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© 2023 International Union of Biochemistry and Molecular Biology, Inc.Antiproliferative activity of Achillea vermicularis extracts was calculated on glial (C6) and keratinocyte (HaCaT) cell lines using XTT assay. It was observed that all extracts of A. vermicularis at the determined concentration were not cytotoxic in HaCaT cell lines. The nanoparticles (NPs) of the extract with the best cytotoxic activity was prepared, and necessary characterization studies were performed. Results showed that NP containing the extract has a lower IC50 value and more cytotoxic activity in C6 cells compared to the only extract. Furthermore, the antiepileptic potentials of these substances were explored in this study. The effect of A. vermicularis extracts on the enzyme activities of carbonic anhydrase I and II isoenzymes (hCA I and hCA II) was measured using spectrophotometry to achieve this goal. A. vermicularis extracts demonstrated high inhibitory activities compared to standard inhibitor (acetazolamide, AAZ), with IC50 values in the range of 5.04–10.8 μg/ml for hCA I, and 5.40–9.22 μg/ml for hCA II. High-performance liquid chromatography diode array detector (HPLC-DAD) was used in this investigation to assess the main chemicals found in the extract and NPs. The results showed that the ethanol extract (157.636 μg/mg extract) and NPs (4.631 μg/mg extract) had a significant amount of the 8-hydroxy salvigenin component.

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

Proteins are bioactive compounds with high potential to be applied in the biopharmaceutical industry, food science and as biocatalysts. However, protein stability is very difficult to maintain outside of the native environment, which hinders their applications. Fluorinated ionic liquids (FILs) are a promising family of surface-active ionic liquids (SAILs) that have an amphiphilic behavior and the ability to self-aggregate in aqueous solutions by the formation of colloidal systems. In this work, the protein lysozyme was selected to infer on the influence of FILs in its stability and activity. Then, the cytotoxicity of FILs was determined to evaluate their biocompatibility, concluding that the selected compounds have neglected cytotoxicity. Therefore, UV–visible spectroscopy was used to infer the FIL-lysozyme interactions, concluding that the predominant interaction is the encapsulation of the lysozyme by FILs. The encapsulation efficiency was also tested, which highly depends on the concentration and anion of FIL. Finally, the bioactivity and thermal stability of lysozyme were evaluated, and the encapsulated lysozyme keeps its activity and thermal stability, concluding that FILs can be a potential stabilizer to be used in protein-based delivery systems. publishersversion published

Lupeol liposomes, modified with Gal-PEG-DSPE, were developed following a thin-film dispersion method. Then, the morphology, physicochemical properties, and in vitro release properties of those liposomes were investigated. The scanning electron microscopic images showed that most of the liposomes were spherical particles; they were similar in size and uniformly dispersed. Both lupeol liposomes and Gal-lupeol liposomes exhibited an average particle size of about 100 nm. The encapsulation efficiency was greater than 85%. The encapsulation efficiency of lupeol liposome and Gal-lupeol liposome, stored with 15% sucrose as glycoprotein for 6 months, was higher than 80%; although the particle size increased, they remained within 200 nm. The cell-uptake study demonstrated that the Gal-lupeol-liposome uptake efficiency was the highest in HepG2 cells. The HepG2 cells treated with the Gal-lupeol liposomes had higher apoptotic efficiency than the lupeol liposome and free lupeol. After HepG2 cells were treated with Gal-lupeol liposome, the expressions of AKT/mTOR-related proteins (p-AKT308 and p-AKT473) were also significantly reduced than the lupeol-liposome and free lupeol group. The in vivo targeting studies showed that Gal-NR-L exhibited liver-targeting effects on FVB mice. The pharmacodynamic study was performed by transfecting AKT and c-MET via the high-pressure tail vein of FVB mice. After Gal-lupeol-L administration, the liver index and liver weight of mice were less than those non-targeted group. The histopathological study showed that the lobular structure in the mice liver was clearer, the vacuoles were more obvious, and the cytoplasm was more abundant after Gal-lupeol-L administration. Also, the qRT-PCR study showed that AFP, GPC3, and EpCAM mRNA expression levels were significantly lower than those non-targeted lupeol-liposomes.

Eugenol antioxidant and antibacterial properties have suggested its use as a natural preservative for food matrices. Eugenol application is compromised due to its high volatility and sensibility to external agents, such as light, heat, oxygen, and moisture. Thus, microencapsulation is viable to increase the eugenol stability. Results have showed that carrageenan combined with rice protein and bovine albumin allow high-quality eugenol microcapsules. These materials show excellent properties, favoring the microcapsules use in food matrices. This study aimed to optimize microcapsules formulation by spray drying, using a simplex-centroid mixture design. Blends of low-lactose whey protein (WP) and/or rice bran protein (RBP) and/or bovine serum albumin (BSA) with carrageenan were used as wall materials. Blends influenced the eugenol retention, microencapsulation efficiency, and size. Pure WP was not efficient for eugenol encapsulation. The highest eugenol retention values, 89.7% and 86.5% were obtained by combining carrageenan with RBP or BSA. RBP and BSA binary interaction with carrageenan showed the highest encapsulation value (80.5%). Scanning electron microscopy, infrared spectroscopy, and thermogravimetry confirmed eugenol inside the microcapsules.

Maltodextrin, modified starch, inulin, alginate, gum arabic, and combinations thereof were used as carrier agents for spray drying of carotenoid-rich goldenberry (Physalis peruviana L.) juice and compared to cellobiose as an alternative carrier. Powders were analyzed with respect to particle size and morphology, yield, moisture content, cold water solubility, suspension stability, hygroscopicity, carotenoid encapsulation efficiency, and carotenoid retention during storage. A high initial carotenoid concentration after spray drying, a high encapsulation efficiency of 77.2%, and a slow carotenoid degradation kinetics favored the high carotenoid content of the cellobiose powder at the end of the storage. Cellobiose might protect the carotenoids from degradation processes by light exposure, high temperature, and oxygen due to a tighter particle crust and larger particle sizes. Therefore, cellobiose may be considered a potential carrier agent for the encapsulation of carotenoid-rich fruit juices., Graphical abstract Image 1, Highlights • Goldenberry juice was spray dried with different carrier agents. • Cellobiose was used as carrier agent in the present study for the first time. • The cellobiose powder provided the best retention of carotenoids. • Spray drying promoted isomerization reactions of all-trans-β-carotene. • Cellobiose proved to be effective for spray drying of carotenoid-rich juices.

Introduction . Drug encapsulation efficiency (EE) is the important parameter of the nanoparticle-based drug formulations. Generally, the methods for evaluation of the EE are based on separation of the free and NP-bound fractions of the drug; however, applicability of these methods for a particulate formulation needs careful consideration. Aim. The purpose of the study was to optimize the procedure for evaluation of the EE for a nanoparticle-based drug formulation taking doxorubicin loaded in the PLGA nanoparticles (PLGA-Dox NP) as a model formulation. Materials and methods. The PLGA-Dox NP were prepared by a “double emulsion” method at pH of the external aqueous phase of 7.4 or 6.4. The NP size and size distribution (PDI) were determined by photon correlation spectroscopy (PCS) and transmission electron microscopy (TEM). For the EE evaluation of doxorubicin, the NP were separated by centrifugation (CF), ultrafiltration (UF), or gel filtration. The efficiency of NP separation by the CF method was evaluated by the PLGA content in the supernatant by capillary electrophoresis (CZE). Results and discussion. The average hydrodynamic diameter of the PLGA-Dox/7.4 and PLGA-Dox/6.4 NP (FCS) was 103 ± 10 nm and 141 ± 8 nm, respectively. According to the TEM data, the main fraction of the NP averaged 50 ± 16 nm. The EE of doxorubicin, determined after the NP separation by centrifugation at 48254.g, was 78.9 ± 1.8 % for the PLGA-Dox/6.4 and 91.5 ± 0.9 % for the PLGA-Dox/7.4 NP with the residual PLGA content in the supernatant of ~5 %. At lower acceleration the NP separation was incomplete leading to underestimation of the EE. Also, the ultrafiltration method using the filters with the NMWL of 50 and 100 kDa enabled the reliable NP separation with the minimal doxorubicin adsorption on the filter (

Methotrexate (MTX) anticancer drug was successfully loaded and released in a controlled manner from polymer micelles made of a diblock copolymer of poly(monomethoxy ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL). The empty and MTX-loaded micelles (MTX/mPEG-PCL) were characterized by electron microscopy. The drug release dependence upon pH 5.4, 6.5, and 7.4 for 30 days was proven and characterized by UV-Vis spectroscopy. The cytotoxic effect of MTX/mPEG-PCL micelles on MCF-7 breast cancer cells was evaluated through an MTT assay. The morphological analysis indicated the successful formation of micelles of 76 and 131 nm for empty and MTX-loaded micelles, respectively. An encapsulation efficiency of 70.2% and a loading capacity of 8.8% were obtained. The in vitro release of MTX showed a gradual and sustained profile over 22 days, with a clear trend to much higher release at acidic pH (80 and 90% for pH 6.7 and 5.5, respectively). The MTX/mPEG-PCL micelles showed an IC50 of MCF-7 cells at 30 µg mL−1. The results suggested that MTX/mPEG-PCL could be a promising drug delivery system for cancer treatment.

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

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

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

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

This study investigated the oxidative stability and physical properties of low-fat mayonnaise fortified with electrosprayed zein capsules loaded with fish oil. A high encapsulation efficiency (EE) (83 ± 1%) was achieved in the encapsulates and semi-spherical capsules with rough surface and mean diameter of 2.4 ± 0.7 μm were obtained. The amount of primary oxidation products of the zein capsules did not increase over the storage, even though the initial content was higher compared to neat fish oil. Cryo-SEM images revealed that the capsules remained intact when they were incorporated into a water-based food matrix like mayonnaise. This explained the lower content of hydroperoxides at the end of the storage for the capsule-enriched mayonnaise (Mayo-C) when compared to mayonnaise enriched with neat fish oil (Mayo-F) (2 meq/kg oil vs. 6 meq/kg oil, respectively). Even though, volatile compounds from the secondary oxidation of omega-3, such as 2-ethylfuran and 1-penten-3-one were found in higher amounts in Mayo-F, a higher overall increase in all other secondary oxidation products was observed in Mayo-C. This increase was attributed to the formation of oxidation volatile compounds from the zein material, together with the oxidation of un-encapsulated fish oil droplets. Moreover, Mayo-C presented higher viscosity and droplet size than Mayo-F, which also increased during storage, although no further alterations of the emulsion like creaming were observed. Overall, these findings indicate the benefits of using zein as hydrophobic shell material for the development of omega-3 loaded-electrosprayed capsules intended to the enrichment of water-based food matrices when compared to the use of hydrophilic wall materials.

In this study, it was aimed to prepare and characterize double (W1/O/W2) emulsions for encapsulation of ferric chloride within the internal aqueous phase (W1). The primary (W1/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 (W1/O:W2) 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 W2 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. © 2019 Elsevier Ltd, 114O209, The authors gratefully acknowledge the financial support provided by TUBITAK (Project no: 114O209 ).

Purpose Opioids have been the main factor for drug overdose deaths in the United States. Current naloxone delivery systems are effective in mitigating the opioid effects only for hours. Naloxone-loaded poly(lactide-co-glycolide) (PLGA) microparticles were prepared as quick- and long-acting naloxone delivery systems to extend the naloxone effect as an opioid antidote. Methods The naloxone-PLGA microparticles were made using an emulsification solvent extraction approach with different formulation and processing parameters. Two PLGA polymers with the lactide:glycolide (L:G) ratios of 50:50 and 75:25 were used, and the drug loading was varied from 21% to 51%. Two different microparticles of different sizes with the average diameters of 23 μm and 50 μm were produced using two homogenization-sieving conditions. All the microparticles were critically characterized, and three of them were evaluated with β-arrestin recruitment assays. Results The naloxone encapsulation efficiency (EE) was in the range of 70–85%. The EE was enhanced when the theoretical naloxone loading was increased from 30% to 60%, the L:G ratio was changed from 50:50 to 75:25, and the average size of the particles was reduced from 50 μm to 23 μm. The in vitro naloxone release duration ranged from 4 to 35 days. Reducing the average size of the microparticles from 50 μm to 23 μm helped eliminate the lag phase and obtain the steady-state drug release profile. The cellular pharmacodynamics of three selected formulations were evaluated by applying DAMGO, a synthetic opioid peptide agonist to a μ-opioid receptor, to recruit β-arrestin 2. Conclusions Naloxone released from the three selected formulations could inhibit DAMGO-induced β-arrestin 2 recruitment. This indicates that the proposed naloxone delivery system is adequate for opioid reversal during the naloxone release duration.

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

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

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

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

Liposomes continue to attract great interest due to their increased bioavailability in the body and because the substances encapsulated are protected while maintaining their effectiveness. The aim of this study is to obtain “giant” liposomes by lipid film hydration using a preparation formula with two different phospholipids, phosphatidylcholine (PC) and phosphatidylserine (PS). Firstly, the macro- and microscopic characterization, total phenols content and antioxidant capacity of the plant Stellaria media (L.) Vill. were assessed. Then, Stellaria media (L.) Vill. extract was encapsulated in both formulations (PCE and PSE) and the liposomes were characterized according to their morphology, size distribution and Zeta potential using optical microscopy and dynamic light scattering. The encapsulation efficiency (EE%) was determined using the Folin–Ciocalteu method and the values of both formulations were compared. PC and PCE liposomes with a diameter between 712 and 1000 nm and PS and PSE liposomes with a diameter between 58 and 1000 nm were obtained. The values EE% of Stellaria media (L.) Vill. extract for PCE and PSE were 92.09% and 84.25%, respectively.

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

This review aims to provide an overview of polymers comprising cholesterol moiety/ies designed to be used in drug delivery. Over the last two decades, there have been many papers published in this field, which are summarized in this review. The primary focus of this article is on the methods of synthesis of polymers bearing cholesterol in the main chain or as side chains. The data related to the composition, molecular weight, and molecular weight distribution of polymers are presented. Moreover, other aspects, such as forms of carriers, types of encapsulated drugs, encapsulation efficiency and capacity, are also included.

In this study, sunflower oil containing α-tocopherol (model for oxidizable lipophilic compounds) was encapsulated using a wall material made of maltodextrin and two different extracts rich in β-glucans and proteins, obtained from the basidiomycete Pleurotus ostreatus. A mixture of maltodextrin and acacia gum was used as control wall material. The aim was to assess P. ostreatus extracts as a sustainable and healthy alternative to common emulsifiers. After the evaluation of the emulsion stability, four powders were produced by spray drying and then analysed for the particle morphology and oil droplets distribution within the solid matrix (by scanning electron microscopy), the emulsion microstructure after their dissolution in water (by laser light diffraction) and the encapsulation efficiency (by solvent extraction of surface oil). In addition, powders were analysed in terms of oil protection against oxidation by spectroscopic determination of conjugated dienes and HPLC evaluation of vitamin E. Results showed that P. ostreatus extracts provided suitable emulsifying properties both in the liquid and in the spray dried emulsions. Moreover, it allowed excellent protection of vitamin E and polyunsaturated fatty acids against oxidation. Hence, P. ostreatus extracts can be exploited as innovative emulsifier to provide physical protection to functional, oxygen sensitive lipophilic ingredients by microencapsulation.

Essential oils are volatile liquids which evaporate and lose their pharmacological effect when exposed to the environment. The aim of this study is to protect nutmeg essential oil from environmental factors by encapsulation (shell material, sodium alginate) and determine the influence of crosslinker concentration (2%, 5% calcium chloride), different emulsifiers (polysorbate 80, sucrose esters), and magnesium aluminometasilicate on microcapsule physical parameters, encapsulation efficiency (EE), swelling index (SI), and other parameters. Nutmeg essential oil (NEO)-loaded calcium alginate microcapsules were prepared by extrusion. The swelling test was performed with and without enzymes in simulated gastric, intestinal, and gastrointestinal media. This study shows that the crosslinker concentration has a significant influence on EE, with 2% calcium chloride solution being more effective than 5%, and capsules being softer with 2% crosslinker solution. Using sucrose esters, EE is higher when polysorbate 80 is used. The swelling index is nearly three times higher in an intestinal medium without enzymes than in the medium with pancreatin. Microcapsule physical parameters depend on the excipients: the hardest capsules were obtained with the biggest amount of sodium alginate, the largest with magnesium aluminometasilicate. Sucrose esters and magnesium aluminometasilicate are new materials used in extrusion.

PTDC/QEQEPR/5841/2014 PTDC/QEQ-FTT/3289/2014 IF/00210/2014/CP1244/CT0003 UIDB/50006/2020 Nowadays, pharmaceutical companies are facing several challenges with the development and approval of new biological products. The unique properties of several fluorinated ionic liquids (FILs), such as their high surfactant power in aqueous solutions, their chemical and biological stability, and low toxicity, favor their application in the pharmaceutical industry. Furthermore, the numerous combinations between cations and anions, in the FILs design, enlarge the possibilities to construct a successful delivery system. Several FILs also proved to not affect the activity, stability, and secondary structure of the therapeutic protein lysozyme. This work aims to study the aggregation behavior of distinct FILs in the protein suitable medium, in the presence or absence of lysozyme. Besides, different incubation conditions were tested to guarantee the optimal enzymatic activity of the protein at more stable delivery systems. Following the optimization of the incubation conditions, the quantification of the encapsulated lysozyme was performed to evaluate the encapsulation efficiency of each FIL-based system. The release of the protein was tested applying variables such as time, temperature, and ultrasound frequency. The experimental results suggest that the aggregation behavior of FILs is not significantly influenced by the protein and/or protein buffer and supports their application for the design of delivery systems with high encapsulation efficiencies, maintaining the biological activity of either encapsulated and released protein. publishersversion published

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

Pluronic® F127 nanoparticles were loaded with citronella essential oil (CEO) and then covered with chitosan-sodium alginate polyelectrolyte complex (PEC). The system was characterized according to size, zeta potential and stability over time. Dynamic light scattering (DLS) in different proportions of water/ethanol as a dispersive medium was important in confirming that PEC covered the F127 nanoparticles. Infrared spectroscopy also indicated interaction of F127 with PEC. The nanoparticle size evaluated by transmission electron microscopy (TEM) and field emission scanning electron microscopy (FESEM) corroborated the value observed in DLS (hydrodynamic radius (RH) range of 100-200 nm). Encapsulation efficiency of 80% for CEO was determined by UV-Vis spectroscopy. The release profile of the CEO was evaluated in phosphate buffer saline (PBS) containing 20% of ethanol and in simulated sweat fluid, achieving 74 and 81%, respectively. The releasing mechanism fitted the Korsmeyer-Peppas mathematical model, indicating Fickian diffusion behavior for both studied media.

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

In this study, development of folic acid-loaded liposomes using a basic amino acid, histidine as a solubilizing agent for folic acid was presented, which tackled the poor solubility of this vitamin. The effect of the liposomal membrane modifiers, cholesterol and SPAN 20 on the characteristics of the final formulations was examined. Liposomes prepared from a commercially available purified soybean lecithin (Phospholipon 90G) by proliposome method were between 503 and 877 nm in average diameter, where cholesterol induced enlargement and SPAN.20 reduction of vesicles. High encapsulation efficiency of 84% and drug loading of 0.123 mg g−1 were achieved, irrespective to the composition. According to AFM images, folic acid-loaded liposomes of a fraction with a nano size were flattened compared to globular empty liposomes. FTIR analysis revealed possible interactions between phospholipids and histidine, while DSC study suggested interactions between folic acid and lipids during heating. Release study done by a Franz diffusion cell showed prolonged release of folic acid from liposomes and the release rate was determined by folic acid solubility. This is the peer-reviewed version of the article: P.M. Batinić, V.B. Đorđević, S.I. Stevanović, B.D. Balanč, S.B. Marković, N.D. Luković, D.Ž. Mijin, B.M. Bugarski, Formulation and characterization of novel liposomes containing histidine for encapsulation of a poorly soluble vitamin, Journal of Drug Delivery Science and Technology, 2020, 59, 101920, doi: [https://doi.org/10.1016/j.jddst.2020.101920] Supplementary information: [https://hdl.handle.net/21.15107/rcub_dais_9518] Published version: [https://hdl.handle.net/21.15107/rcub_dais_9516]

The aim of this study was to improve the stability and antioxidant activity of yarrow phenolic compounds upon an in vitro simulated gastrointestinal digestion. Therefore, two types of caseins-based delivery systems, sodium caseinate stabilized nanoemulsions (NEs) and glucono delta-lactone acidified milk gels (MGs), were formulated containing an ultrasound-assisted yarrow extract (YE) at two concentrations (1 and 2.5 mg/mL). Formulations with 1 mg/mL of YE were chosen based on their higher encapsulation efficiency to perform the in vitro digestion experiments. After digestion, YE-loaded NEs only partially protected phenolic compounds from degradation; meanwhile the phenolic composition of YE including in MGs after digestion was quite similar to undigested YE. Moreover, the antioxidant activity of MGs after digestion was higher than NEs digested samples, which confirms the higher protection of YE phenolic compound by the milk gels systems. This research demonstrated the potential use of acidified MGs as carriers to improve the stability and antioxidant activity of yarrow phenolic compounds. Therefore, these matrices could be employed to develop new dairy products enriched with phenolic compounds., This work was supported by Spanish Government (FORCHRONIC Project: ALG-2016-76736-C3-1-R), by Comunidad Autónoma de Madrid (ALIBIRD project: P2018/BAA-4343) and by the Natural Sciences and Engineering Council of Canada, through the Canada Research Chair programme.

Polyurea, a controlled release material, has been widely applied in agricultural fields due to high thermal stability and low cost. In this article oxyfluorfen polyurea microcapsules suspension was successfully prepared by interfacial polymerization using diisocyanate and polyamines such as Ethylenediamine, Hexamethylenediamine, Diethylenetriamine in presence of green solvent, i.e., N,N-dimethyldecanamide. The microcapsule suspension of oxyfluorfen has not been researched yet by using solvent N,N-dimethyldecanamide and polyamines. The effect and the type of diamines on the morphology and properties of the microcapsules have been investigated. The synthesized microcapsules were characterized by scanning electron microscope, ultraviolet spectrometry, Fourier transform iInfrared spectrometer, thermogravimetric analysis and particle size analyser. The effect of the core to shell ratio on encapsulation efficiency and release kinetics were also studied. The oxyfluorfen microcapsules had an excellent encapsulation efficiency (98.2%) using EDA as the monomer and Release kinetics depended upon the type of monomers used and also on core to shell ratio used (6.5:1, 5:1, 4:1). As core to shell ratio was increased the encapsulation efficiency was found to decrease. Prepared Microcapsules when sprayed on paddy crop was found to be safe in comparison with Emulsifiable concentrate sample.

Made available in DSpace on 2021-06-25T10:52:59Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-01-01 Insulin is an important anabolic hormone that regulates the metabolism of carbohydrates, lipids and proteins. In this study, a reverse-phase liquid chromatography (RP-LC) method was successfully validated and tested for the encapsulation efficiency assay of insulin and in vitro release studies. HPLC analyses were carried out using a RP C18- Luna® Phenomenex (4.6 × 250 mm, 5 μm particle size) column maintained at room temperature, using a mobile phase constituted by a mixture of acetonitrile and 0.1% TFA aqueous solution (60:40, v/v), in an isocratic mode with a flow rate of 1.0 mL/ min, with ultraviolet detection at 214 nm and 20 μL of injection volume. Method validation was performed according recognized guidelines for system suitability, specificity, linearity, precision, accuracy, LOD, LOQ and robustness. The method was shown to be linear in the range of 0.5–100 µg/mL (r2 = 0.9993) selective, precise, robust, accurate with LOD and LOQ values were 0.097 µg/mL and 0.294 µg/mL, respectively. The developed method proved to be adequate to analyze the encapsulation efficiency and the profile of insulin release from liposomes. São Paulo State University (UNESP) School of Pharmaceutical Sciences Department of Drugs and Medicines, Rodovia Araraquara-Jaú, km1 Federal University of Ceará School of Pharmacy Dentistry and Nursing Department of Pharmacy São Paulo State University (UNESP) School of Pharmaceutical Sciences Department of Drugs and Medicines, Rodovia Araraquara-Jaú, km1

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

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

The present study reports the fabrication of hybrid nanoparticles consisting of nickel ferrite (NFO) for anti cancer drug delivery. The hybrid system was formulated from poly(vinyl alcohol)/stearic acid with PEG containing nickel ferrite for zidovudine (AZT) delivery. The nickel ferrite nanoparticles were characterized by XRD and TEM analysis. The hybrid nanoparticles were characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM), and their influence on biological systems was evaluated by blood compatibility and cell viability studies. The encapsulation of AZT into the hybrid nanoparticles was assessed by evaluating the drug loading, encapsulation efficiency and release studies. The advantages of incorporating magnetic nanoparticles into self-assembled hybrid nanoparticles include the ability to load large amounts of drugs along with control over drug release. In this regard, the presented nickel ferrite reinforced hybrid nanoparticles containing zidovudine is a demanding platform that can act in a pH responsive manner enabling site specific intracellular anticancer drug delivery. Its impact is therefore noteworthy, extensive, and prevalent in cancer therapy. Scopus

Drug-loaded poly (vinyl alcohol) (PVA)-based microparticles have been synthetized by using membrane emulsification and chemical cross-linking. The encapsulation of two water-soluble molecules, catechol (CA) and diclofenac sodium (DS), has been considered as case studies. PVA hydrogels have been recognized as promising biomaterials and suitable candidates for drug delivery. However, the encapsulation of hydrophilic, low molecular weight drugs in particulate materials is currently an ambitious goal. The purpose of this work was to develop high-drug loading systems for hydrophilic molecule delivery based on uniformly distributed particulate carriers. Membrane emulsification has been used as advanced manufacturing method to design drug-loaded PVA microparticles with target properties in terms of particle size, particle size distribution, structure and functional activity. A special emphasis is laid on the important factors that contribute to tune the structured properties of microparticles, encapsulation efficiency/drug loading and drug delivery. In particular, the influence of emulsification method (membrane and homogenizing approaches), phase compositions (PVA concentration, drug concentration, physicochemical properties of drug), cross-linking reaction conditions (cross-linking agent concentration, acidic media) has been studied. Finally, the potential of PVA-based microparticles as drug delivery carriers as well as their in vitro cytotoxicity have been evaluated., The authors acknowledge for the financial support the project PON01_01545, Olio più, within the framework PON Ricerca e Competitività 2007-2013.