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A zwitterionic, stimuli-responsive liposomal system was meticulously designed for the precise and controlled delivery of curcumin, leveraging enzyme-specific and hyperthermic stimuli to enhance therapeutic outcomes. This platform is specifically engineered to release curcumin in response to phospholipase A2 , an enzyme that degrades phospholipids, enabling highly targeted and site-specific drug release. Mild hyperthermia (40 °C) further enhances membrane permeability and activates thermosensitive carriers, optimizing drug delivery. Curcumin encapsulation is facilitated through a combination of zwitterionic and electrostatic interactions, significantly improving both loading capacity and encapsulation efficiency. A design of experiments (DoE) approach was employed to systematically optimize lipid-to-cholesterol ratios and formulation conditions. The liposomal system was thoroughly characterized using dynamic light scattering, zeta potential measurements, and transmission electron microscopy, ensuring stability and structural integrity. Notably, this system effectively encapsulates hydrophobic curcumin while maintaining particle size and bioactivity. In vitro studies revealed robust antioxidant and anti-ROS activities, alongside excellent biocompatibility, with no cytotoxicity observed at concentrations up to 2000 μg/mL. Furthermore, the zwitterionic liposomes enhanced M2 macrophage polarization and reduced oxidative stress. This advanced platform offers a promising, biocompatible solution for targeted curcumin delivery.

Objective: The objective of this study was to develop and optimize palbociclib-loaded nanobubbles for targeted breast cancer therapy., Materials and Methods: Biocompatible poly(DL-lactide-co-glycolide) was used to create nanobubbles loaded with palbociclib. The formulation process was meticulously crafted using a three-level Box-Behnken design and a double emulsion solvent evaporation method to precisely tailor the nanobubbles' properties., Results: The Derringer's desirability method optimized variables by transforming responses into a desirability scale, resulting in a global desirability value. Optimal settings, A: 526.97mg, B: 250mg,C: 2.0% w/v, D: 6101rpm, achieved a D value of 0.949. Palbociclib nanobubbles demonstrated a smaller particle size (31.78±2.12) than plain nanobubbles (38.56±3.56). PDI values indicated a uniform size distribution. The zeta potential remained consistent, with values of -31.34±3.36 for plain and -31.56±3.12 for drug-loaded nanobubbles. Encapsulation efficiency was 70.12%, highlighting effective drug encapsulation. Palbociclib release was significantly higher from nanobubbles in pH 7.4, especially with ultrasound, releasing almost 99.34% of the drug. Hemolytic activity assays confirmed safety for injection. Fluorescent intensity analysis revealed a two-fold increase in cellular uptake of palbociclib facilitated by ultrasound. The MTT assay demonstrated enhanced cytotoxicity of palbociclib-loaded nanobubbles, especially with ultrasound, emphasizing their potential for improved therapeutic efficacy. The IC 50 values for palbociclib, without ultrasound, and with ultrasound were 98.3μM, 72.34μM, and 61.34μM, respectively., Conclusion: The significant findings of this study emphasize the potential of palbociclib-loaded nanobubbles as a promising therapeutic system for improved breast cancer treatment., (Copyright © 2024 Académie Nationale de Pharmacie. Published by Elsevier Masson SAS. All rights reserved.)

This study examined the rheological properties, interfacial characteristics, particle size, zeta potential, Turbiscan stability index (TSI), morphology, and encapsulation efficiency of curcumin (Cur) loaded fish gelatin (FG) emulsions modified with γ-polyglutamic acid (γ-PGA). The results showed that adding γ-PGA significantly increased curcumin encapsulation efficiency. At 0.3 mg/mL, FG emulsions had an encapsulation efficiency of 80.14 %, while FG-γ-PGA emulsions reached 90.35 %. The FG-γ-PGA emulsions also showed enhanced stability and resistance to phase separation, remaining stable for seven days, compared to three days for FG emulsions. After 24 h, the TSI of FG emulsions with 0.6 mg/mL Cur was 2.46, significantly higher than the 0.55 TSI for FG-γ-PGA emulsions at the same concentration. FG-γ-PGA emulsions had smaller droplet sizes, and analysis of interfacial characteristics, particle size, and zeta potential indicated better system stability than FG emulsions. These improved properties of FG-γ-PGA emulsions highlight their potential as efficient carriers for curcumin. Overall, the favorable characteristics of FG-γ-PGA emulsions suggest promising applications in the food industry, especially for developing functional foods with extended shelf life and enhanced nutritional benefits., Competing Interests: Declaration of competing interest The authors declare that they have no conflict of interest to this work, and the manuscript is approved by all authors for publication., (Copyright © 2024 Elsevier B.V. All rights reserved.)

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., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

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., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier B.V. All rights reserved.)

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., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

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., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Segale L., Giovannelli L. are co-founders and members of the advisory board of the company APTSol S.r.l., Milanesi A. is member of advisory board of the company APTSol S.r.l. Torre M.L. is co-founder and member of the advisory board of the company Pharmaexceed. The other authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 The Authors. Published by Elsevier B.V. All rights reserved.)

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.

Ultrasmall polymer nanoparticles are rapidly gaining importance as nanocarriers for drugs and contrast agents. Here, a straightforward modular approach to efficiently loaded and stable sub-20-nm polymer particles is developed. In order to obtain ultrasmall polymer nanoparticles, we investigated the influence of one to two charged groups per polymer chain on the size of particles obtained by nanoprecipitation. Negatively charged carboxylate and sulfonate or positively charged trimethylammonium groups were introduced into the polymers poly(d,l-lactide-co-glycolide) (PLGA), polycaprolactone (PCL), and poly(methyl methacrylate) (PMMA). According to dynamic light scattering, atomic force and electron microscopy, the presence of one to two charged groups per polymer chain can strongly reduce the size of polymer nanoparticles made by nanoprecipitation. The particle size can be further decreased to less than 15 nm by decreasing the concentration of polymer in the solvent used for nanoprecipitation. We then show that even very small nanocarriers of 15 nm size preserve the capacity to encapsulate large amounts of ionic dyes with bulky counterions at efficiencies >90%, which generates polymer nanoparticles 10-fold brighter than quantum dots of the same size. Postmodification of their surface with the PEG containing amphiphiles Tween 80 and pluronic F-127 led to particles that were stable under physiological conditions and in the presence of 10% fetal bovine serum. This modular route could become a general method for the preparation of ultrasmall polymer nanoparticles as nanocarriers of contrast agents and drugs.

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

The influence of air inlet temperature at 155, 165 and 175 °C and whey protein isolate (WPI) of 15, 25 and 35% concentration on numerous parameters of ginger oleoresin powder produced by spray drying was examined in this research. Powder recovery increased dramatically from 23.35 to 68.43% and 53.66 to 64.27%, respectively, as WPI concentration increased from 15 to 35% and inlet temperature decreased from 155 to 175 °C. Increases in WPI concentration and inlet temperature enhanced dissolving time from 22.36 to 32.17 s and 19.54 to 24.24 s respectively. Water activity, encapsulation efficiency of ginger oleoresin microcapsules increased from 0.16 to 0.22, 75.28 to 82.43% respectively, while total phenolic content decreased from 27.13 to 19.04 (mg GAE/g) when WPI concentration increased. Lower encapsulation efficiency (78.66%) and higher total phenol content (23.57 mg GAE/g) were reported at higher inlet temperatures (175 °C). The encapsulated oleoresin samples also exhibited smaller-sized particles which were tightly packed at higher inlet temperatures. Micrographs of the powdered sample revealed smooth morphology. [ABSTRACT FROM AUTHOR]

Vitamin E acetate (VEA) is commonly used in manufacturing pharmaceuticals, food additives, and animal feeds. However, VEA possesses disadvantages, including low water solubility, low bioavailability, and susceptibility to degradation and oxidation. This study investigated the use of cocoliposomes for encapsulating VEA (VEACL). The cocoliposomes consisted of coconut phospholipids (CocoPLs) and cholesterol (Chol). Several parameters, such as functional groups, transition temperature, encapsulation efficiency (EE), release profile, particle size, polydispersity index, and zeta potential, were analyzed to evaluate the impact of cholesterol inclusion on the cocoliposome membrane. The results show that the Fourier transform infrared spectra of VEACL do not exhibit any new, distinct peaks that differ from the peaks of its constituent composition. Therefore, it confirmed that no chemical reactions occurred during the manufacturing of VEACL. Cholesterol in the system raises the transition temperature of phospholipids and enhances the stability of VEACL. The EE remains above 80% despite a 20% increase in cholesterol levels. The release rate of VEA from cocoliposomes was slower with VEACL–20%Chol compared to VEACL–0%Chol. The cholesterol level leads to a decrease in particle size and an increase in the negative zeta potential of the cocoliposomes. Data show that cocoliposomes are effective carriers for VEA encapsulation.

Background: Nano-structure Lipid Carriers (NLCs) are small spheres extending in scale from 10 to 1000 nanometres comprised of biocompatible and biodegradable lipids. These spheres can encapsulate both hydrophilic and lipophilic drugs, preserving them from degradation and increasing their distribution to the intended place in the body. Imipramine, a tricyclic antidepressant, has been investigated in hamster model at 5-10 mg/kg for experimental leishmaniasis. The goal of this research is to develop Imipramine in a nano-structured lipid carrier formulation for targeting macrophage cells. Materials and Methods: Imipramine-loaded NLCs were created employing Glyceryl Monostearate (GMS) as the solid lipid constituent alongside oleic acid as the liquid lipid, while tween80 acted as the surfactant. The process of hot homogenization was employed to prepare the NLCs. The formulation was optimized using 2³ factorial designs using design expert software. The optimised formulation was further used for the preparation of mannose functionalized imipramine-loaded NLCs. Results: The IMP-NLC opt and M-NLC show a globule size of 348.5±0.81 nm and 459.4±0.28 nm with encapsulation efficiency of 61.6±0.326% and 64.48±0.408%, respectively. The drug release in vitro demonstrates a dual-phase pattern, featuring an early rapid sudden release followed by a gradual and slower release. The surface morphology, drug release kinetics and stability were also used to characterize the prepared NLCs. Conclusion: This study concludes that nanostructured lipid carriers demonstrate considerable encapsulation efficiency, release and stability for further pre-clinical investigation. [ABSTRACT FROM AUTHOR]

Pickering emulsions are suspensions of droplets of one liquid in another immiscible liquid which are stabilized by solid particles adsorbed at the droplet-liquid interface. The stabilization of emulsion is done by the solid particles that physically prevent droplets from coalescing. It is possible to alter the emulsifying capabilities of starch by expanding its surface area or changing its charge. Pickering emulsions are stabilized by components such as starch, cellulose, or chitosan. Starch based Pickering emulsions are highly biodegradable and have low toxicity. The inclusion of starch assists in the development of more stable and long-lasting emulsions, extending the shelf life of the developed products. Starch stabilized Pickering emulsions can be utilized to encapsulate pharmaceuticals or nutrients for systemic or targeted administration. The potential for controlled release of Pickering emulsions is highlighted in this review when behavior varies in response to environmental factors like temperature, pH, or light. The investigation emphasized Pickering emulsions with biocompatible and biodegradable particles and focused on numerous environmentally friendly and sustainable techniques for making Pickering emulsions, such as using waste or renewable resource-derived particles. The review focuses on the development, characterization, and applications of Pickering emulsions based on biological macromolecules of starch.

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

For improving solubility and bioaccessibility of phytosterols (PS), phytosterol nanoparticles (PNPs) were prepared by emulsification–evaporation combined high-pressure homogenization method. The organic phase was formed with the dissolved PS and soybean lecithin (SL) in anhydrous ethanol, then mixed with soy protein isolate (SPI) solution, and homogenized into nanoparticles, followed by the evaporation of ethanol. The optimum fabrication conditions were determined as PS (1%, w/v): SL of 1:4, SPI content of 0.75% (w/v), and ethanol volume of 16 ml. PNPs were characterized to have average particle size 93.35 nm, polydispersity index (PDI) 0.179, zeta potential −29.3 mV, and encapsulation efficiency (EE) 97.3%. The impact of temperature, pH, and ionic strength on the stability of fabricated PNPs was determined. After 3-h in vitro digestion, the bioaccessibility of PS in nanoparticles reached 70.8%, significantly higher than the 18.2% of raw PS. Upon freeze-drying, the particle size of PNPs increased to 199.1 nm, resulting in a bimodal distribution. The solubility of PS in water could reach up to 2.122 mg/ml, ~155 times higher than that of raw PS. Therefore, this study contributes to the development of functional PS-food ingredients.

The main purpose of this Letter was to develop and optimise recombinant hepatitis B antigen‐loaded chitosan nanoparticles (rHBsAg‐CS NPs) as a new adjuvant for hepatitis B vaccine through designing by response surface methodology (RSM). The NPs were prepared by employing ionic gelation technique. RSM was utilised by selecting the independent variablesincluding the concentration of CS, tripolyphosphate and antigen concentration as well as pH and homogenisation speed to obtain maximum encapsulation efficiency (EE) and loading capacity (LC). EE and LC of the optimised preparation were 93.2 ± 1.1 and 25.6 ± 1.38%, respectively. Optimised NPs showed spherical shape, particle size of 187 ± 14 nm and positive zeta potential (+31.3 ± 1.5 mV). In vitro release profile of optimised formulation revealed an initial burst, followed by a slow sustained antigen release. Cell viability assay indicated that the toxicity of NPs was concentration‐dependent. SDS‐PAGE analysis confirmed the structural stability and integrity of the released antigen. ELISA and Ouchterlony double immunodiffusion tests of released antigen showed that the antigenicity was preserved during the process of NP formation. [ABSTRACT FROM AUTHOR]

The present study aimed to develop a surface‐modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE‐40‐S) to improve the oral bioavailability of poorly water‐soluble Biopharmaceutics Classification System class‐II drug like tamoxifen (TMX). Also aimed to screen the most influential factors affecting the particle size (PS) using Taguchi (L12 (211)) orthogonal array design (TgL12 OA). Then, to optimize the TMX loaded POE‐40‐S (P) surface‐modified NLCs (TMX‐loaded‐PEG‐40‐S coated NLC (PNLCs) or PNLCs) by central composite design (CCD) using a four‐factor, five‐level model. The most influential factors affecting the PS was screened and optimized. The in‐vitro study showed that increased drug‐loading (DL) and encapsulation efficiency (EE), decreased PS and charge, sustained drug release for the prolonged period of the time with good stability and suppressed protein adsorption. The Ex‐vivo study showed that decreased mucous binding with five‐fold enhanced permeability of PNLC formulation after surface modification with POE‐40‐S. The in‐vitro cytotoxicity study showed that the blank carrier is biocompatible and cytotoxicity of the formulation was dependent on the concentration of the drug. Finally, it can be concluded that the surface‐modified PNLCs formulation was an effective, biocompatible, stable formulation in the enhancement of dissolution rate, solubility, stability with reduced mucus adhesion and increased permeability thereby which indicates its enhanced oral bioavailability. [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]

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In this study, the authors developed pectin‐stabilised selenium nanoparticles (pectin‐SeNPs) for curcumin (Cur) encapsulation and evaluated their physicochemical properties and biological activities. Results showed that pectin‐SeNPs and Cur‐loaded pectin‐SeNPs (pectin‐SeNPs@Cur) exhibited monodisperse and homogeneous spherical structures in aqueous solutions with mean particle sizes of ∼61 and ∼119 nm, respectively. Cur was successfully encapsulated into pectin‐SeNPs through hydrogen bonding interactions with an encapsulation efficiency of ∼60.6%, a loading content of ∼7.4%, and a pH‐dependent and controlled drug release in vitro. After encapsulation was completed, pectin‐SeNPs@Cur showed enhanced water solubility (∼500‐fold), dispersibility, and storage stability compared with those of free Cur. Moreover, pectin‐SeNPs@Cur possessed significant free radical scavenging ability and antioxidant capacity in vitro, which were stronger than those of pectin‐SeNPs. Antitumour activity assay in vitro demonstrated that pectin‐SeNPs@Cur could inhibit the growth of HepG2 cells in a concentration‐dependent manner, and the nanocarrier pectin‐SeNPs exhibited a low cytotoxic activity against HepG2 cells. Therefore, the results suggested that pectin‐SeNPs could function as effective nanovectors for the enhancement of the water solubility, stability, and in vitro bioactivities of hydrophobic Cur. [ABSTRACT FROM AUTHOR]

Present investigation aimed to prepare, optimise, and characterise lipid nanocapsules (LNCs) for improving the solubility and bioavailability of efavirenz (EFV). EFV‐loaded LNCs were prepared by the phase‐inversion temperature method and the influence of various formulation variables was assessed using Box–Behnken design. The prepared formulations were characterised for particle size, polydispersity index (PdI), zeta potential, encapsulation efficiency (EE), and release efficiency (RE). The biocompatibility of optimised formulation on Caco‐2 cells was determined using 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyltetrazolium bromide assay. Then, it was subjected to ex‐vivo permeation using rat intestine. EFV‐loaded LNCs were found to be spherical shape in the range of 20–100 nm with EE of 82–97%. The best results obtained from LNCs prepared by 17.5% labrafac and 10% solutol HS15 when the volume ratio of the diluting aqueous phase to the initial emulsion was 3.5. The mean particle size, zeta potential, PdI, EE, drug loading%, and RE during 144 h of optimised formulation were confirmed to 60.71 nm, −35.93 mV, 0.09, 92.60, 7.39 and 55.96%, respectively. Optimised LNCs increased the ex vivo intestinal permeation of EFV when compared with drug suspension. Thus, LNCs could be promising for improved oral delivery of EFV. [ABSTRACT FROM AUTHOR]

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.

Virgin coconut oil (VCO) has been shown to have health-promoting effects due to its high medium-chain fatty acid (MCFA) content and antioxidant properties, however, its taste and feeling of greasiness are not acceptable to many consumers. In this study, VCO was microencapsulated to develop a new and healthy consumable food product. Spray drying VCO with supercritical carbon dioxide (SC-CO 2 ) at pressures from 12 to 16 MPa, temperatures from 40 to 60 °C was studied for an emulsion feed flow rate that was varied from 3 to 5 mL/min. The encapsulation efficiencies ranged from 73% to 80%, the microcapsules were spherical with diameters that ranged from 27 to 72 μm and the antioxidant activities of the retained microencapsulated oil ranged from 0.6 to 1.0 mmol butylated hydroxytoluene (BHT) equivalent/ml oil and 0.8–1.3 mmol trolox equivalent/ml oil for 2,2-diphenyl-1-picrylhydrazyl (DPPH) tests and 2,2′-azino-bis (ABTS) tests, respectively. SC-CO 2 spray drying is an effective method to encapsulate VCO and other food oils. [ABSTRACT FROM AUTHOR]

The aim of this research was to develop novel W1/O/W2 nanoemulsions for encapsulating Hohenbuehelia serotina polysaccharides to resolve the low soluble and unstable problems. The prepared parameters (PVA content, polysaccharides concentration, stirring speed and stirring time) of H. serotina polysaccharides nanoemulsions were optimized based on the response surface methodology. Through systematic analysis of the model, the optimal conditions were chosen as PVA content of 0.60%, polysaccharides concentration of 9.7 μg/mL, stirring speed of 11,000 rpm, and stirring time of 2.4 min. Under the optimal prepared conditions, the encapsulation efficiency and particle size were respectively 75.42 ± 0.69% and 410.1 ± 2.3 nm, which were well consistent with the predicted values. The optimized nanoemulsions possessed the spherical multilayer structure with the zeta potential value of −52.34 ± 5.62 mV, and they could be stably stored at 25 °C for 6 days. Moreover, the nanoemulsions had the excellent sustained-release characteristics in the simulated gastric fluid. This study may provide a valuable contribution for the application of nanoemulsions in the functional food field. [ABSTRACT FROM AUTHOR]

The authors prepared surface modified (with polyelectrolyte layers), tea polyphenols (TPP) encapsulated, gelatin nanoparticles (TPP‐GNP) and characterised them. The size of the spherical nanoparticles was ∼50 nm. Number of polyelectrolyte layers and incubation time influenced the encapsulation efficiency (EE); highest EE was noted in nanoparticles with six polyelectrolyte layers (TPP‐GNP‐6L) incubated for 4 h. TPP released from TPP‐GNP‐6L in simulated biological fluids indicated protection and controlled release of TPP due to encapsulation. Mathematical modelling indicated anomalous type as a predominant mode of TPP release. TPP‐GNP‐6L exhibited enhanced pharmacokinetics in rabbit model compared with free TPP. The area under the concentration‐time curve and mean residence time were significantly higher in TPP‐GNP‐6L compared with free TPP which provide an evidence of higher bioavailability of TPP due to encapsulation. The authors demonstrated that encapsulation of TPP into GNPs favoured slow and sustained release of TPP with improved pharmacokinetics and bioavailability thereby can prolong the action of TPP. [ABSTRACT FROM AUTHOR]

The double emulsion technology has a potential effect on the development of diversity and quality of functional foods by means of decreasing oil or salt concentration, encapsulating and controlling release of valuable components. In this study, it was aimed to formulate stable double emulsions to be used in food systems. W1/O ratios of primary emulsions, stabilized by polyglycerol polyricinoleate (PGPR), were designed as 2:8 and 4:6, and (W1/O)/W2 ratios of the double emulsions were used as 2:8 and 4:6. W/O/W phase ratios, homogenization methods applied to primary emulsion (high-speed homogenization, ultrasonic homogenization), and emulsifier types used in W2 phase [sodium caseinate (SC), xanthan gum, lecithin-whey protein concentrate] were used as independent variables. Particle size and distributions, stability, encapsulation efficiency (EE), rheological properties, long-term stability, and morphological properties of the double emulsions were investigated. The double emulsions prepared with SC and (W1/O)/W2 ratio of 4:6, were found to have the higher stability values, higher apparent viscosity, and lower particle size. High-speed homogenization applied to primary emulsion reduced particle size of the double emulsion and increased apparent viscosity, but did not affect stability and EE of the double emulsions, significantly. [ABSTRACT FROM PUBLISHER]

Atorvastatin known to be a potential inhibitor of HMG‐CoA reductase involved in the synthesis of cholesterol. It is touted as miracle drug due to its profound effect in decreasing the low‐density lipoproteins in blood. Unfortunately, the high dosage used poses side‐effects relatively in comparison to other statins. On the other hand, curcumin has a diverse therapeutic potential in health and disease. However, the poor aqueous solubility and low bioavailability hinders the therapeutic potential of it when administrated orally. Therefore, it was thought to minimise the frequency of atorvastatin doses to avoid the possibility of drug resistance and also to overcome the limitations of curcumin for desirable therapeutic effects by using nanocarriers in drug delivery. In this investigation, synergistic effect of atorvastatin and curcumin nanocarriers was encapsulated by chitosan polymer. The chitosan nanocarriers prepared by ionic gelation method were characterised for their particle size, zeta potential, and other parameters. The drug‐loaded nanocarriers exhibited good encapsulation efficiency (74.25%) and showed a slow and sustained release of atorvastatin and curcumin 60.36 and 61.44%, respectively, in a span of 48 h. The drug‐loaded nanocarriers found to be haemocompatible and qualified for drug delivery in atherosclerosis. [ABSTRACT FROM AUTHOR]

In this study, PLGA or PLGA-PEG blend nanoparticles were developed loading amphotericin B (AmB), an antifungal agent broadly used in therapy. A 22 × 31factorial experimental design was conducted to indicate an optimal formulation of nanoparticles containing AmB and demonstrate the influence of the interactions of components on the mean particle size and drug encapsulation efficiency. The independent variables analyzed were polymer amount (two levels) and organic phase (three factors in one level). The parameters methanol as cosolvent and higher polymer amount originated from the higher AmB encapsulation, but with the larger particle size. The selected optimized parameters were set as the lower polymer amount and ethyl acetate as cosolvent in organic phase, for both PLGA and PLGA-PEG nanoparticles. These parameters originated from nanoparticles with the size of 189.5 ± 90 nm and 169 ± 6.9 nm and AmB encapsulation efficiency of 94.0 ± 1.3% and 92.8 ± 2.9% for PLGA and PLGA-PEG nanoparticles, respectively. Additionally, these formulations showed a narrow size distribution indicating homogeneity in the particle size. PLGA and PLGA-PEG nanoparticles are potential carrier for AmB delivery and the factorial design presented an important tool in optimizing nanoparticles formulations. [ABSTRACT FROM AUTHOR]

Background: PLA-PEG-PLA triblock polymer nanoparticles are promising tools for targeted dug delivery. The main aim in designing polymeric nanoparticles for drug delivery is achieving a controlled and targeted release of a specific drug at the therapeutically optimal rate and choosing a suitable preparation method to encapsulate the drug efficiently, which depends mainly on the nature of the drug (hydrophilic or hydrophobic). In this study, methotrexate (MTX)-loaded nanoparticles were prepared by the double emulsion method. Method: Biodegradable polymer polyethylene glycolpolylactide acid tri-block was used with poly(vinyl alcohol) as emulsifier. The resulting methotrexate polymer nanoparticles were coated with bovine serum albumin in order to improve their biocompatibility. This study focused on particle size distribution, zeta potential, encapsulation efficiency, loading capacity, and in vitro drug release at various concentrations of PVA (0.5%, 1%, 2%, and 3%). Results: Reduced particle size of methotrexate-loaded nanoparticles was obtained using lower PVA concentrations. Enhanced encapsulation efficiency and loading capacity was obtained using 1% PVA. FT-IR characterization was conducted for the void polymer nanoparticles and for drug-loaded nanoparticles with methotrexate, and the proteincoated nanoparticles in solid state showed the structure of the plain PEG-PLA and the drug-loaded nanoparticles with methotrexate. The methotrexate-loaded PLA-PEG-PLA nanoparticles have been studied in vitro; the drug release, drug loading, and yield are reported. Conclusion: The drug release profilewasmonitored over a period of 168 hours, and was free of burst effect before the protein coating. The results obtained from this work are promising; this work can be taken further to develop MTX based therapies. [ABSTRACT FROM AUTHOR]

Poly lactic-co-glycolic acid (PLGA) is a biodegradable polymer with good biocompatibility. Because the products of its hydrolysis process are Lactic acid (LA) and Glycolic acid (GA), the middle products of normal metabolism, which are finally catabolized into carbon dioxide and water that are respectively eliminated via lungs and kidneys and make no bad effects on human bodies, it is often as the preferred carrier to be used to prepare microspheres.In recent years, microsphere has developed rapidly in pharmaceutical field and it has turned out to be a potential formulation with great advantages inanticancer, vaccine, protein administration and gene therapy, diagnostic reagents and cytoskeleton. At present, some PLGA microspheres have been approved by the FDA in US and have acquired satisfactory results in clinical application without serious side effects being reported. However the quality of domestic PLGA microspheres still exists many problems such as the bigger particle size, the lower encapsulation efficiency and drug loading and the larger burst rate which have great scope to improve. This article will review the influence factors such as the physicochemical properties of the drug itself, the preparation method, structure features of PLGA and organic solvents on particle size, encapsulation efficiency during the procedure of PLGA microspheres encapsuled with hydrophilic drugs in order to make a good theory basis of improving pesticide effects of medicine loaded by PLGA. [ABSTRACT FROM AUTHOR]

In the field of keratoconus treatment, a lipid-based liquid crystal nanoparticles system has been developed to improve the preocular retention and ocular bioavailability of riboflavin, a water-soluble drug. The formulation of this ophthalmic drug delivery system was optimized by a simplex lattice experimental design. The delivery system is composed of three main components that are mono acyl glycerol (monoolein), poloxamer 407 and water and two secondary components that are riboflavin and glycerol (added to adjust the osmotic pressure). The amounts of these three main components were selected as the factors to systematically optimize the dependent variables that are the encapsulation efficiency and the particle size. In this way, 12 formulas describing experimental domain of interest were prepared. Results obtained using small angle X-rays scattering (SAXS) and cryo-transmission electron microscopy (cryo-TEM) evidenced the presence of nano-objects with either sponge or hexagonal inverted structure. In the zone of interest, the percentage of each component was determined to obtain both high encapsulation efficiency and small size of particles. Two optimized formulations were found: F7 and F1. They are very close in the ternary phase diagram as they contain 6.83% of poloxamer 407; 44.18% and 42.03% of monoolein; 46.29% and 48.44% of water for F7 and F11, respectively. These formulations displayed a good compromise between inputs and outputs investigated. [ABSTRACT FROM AUTHOR]

To develop self-assembled liquid crystalline nanoparticles as a drug delivery system for keratoconus treatment, a formulation containing riboflavin a water-soluble drug, two surfactants (poloxamer 407 and mono acyl glycerol - monoolein-) and water was optimized and prepared by emulsification and a homogenization process. A fractional factorial design was applied to estimate the main effects and interaction effects of five parameters on two responses, namely particle size and encapsulation efficiency. The five parameters are the temperature of the two phases, the duration of emulsification, the presence of heating during homogenization, the number of passes and pressure. The most influent parameters are the presence of heating during the homogenization and the pressure that led to the production of nanoparticles with an average size of 145 nm and an average encapsulation efficiency of 46%. [ABSTRACT FROM AUTHOR]

The aim of this study was to produce cinnarizine loaded Eudragit® L100-55 microparticles by coacervation technique in order to achieve pH responsive drug release using hydroxypropyl methycellulose (HPMC) as stabilizer. The effect of enteric polymer: HPMC ratio on properties of microparticles was investigated with regard to particle size distribution, morphology, yield, encapsulation efficiency, in vitro drug release profiles and interaction between cinnarizine and Eudragit® L100-55. High drug encapsulation efficiency was seen in all microparticles. Particle diameter increased when the enteric polymer content was higher relative to HPMC. In vitro dissolution studies demonstrated that the drug release from the microparticles was dependent upon enteric polymer: HPMC ratio and particle size distribution. At the ratio of at least 3.75:1 of enteric polymer: HPMC, drug release was suppressed most significantly in low pH (hydrochloric acid as medium) while rapid drug release was observed in pH 7.4. [ABSTRACT FROM AUTHOR]

A robust experimental design method was developed using a response surface methodology and models to facilitate the development process of retinol solid lipid nanoparticles (SLNs). The SLNs were evaluated to determine how different parameters including lipid and surfactant affect size and encapsulation efficiency. This was conducted using factorial analysis and a robust design (RD) method was used to achieve optimal formulations. Two models were developed based on the RD principle and both mean and variance of the response characteristics were estimated functionally using the least squares method. They proved useful in formulation studies aiming to develop optimum by allowing a systematic and reliable design method. A model for maximizing the overall desirability represented by the geometric mean of all objectives was found to provide a better solution. The newly designed method provides useful information to characterize significant factors and obtain optimum formulations, thereby allowing a systematic and reliable design method. [ABSTRACT FROM AUTHOR]

Abstract: The purpose of this study was to extend QbD principles to liposomal drug products containing a hydrophilic active pharmaceutical ingredient (API) to demonstrate both the feasibility and the advantages of applying QbD concepts to liposome based complex parenteral controlled release systems. The anti-viral drug Tenofovir was selected as a model compound. Desired properties for two of the key liposome drug product qualities, namely the particle size and drug encapsulation efficiency, were defined and evaluated. It was observed that the liposome preparation process significantly affects liposome particle size, and this resulted in considerable variation in the drug encapsulation efficiency. Lipid chain length did not have a significant effect on drug encapsulation efficiency. However, lipid concentration did affect the drug encapsulation efficiency with higher lipid concentrations resulting in higher drug encapsulation. The use of risk assessment in this study assisted the identification of eight high risk factors that may impact liposome drug encapsulation efficiency and particle size. [Copyright &y& Elsevier]

Nonionic surfactant based vesicles (niosomes) are novel drug delivery systems formed from the self-assembly of nonionic amphiphiles in aqueous media. In the present study niosomal formulations of Paclitaxel (PCT), an antineoplastic agent, were prepared using different surfactants (Tween 20, 60, Span 20, 40, 60, Brij 76, 78, 72) by film hydration method. PCT was successfully entrapped in all of the formulations with encapsulation efficiencies ranging between 12.1 ± 1.36% and 96.6 ± 0.482%. Z-average sizes of the niosomes were between 229.3 and 588.2 nm. Depending on the addition of the negatively charged dicetyl phosphate to the formulations negative zeta potential values were obtained. High surface charges showed that niosomes can be suspended in water well and this is beneficial for their storage and administration. PCT released from niosomes by a diffusion controlled mechanism. The slow release observed from these formulations might be beneficial for reducing the toxic side effects of PCT. The niosome preparation method was found to be repeatable in terms of size distribution, zeta potential and % drug loading values. The efficiency of niosomes to protect PCT against gastrointestinal enzymes (trypsin, chymotrypsin, and pepsin) was also evaluated for PCT oral delivery. Among all formulations, gastrointestinal stability of PCT was well preserved with Span 40 niosomes. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2049–2060, 2010 [ABSTRACT FROM AUTHOR]

For thermal adaptable fabrics, the polyurethane-urea microcapsules containing phase-change materials (PCMs: hexadecane, octadecane and eicosane) were successfully synthesized by interfacial polycondensation using 2,4-toluene diisocyanate (TDI)/poly(ethylene glycol) (PEG400)/ethylene diamine (EDA) as shell monomers and nonionic surfactant NP-12 in an emulsion system under stirring rates of 3,000∼13,000 rpm. The mean particle size of microcapsule decreased significantly with increasing the stirring rate up to 11,000 rpm, and then leveled off. The mean particle size increased with increasing the content and molecular weight (eicosane > octadecane > hexadecane) of PCMs at the same stirring rate. The mean particle sizes of microcapsules were found to decrease with increasing the NP-12 content up to 1.5 wt%, and thereafter increased a little. It was found that the melting temperature (Tm) and crystallization temperature (Tc) of three kinds of encapsulated PCMs and their enthalpy changes (ΔHm, ΔHc) increased with increasing PCM contents. The encapsulation efficiencies (Ee) of hexadecane microcapsule linearly increased with increasing the content of hexadecane. It was found that the stable microcapsule containing 50 wt% of hexadecane could be obtained in this study. However, Ee of octadecane and eicosane microcapsules increased with increasing PCM’s contents up to 40 wt%, and then decreased a little. By considering the encapsulation efficiency, it was found that the maximum/optimum contents of octadecane and eicosane microcapsules were about 40 wt%. By the dynamic thermal performance test, it was found that the maximum buffering levels of Nylon fabrics coated with hexadecane, octadecane, and eicosane microcapsules were about −2.4/+2.9°C, −3.6/+3.6°C and −4.0/+4.7°C, respectively. [ABSTRACT FROM AUTHOR]

Abstract: A novel method is described for the preparation of sterile submicron unilamellar liposomes. The method is based on the lyophilization of double emulsions containing disaccharides as lyoprotectants in both the inner and outer aqueous phase. Using various phospholipids or mixtures of lipids as emulsifiers, the double emulsions can be prepared by a two-step emulsification, including hydrophilic agents in the inner aqueous phase or lipophilic agents in the oil phase. Then, the double emulsions are lyophilized after sterilization by passing them through a 0.22-μm pore filter. Rehydration of the lyophilized products results in liposomes with a relatively high encapsulation efficiency (for calcein, 87%; 5-fluorouracil, 19%; flurbiprofen, 93%) and a size below 200 nm measured by the dynamic light scattering technique (DLS) and the atomic force microscopy (AFM). The liposomes were found to be unilamellar from freeze-fracture electron micrographs and X-ray diffraction patterns. In addition, the liposomes can be reconstituted just before use by rehydration of the lyophilized products which are relatively stable. Thus, this reproducible and simple technique can be used to prepare sterilized, submicron unilamellar liposomes with a relatively high encapsulation efficiency, and excellent stability during long-term storage. [Copyright &y& Elsevier]