Nutraceutical Delivery Research Articles

Curcumin encapsulated zein/caseinate-alginate nanoparticles: Release and antioxidant activity under in vitro simulated gastrointestinal digestion

Curcumin-loaded zein/sodium caseinate-alginate nanoparticles were successfully fabricated using a pH-shift method/electrostatic deposition method. These nanoparticles produced were spheroids with a mean diameter of 177 nm and a zeta-potential of −39.9 mV at pH 7.3. The curcumin was an amorphous, and the content in the nanoparticles was around 4.9% (w/w) and the encapsulation efficiency was around 83.1%. Aqueous dispersions of the curcumin-loaded nanoparticles were resistant to aggregation when subjected to pH changes (pH 7.3 to 2.0) and sodium chloride addition (1.6 M), which was mainly attributed to the strong steric and electrostatic repulsion provided by the outer alginate layer. An in vitro simulated digestion study showed that the curcumin was mainly released during the small intestine phase and that its bioaccessibility was relatively high (80.3%), which was around 5.7-fold higher than that of non-encapsulated curcumin mixed with curcumin-free nanoparticles. In the cell culture assay, the curcumin reduced reactive oxygen species (ROS), increased superoxide dismutase (SOD) and catalase (CAT) activity, and reduced malondialdehyde (MDA) accumulation in hydrogen peroxide-treated HepG2 cells. The results suggested that nanoparticles prepared by pH shift/electrostatic deposition method are effective at delivering curcumin and may be utilized as nutraceutical delivery systems in food and drug industry.

Development of food-grade oleogel via the aerogel-templated method: Oxidation stability, astaxanthin delivery and emulsifying application

Templates for the fabrication of food-grade oleogels were prepared by freeze-drying of whey protein isolate (WPI)–carboxymethyl chitosan (CMCS) heat-set hydrogels, and the effect of the concentration of CMCS on aerogel properties was explored. It was observed that both the oil adsorption capacity and oil binding capacity were significantly improved when the CMCS concentration was up to 0.75% (w/w). With the further increase of CMCS concentration, the oil absorption capacity decreased. Scanning electric microscopy images exhibited that the corresponding aerogel showed dense and uniform porous networks. Compared with bulk oil, WPI–CMCS aerogel gel showed excellent oxidation stability. In addition, the delivery efficiency of aerogel-based oleogels as nutraceutical delivery carriers for astaxanthin (AST) was assessed. The bioaccessibility of AST in WPI–CMCS oleogels was significantly higher than that of bulk oil. Finally, the emulsification of aerogel-based oleogels was tested by TSI and droplet size. In comparison with WPI oleogel, the WPI–CMCS oleogel exhibited better physical stability and smaller droplet size. This work indicates that the path of oil structuring is not limited to the selection of existing oleogelators. The construction of aerogel templates from various protein/polysaccharide for oil absorption is also a promising path. • Oleogel could be prepared from whey protein isolate–carboxymethyl chitosan aerogel. • Aerogel-based oleogels (AOs) exhibited superior oxidation stability. • AOs could serve as efficacious vehicles for hydrophobic nutraceuticals. • AOs improved the lipolysis rate and the bioaccessibility of astaxanthin. • The prepared AO-based emulsion showed superior physical stability.

Oral supplementation of solvent-free kynurenic acid/cyclodextrin nanosponges complexes increased its bioavailability

Many nutraceuticals present problems due to their poor water solubility or stability, which prevents the final bioactivity achievement. For that reason, the oral administration of KYNA complexed with HPβ-CD and βNS-CDI nanosponges was evaluated in mice. The solvent-free technology was used to prepare the complexes in a complete comparison between kneading in ball milling and classical inclusion complex preparation. The solvent-free ones showed higher strength and efficiency with ball milling, considerably reducing time. A 50 mg KYNA/kg/day dosage was orally administered in formulations showing a higher bioavailability when the nutraceutical was complexed with βNS-CDI compared to HPβ-CD and free KYNA, respectively. Several antioxidant statuses demonstrated a higher global antioxidant level perfectly related to bioavailability. Finally, the formulation of KYNA reduced the temporal oxidative stress damage in the kidney and liver, making βNS-CDI the best formulation. These results suggest an important future application of cyclodextrin-based nanosponges for the oral delivery of nutraceuticals and their stabilization.

Chitosan on the surface of nanoparticles for enhanced drug delivery: A comprehensive review.

The ability of chitosan (CTS) to promote mucoadhesion, trigger positive/negative surface interactions, and open tight junctions has inspired researchers to coat lipid-based and polymeric-based nanoparticles with CTS in an attempt to reach new heights in the delivery of drugs and nutraceuticals across different routes. This article discusses literature relevant to the pharmaceutical and biomedical area published in the last 10years on nanoparticles overlaid with CTS. Herein, we addressed the technical aspects of the coating procedure by adding CTS solution to nanoparticles that have already been produced or during the production phase. Besides, we reviewed the applications of CTS coated nanoparticles as drug delivery systems in the oral and non-oral routes of administrations. Special attention was paid to the physicochemical and biological benefits of the CTS coating, such as improving physicochemical stability, enhancing cell and tissue interactions, controlled drug release, and augmentation of active substance bioavailability and efficacy. Moreover, this review projects the current standing and future prospects of the delivery system. The future calls for more investigations on therapeutic proteins, genes and vaccines as potential cargos. Extensive studies on the merits of integrating CTS with hydropolymer-synthesized nanoparticles and using longer-chain and chemically-modified variants of CTS are also warranted.

Microbial Polysaccharide-Based Nanoformulations for Nutraceutical Delivery.

In recent times, nutrition and diet have become prominent health paradigms due to sedentary lifestyle disorders. Preventive health care strategies are becoming increasingly popular instead of treating and managing diseases. A nutraceutical is an innovative concept that offers additional health benefits beyond its fundamental nutritional value. These nutraceuticals have the potential to reduce the exorbitant use of synthetic drugs because the modern medicine approach of treating diseases with high-tech, expensive supplements, and long-term consequences aggravates consumers. However, most nutraceuticals are plant-derived, making them susceptible to degradation and prone to chemical instability, poor solubility, unpleasant taste, and bioactivity loss before absorption to the targeted site. To counteract this problem, the bioavailability of these labile compounds can be maximized by encapsulating them in protective nanocarriers. It is crucial that nanoencapsulation technologies convert bioactive compounds into forms that can be easily combined with functional foods and beverages without adversely affecting their organoleptic properties. In recent years, nanoformulations using food-grade materials, such as polysaccharides, proteins, lipids, etc., have received considerable attention. Among them, microbial polysaccharides are biocompatible, nontoxic, and nonimmunogenic, and most of them are US-FDA approved and can undergo tailored modifications. The nanoformulation of microbial polysaccharide is a relatively new frontier which has several advantages over existing systems. The present article, for the first time, comprehensively reviews microbial polysaccharides-based nanodelivery systems for nutraceuticals and discusses various techno-commercial aspects of these nanotechnological preparations. Moreover, this has also attempted to draw a future research perspective in this area.

Physical and functional properties of plant-based pre-emulsified chewable gels for the oral delivery of nutraceuticals

Gelatin-based pre-emulsified chewable gels have presented advantages over traditional tablets, bulk oils, hard and soft capsules for oral delivery. Ethical, ecological, and religious considerations have increased the demand for plant-based gelling agents which can be formulated into chewable emulsion gels. Plant-based polysaccharide emulsion gels prepared with agar and pectin were compared to gelatin emulsion gels regarding rheological, textural, and functional properties. The agar emulsion gel had higher gelling/melting temperatures (Tg: 40 °C, Tm: 90 °C) than the gelatin emulsion gel (Tg: 37 °C, Tm: 45 °C), whereas pectin emulsion gel had a more similar gelling/melting profile to the gelatin formulation (Tg: 38 °C, Tm: 54 °C). Texture analyses revealed that the agar emulsion gel had a harder and more brittle texture, whereas pectin emulsion gel had a softer texture than the gelatin emulsion gel. Pectin emulsion gels had the largest average droplet size (32 μm), followed by agar (13 μm) and gelatin emulsion gels (1 μm). The in vitro lipolysis experiments indicated that the polysaccharide emulsion gels were lipolyzed to a lower extent and had a slower initial lipolysis rate (agar: 2.8 μmol FFA/sec, pectin: 4.3 μmol FFA/sec), compared to the gelatin emulsion gel (24.9 μmol FFA/sec). The industrial potential and challenges of the polysaccharide emulsion gels were evaluated, and the results show that plant based pre-emulsified chewable gels can be manufactured for the oral delivery of nutraceuticals.

Potential Utility of Ultrasound-Enhanced Delivery of Antibiotics, Anti-Inflammatory Agents, and Nutraceuticals: A Mini Review.

Ultrasound technology has therapeutic properties that can be harnessed to enhance topical drug delivery in a process known as phonophoresis. The literature on this method of drug delivery is currently sparse and scattered. In this review, we explore in vivo and in vitro controlled trials as well as studies detailing the mechanism of action in phonophoresis to gain a clearer picture of the treatment modality and explore its utility in chronic wound management. Upon review, we believe that phonophoresis has the potential to aid in chronic wound management, particularly against complicated bacterial biofilms. This would offer a minimally invasive wound management option for patients in the community.

Enhancing emulsion stability and performance using dual-fibrous complexes: Whey protein fibrils and cellulose nanocrystals

Edible proteins can self-assemble into fibrils, which can improve their performance as emulsifiers. However, they are limited in some food applications. We prepared whey protein isolate fibril-cellulose nanocrystal complexes (WPIF-CNC) by electrostatic complexation. The stabilities of emulsions prepared using either WPIF or WPIF-CNC were compared to evaluate the effect of complexation on emulsion formation and properties. Moreover, the potential of the emulsions to act as delivery systems for curcumin was investigated. WPIF and CNC were found to complex by hydrogen bonding, hydrophobic, and electrostatic interactions. The complexes formed were good Pickering stabilizers in oil-in-water emulsions. Emulsions formulated using the complexes were more resistant to creaming than those stabilized by WPIF. The complexes were able to form self-supporting gelled emulsions at 70 % oil concentration, which protected curcumin from photo- and thermal-degradation. Consequently, dual-fibrous complexes may have application in the food industry as novel emulsifiers for the creation of nutraceutical delivery systems.

Protective effect of surfactant modified phytosterol oleogels on loaded curcumin.

Oleogels represent one of the most important carriers for the delivery of lipophilic nutraceuticals. Phytosterols (PS), plant-derived natural sterol compounds, are preferred for oleogel preparation due to their self-assembly properties and health function. However, the relationship between the physical properties of PS-based oleogels and the chemical stability of loaded bioactive compounds is still unclear. The influence of lecithin (LC) and glycerol monostearate (GMS) on the physical properties of PS-based oleogels made of liquid coconut oil and the stability of curcumin as a model bioactive loaded in the oleogels was investigated. Results showed that the flow consistency index was much higher for GMS-containing oleogels than that for LC-containing oleogels. The optical microscopy and X-ray scattering analysis showed that the addition of GMS in the PS oleogels promoted the formation of a crystal mixture with different crystal polymorph structures, whereas LC addition promoted the formation of needle-like crystals of PS. Using curcumin as a model lipophilic nutraceutical, the GMS-enriched PS oleogels with high crystallinity and flow consistency index exhibited a good retention ratio and scavenging activity of the loaded curcumin when stored at room temperature. This study shows that enhancing the firmness of oleogels made from PS and liquid coconut oil is beneficial to the retention and chemical stability of a loaded bioactive (curcumin). The findings of the study will boost the development of PS-based oleogel formulations for lipophilic nutraceutical delivery. © 2022 Society of Chemical Industry.

Investigation of Factors Influencing Formation of Nanoemulsion by Spontaneous Emulsification: Impact on Droplet Size, Polydispersity Index, and Stability.

Interest in nanoemulsion technology has increased steadily in recent years for its widespread applications in the delivery of pharmaceuticals, nutraceuticals, and cosmeceuticals. Rational selection of the composition and the preparation method is crucial for developing a stable nanoemulsion system with desired physicochemical characteristics. In the present study, we investigate the influence of intricate factors including composition and preparation conditions that affect characteristic parameters and the stability of the nanoemulsion formation prepared by the spontaneous emulsification method. Octanoic acid, capryol 90, and ethyl oleate were selected to represent oil phases of different carbon–chain lengths. We explored the impact of the addition mode of the oil–Smix phase and aqueous phase, vortexing time, Km (surfactant/cosurfactant) ratio, and the replacement of water by buffers of different pH as an aqueous system. The phase behavior study showed that the Smix phase had a significant impact on the nanoemulsifying ability of the nanoemulsions composed of oil phases of varying carbon-chain lengths. The mode of mixing of the oil–Smix phase to the aqueous phase markedly influenced the mean droplet size and size distribution of the nanoemulsions composed of oil phases as capryol 90. Vortexing time also impacted the mean droplet size and the stability of the generated nanoemulsion system depending on the varying carbon-chain length of the oil phase. The replacement of the water phase by aqueous buffers of pH 1.2, 5.5, 6.8, and 7.4 has altered the mean droplet size and size distribution of the nanoemulsion system. Further, the Km ratio also had a significant influence on the formation of the nanoemulsion system. The findings of this investigation are useful in understanding how the formulation composition and process parameters of the spontaneous emulsification technique are responsible for affecting the physicochemical characteristics and stability of the nanoemulsion system composed of oil of varying carbon-chain (C8-C18) length.

Transdermal Nutraceuticals Delivery System for CNS Disease.

Herbal medicines are being used by humans since the oldest civilizations and have been an integral part of traditional and alternative medicines. In recent times, pharmaceutical and biomedical scientists are taking interest in developing nutraceutical-based medicines to overcome the side effects and adverse drug reactions caused by allopathic medicines. Nutraceuticals have started occupying the global market. Nutraceuticals have gained widespread acceptance due to their efficacy in treating difficult to treat diseases, low toxicity, low cost, easy accessibility, etc. Safety and efficacy are other important factors in the commercialization process of nutraceuticals. Different novel advanced drug delivery systems have been constantly studied to improve the efficacy and bioavailability of medicines obtained from herbal sources. The transdermal drug delivery system provides a potent alternative to the conventional method of using nutraceuticals. The development of transdermal system-based nutraceuticals could provide the advantage of enhanced bioavailability, improved solubility, bypass of the first-pass metabolism, and targeted delivery of drugs in brain-related disorders. It additionally provides the advantage of being non-invasive. This article reviews the potential effects of various nutraceuticals in brain-related disorders as well as trends in transdermal nano-systems to deliver such nutraceuticals. We have also focused on advantages, applications as well as recent United States-based patents which emphasize emerging interest towards transdermal nutraceuticals in brain disorders.

Modulation of Fabrication and Nutraceutical Delivery Performance of Ovalbumin-Stabilized Oleogel-Based Nanoemulsions via Complexation with Gum Arabic.

Protein–polysaccharide complexes, which involve Maillard-type protein–polysaccharide conjugates and electrostatic protein–polysaccharide complexes, have the potential to stabilize oleogel-based nanoemulsions for nutraceutical delivery. Here, ovalbumin (OVA) and gum arabic (GA) were used to prepare OVA–GA conjugate (OGC) and OVA–GA mixture (OGM), followed by the fabrication of astaxanthin-loaded oleogel-based nanoemulsions. Carnauba wax (5% w/w) and rice bran oil were mixed to prepare food-grade oleogel. The successful preparation of OGC was verified by means of SDS-PAGE analysis and free amino groups determination. OGC endowed oleogel-based nanoemulsions with smaller emulsion droplets and higher stability during 30-day storage, implying more outstanding emulsifying capability than OGM. Both OGC-stabilized nanoemulsions and OGM-stabilized nanoemulsions could enhance the extent of lipolysis and the bioaccessibility of astaxanthin compared with oleogel. Meanwhile, OGC exhibited significantly better than OGM, which indicated that OGC-stabilized oleogel-based nanoemulsions possessed more desirable nutraceutical delivery performance than OGM-stabilized oleogel-based nanoemulsions. This study may fill a gap in the influence of different protein–polysaccharide complexes on oleogel-based nanoemulsions and contribute to deeper insights about novel oleogel-based nanoemulsions for their applications in the food industry.

PH-Responsive Hydrogel Beads Based on Alginate, κ-Carrageenan and Poloxamer for Enhanced Curcumin, Natural Bioactive Compound, Encapsulation and Controlled Release Efficiency.

Polyphenolic compounds are used for treating various diseases due to their antioxidant and anticancer properties. However, utilization of hydrophobic compounds is limited due to their low bioavailability. In order to achieve a greater application of hydrophobic bioactive compounds, hydrogel beads based on biopolymers can be used as carriers for their enhanced incorporation and controlled delivery. In this study, beads based on the biopolymers-κ-carrageenan, sodium alginate and poloxamer 407 were prepared for encapsulation of curcumin. The prepared beads were characterized using IR, SEM, TGA and DSC. The curcumin encapsulation efficiency in the developed beads was 95.74 ± 2.24%. The release kinetics of the curcumin was monitored in systems that simulate the oral delivery (pH 1.2 and 7.4) of curcumin. The drug release profiles of the prepared beads with curcumin indicated that the curcumin release was significantly increased compared with the dissolution of curcumin itself. The cumulative release of curcumin from the beads was achieved within 24 h, with a final release rate of 12.07% (gastric fluid) as well as 81.93% (intestinal fluid). Both the in vitro and in vivo studies showed that new hydrogel beads based on carbohydrates and poloxamer improved curcumin’s bioavailability, and they can be used as powerful carriers for the oral delivery of different hydrophobic nutraceuticals.

A Comprehensive Review on Nanotechnological Approaches for Enhanced Delivery of Nutraceuticals in the Management of Osteoporosis

Abstract:Osteoporosis is a chronic, progressive bone condition that is most prevalent in postmen-opausal women and the elderly population. An imbalance in the natural bone remodeling process, which is involved in the formation of bone and resorption, is responsible for osteoporosis, leading to bone fragility. It shows no clinical manifestation until a fracture takes place. Osteoporosis is a glob-al epidemic that reduces the quality of life, increases the chances of disabilities, and adds on a huge financial load. Early diagnosis and treatment can help in preventing the disease. Several drug regi-mens are used in treating the condition; however, the drugs are accompanied by several adverse ef-fects. Nutraceuticals, like herbs, minerals, vitamins, and dairy products, support skeletal strength and integrity. Therefore, the use of different types of nutraceuticals can improve overall bone strength and provide improved treatment of osteoporosis. The review paper focuses on providing in-depth knowledge about the various nutraceuticals that are used in the management of osteoporosis along with the novel nanotechnology-based delivery approaches for enhanced delivery of nutraceu-ticals as the advent of nanotechnology in pharmaceuticals have opened new avenues in the chal-lenging arena of nutraceuticals for providing benefits like stability, higher efficiency, solubility, en-hanced bioavailability, permeability, and production without additives.

Fast-dissolving antioxidant nanofibers based on Spirulina protein concentrate and gelatin developed using needleless electrospinning

Spirulina is a microalga that is well-known for its high protein content and biological activities directly related to its antioxidant capacity. The objective of this study was to produce fast-dissolving antioxidant nanofibers based on Spirulina protein concentrate (SPC) and gelatin using needleless electrospinning technique. The effect of mixing ratios of SPC (10% w/w) and gelatin (20% w/w) on the viscosity, electrical conductivity and surface tension of electrospinning solutions as well as diameter and morphology of resulting nanofibers was investigated. Increasing the SPC level in the solution blends resulted in a decrease in apparent viscosity and electrical conductivity and an almost stable trend in surface tension (29.25–32.19 mN/m) that led to diminish of diameter of the nanofibers. Scanning electron microscopy images showed that SPC/gelatin ratio of 40:60 led to the production of uniform and bead-free nanofibers with a relatively smaller average diameter (208.7 ± 46.5 nm). Atomic force microscopy images indicated mesh-like, fibrillary, and bead-free structures. Fourier transform infrared spectroscopy verified the formation of composite nanofibers and intermolecular interactions between both proteins. X-ray diffraction and thermal analysis showed higher amorphous structure and stability of produced SPC/gelatin nanofibers in comparison to pure materials which was favorable for formation of stable fast-dissolving fibers. Results of DPPH and ABTS radical scavenging activities showed that the antioxidant activity of composite nanofibers significantly improved with increasing SPC mixing ratio (p < 0.05). The dissolution test demonstrated that SPC/gelatin nanofibers can be rapidly dissolved in aqueous medium within 2 s. Finally, the results indicated that the electrospun SPC/gelatin nanofibers could be potentially used for nutraceutical delivery in food and packaging applications under high humidity.

Phospholipid and menthol based nanovesicle impregnated transdermal patch for nutraceutical delivery to diminish folate and iron deficiency

Adequate micronutrient availability is particularly important in women, children and infants. Micronutrient deficiencies are the major cause of maternal and neonatal morbidity. To overcome this, WHO recommends the use of folic acid and iron supplements for reducing anaemia and improving the health of the mother and infants. Oral intake of supplements for nutritional deficiencies are associated with gastric irritation, nausea, constipation and non-patient compliance due to associated taste. In case of absorption deficiency nutrients administered orally pass-through digestive tract unabsorbed. In the present study, we propose transdermal delivery of nutraceuticals to avoid the limitations associated with oral intake. Transdermal delivery has limited use because of the closely packed barrier of the stratum corneum that limits the permeability of molecules across skin. Here, we have used biomimetic nanovesicles impregnated in transdermal patches for delivery of folic acid and iron. Nanovesicles are prepared using an abundant component of cell membrane, phosphatidyl choline and a permeation enhancer. Further these nanovesicles are impregnated onto polyacrylate based transdermal patch. In vitro studies have shown the ability of nanovesicles to fluidise skin lipids and penetrate into deeper skin. In vivo application of transdermal patches gradually increased the systemic concentration of nutraceuticals. Post application of the patch, five-fold increase in plasma folic acid concentration and 1.5-fold increase in plasma iron concertation was achieved in 6 h. Developed nanovesicles were compatible with keratinocytes and fibroblasts as tested in vitro and have the potential to enhance the cellular uptake of molecules. Skin irritation studies on human volunteers have confirmed the safety of nutraceutical loaded nanovesicles. Thus, the developed nutraceutical loaded transdermal patches provide a potential, easy to use platform for micronutrient delivery in infants and mothers.

Nutraceutical Concepts and Dextrin-Based Delivery Systems.

Nutraceuticals are bioactive or chemical compounds acclaimed for their valuable biological activities and health-promoting effects. The global community is faced with many health concerns such as cancers, cardiovascular and neurodegenerative diseases, diabetes, arthritis, osteoporosis, etc. The effect of nutraceuticals is similar to pharmaceuticals, even though the term nutraceutical has no regulatory definition. The usage of nutraceuticals, to prevent and treat the aforementioned diseases, is limited by several features such as poor water solubility, low bioavailability, low stability, low permeability, low efficacy, etc. These downsides can be overcome by the application of the field of nanotechnology manipulating the properties and structures of materials at the nanometer scale. In this review, the linear and cyclic dextrin, formed during the enzymatic degradation of starch, are highlighted as highly promising nanomaterials- based drug delivery systems. The modified cyclic dextrin, cyclodextrin (CD)-based nanosponges (NSs), are well-known delivery systems of several nutraceuticals such as quercetin, curcumin, resveratrol, thyme essential oil, melatonin, and appear as a more advanced drug delivery system than modified linear dextrin. CD-based NSs prolong and control the nutraceuticals release, and display higher biocompatibility, stability, and solubility of poorly water-soluble nutraceuticals than the CD-inclusion complexes, or uncomplexed nutraceuticals. In addition, the well-explored CD-based NSs pathways, as drug delivery systems, are described. Although important progress is made in drug delivery, all the findings will serve as a source for the use of CD-based nanosystems for nutraceutical delivery. To sum up, our review introduces the extensive literature about the nutraceutical concepts, synthesis, characterization, and applications of the CD-based nano delivery systems that will further contribute to the nutraceutical delivery with more potent nanosystems based on linear dextrins.

Molecular dynamics simulations of duodenal self assembly in the presence of different fatty acids

A comprehensive understanding of dietary mixed micelle formation in the presence of lipid digestion products is crucial for an effective design of nutraceutical delivery systems. This study aimed to investigate the duodenal self-assembly of bile lipids and fatty acids (FA) with different characteristics via coarse-grained molecular dynamics (MD) simulations. The results show that increase in FA chain length and unsaturation degree lead to micelles with lower/higher fractions of FAs/bile salts (BS), lower core and surface packing densities, decreased ordering of lipid tails, thus more fluid internal structures. Our findings provide molecular insight into the instability of intestinal colloidal structures composed of long unsaturated FAs. We show the correlation between FA unsaturation degree and lipid packing density is a significant factor in determining the intermicellar BS concentrations. Overall, this study advances the knowledge in the field by establishing a more integral relationship between the FA characteristics and micelle structural properties over a wider range of FA types through MD simulations.

Cyclodextrin-based metal–organic framework nanoparticles as superior carriers for curcumin: Study of encapsulation mechanism, solubility, release kinetics, and antioxidative stability

In this paper, we propose a facile program of preparing nanoscale γ-cyclodextrin-based metal–organic frameworks (Nano-CD-MOFs) for the encapsulation of curcumin. Such Nano-CD-MOFs not only possess excellent mono-dispersity and crystalline structure, but also perform superior loading capacity. The results of N2 adsorption–desorption, XRD, DSC, and microtopography are utilized to confirm the presence status of encapsulated curcumin and further reveal the encapsulation mechanism of Nano-CD-MOFs. Curcumin-loaded Nano-CD-MOFs (Cur-Nano-CD-MOFs) dramatically increase curcumin solubility and a top-down uniform dispersion in the dissolution process. The perfect fitting of First-order and Korsmeyer-Peppas models suggests that the release performance of Nano-CD-MOFs is controlled by the loaded quantity of curcumin and related to Fickian diffusion. Moreover, the antioxidative stability of Cur-Nano-CD-MOFs is considerably enhanced even after 120 min of persistent ultraviolet irradiation. Therefore, we suggest that such Nano-CD-MOFs can be promoted as an advanced carrier for the delivery of curcumin or other nutraceuticals.

Ferulic acid loaded pickering emulsions stabilized by resistant starch nanoparticles using ultrasonication: Characterization, in vitro release and nutraceutical potential

The use of starch based nanoparticles have gained momentum in stabilizing pickering emulsions for it’s numerous advantages. In present study resistant starch (RS) was isolated from lotus stem using enzymatic digestion and subjected to nanoprecipitation and ultrasonication to yield resistant starch nanoparticles (RSN). RSN of varying concentrations (2%, 10% and 20%) were used to stabilize the flax seed-oil water mixture to form pickering emulsions. The emulsions were used to nanoencapsulate ferulic acid (FA) – a well known bioactive via ultrasonication. The emulsions were lyophilized to form FA loaded lyophilized pickering emulsion (FA-LPE). The FA-LPE (2%, 10 % and 20%) were characterized using dynamic light scattering (DLS), light microscopy, scanning electron microscopy (SEM), transmission electron microscopy (TEM), atomic force microscopy (AFM) and attenuated total reflectance fourier transform infra-spectroscopy (ATR-FTIR). AFM showed FA-LPE as spherical droplets embedded in the matrix with maximum peak height of 8.47 nm and maximum pit height of 1.69 nm. SEM presented FA-LPE as an irregular and continuous surface having multiple folds and holes. The ATR-FTIR spectra of all the samples displayed peaks of C = C aromatic rings of FA at 1600 cm−1 and 1439 cm−1, signifying successful encapsulation. In vitro release assay displayed more controlled release of FA from FA-LPE (20%). Bioactivity of FA-LPE was evaluated in terms of anti-cancer, anti-diabetic, angiotensin converting enzyme (ACE) inhibition and prevention against oxidative damage under simulated gastro-intestinal conditions (SGID). The bioactivity of FA-LPE (20%) was significantly higher than FA-LPE (2%) and FA-LPE (10%). Key findings reveal that pickering emulsions can prevent FA under harsh SGID conditions and provide an approach to facilitate the design of pickering emulsions with high stability for nutraceutical delivery in food and supplement products.