drugs. • In vitro CaCo-2 cell lines showed the low cytotoxicity used by the nanosized mixed micelle. [ABSTRACT FROM AUTHOR]

Abstract Background Natural products can exert promising nutritional and medicinal value, and traditionally used in pursuit of health and well-being. Despite having a potential therapeutic effect, natural compounds tend to show limited biological activity due to their environmental-instability, poor solubility, gastric-degradation, uncontrolled-release, poor bioavailability, and unspecific delivery. Therefore, liposomal delivery of natural compounds has been considered as a potential tool to overcome the limitations associated with delivery in in vivo. Scope and approach Liposomes are attractive and effective nano-carriers for the delivery of natural compounds and pharmaceuticals, which can enhance their bioavailability and therapeutic effect. In this review, we critically discussed the fundamentals and generation-wise chronological liposomal improvements, affecting factors associated with the formation of liposome, and mechanism of cellular internalization. Besides, we discussed the efficiency of liposomal systems for the encapsulation and successful delivery of natural products in treating human diseases and the challenges associated with the liposomal delivery of natural products. Key findings and conclusions Formulation parameters, i.e. phospholipid type, phospholipid-to-cholesterol ratio, and encapsulated compounds could play a significant role in the liposomal preparation. Studies have shown that liposomal delivery of natural products could significantly increase the protective effect of natural product against cancer, hepato-/neuro-toxicity, inflammation, oxidative stress, hyperlipidemia, and microbial disease. Further studies concerning the improved liposomal systems and more in vivo studies could shed a light to evaluate the therapeutic efficacy of natural compounds by understanding the physicochemical stability, target mechanisms, cellular internalization and release kinetics. Highlights • Liposomes are attractive and effective delivery systems for natural compounds. • Different generations of liposomes are addressed. • Factors behind the formation of stabilized liposome. • Cellular internalization of different liposomal systems. • Efficiency of liposomes to improve the biological efficacy of natural products. [ABSTRACT FROM AUTHOR]

Abstract Tyrosol, hydroxytyrosol and oleuropein are among the major phenolic compounds in fruits, leaves and oils from Olea europaea L. These natural antioxidants molecules revealed several beneficial effects on human health, but a low bioavailability and accessibility to targeted site. Liposomes are drug/nutraceutical delivery carriers, used for driving bioactive molecules to desired target tissues, decreasing potential side effects and protecting the encapsulated molecule from enzymatic metabolic processes. In this study, zwitterionic liposomes containing tyrosol, hydroxytyrosol and oleuropein were synthesized and characterized for their size and surface charge. Particular attention was devoted to the determination of encapsulation efficiency (EE%), quantifying the loaded Tyr, HTyr and Ole amount, by using three different techniques: direct UV spectrophotometry, High Performance Liquid Chromatography and Trolox Equivalent Antioxidant Capacity assay. The results revealed higher EE% for oleuropein. Cyto-toxicity and cyto-compatibility of liposomes were also tested on human chondrocyte cells. Graphical abstract Unlabelled Image Highlights • DOPC/DOPE liposomes loaded with antioxidants from Olea europaea L were synthesized. • Plain and loaded liposomes were chemically characterized. • Loaded liposomes encapsulation efficiency percentages were determined. • Plain and loaded liposomes were assayed on human chondrocyte cells. [ABSTRACT FROM AUTHOR]

[Display omitted] • FTIR results demonstrated there was electrostatic interaction between SPI and CSG. • The hyssop-loaded double emulsion was stabilized by SPI alone and combined with CSG. • SPI/CSG-stabilized double emulsion showed higher encapsulation efficiency. • The encapsulated extract was better than the free form in oil oxidation control. The aim of this study was to encapsulate hyssop (Hyssopus officinalis L.) extract obtained through ultrasound-assisted cold plasma pretreatment extraction within a double emulsion stabilized by soy protein isolate alone (SPI) and combined with chia seed gum (CSG) in the external aqueous phase on the stabilization of canola oil. FTIR analysis verified that there were electrostatic interactions between CSG and SPI. The SPI/CSG-stabilized emulsion demonstrated lower viscosity, smaller droplets, higher ζ-potential, and encapsulation efficiency compared to the SPI-stabilized emulsion. Non-Newtonian, pseudoplastic behaviors were shown by emulsions. Also, according to the dynamic rheological parameters (G' and G''), the SPI/CSG-stabilized emulsion had elastic behavior with weak gel properties. The antioxidant activity of the encapsulated extract at 1500 ppm during the storage in canola oil was investigated and compared to unencapsulated extract and TBHQ. The results showed that oil containing encapsulated extract had lower oxidative alterations than the unencapsulated form. [ABSTRACT FROM AUTHOR]

• Ultrasound enhanced hydrogen bond interaction between icaritin and pectin. • NMR data indicated that 7-OH of icaritin was involved in hydrogen bond formation. • Ultrasound-modified IPMs displayed strong anti-proliferation activity. • Ultrasound-modified IPMs displayed decreased particle size. Pectin can improve the bioaccessibility of icaritin as a nanocarrier, and ultrasound can modify the pectin structure. However, the interaction between ultrasound-modified pectin (UMP) and icaritin remains unclearly. In this work, the effects of UMP on the physiochemical properties of icaritin/pectin micelles (IPMs) were investigated. The IPMs prepared with UMP (UMP-IPMs) showed lower encapsulation efficiencies and loading capacities, comparing with native IPMs. UMP-IPMs had smaller particle sizes (325–399 nm) than native IPMs (551 nm). The Mw, viscosity, G' and G" of pectin were determined. NMR spectra indicated that the repeating unit in pectins remained consistently before and after ultrasound treatment, and 7-OH of icaritin was involved in hydrogen bond formation with pectin. The larger chemical shift movement of 6-H and 7-OH for U3-IPMs than P0-IPMs suggested that stronger hydrogen bond interaction between icaritin and pectin. UMP-IPMs exhibited stronger anti-proliferation activities against HepG2 cells than native IPMs. [ABSTRACT FROM AUTHOR]