Development of Chrysin Loaded Oil-in-Water Nanoemulsion for Improving Bioaccessibility (original) (raw)

Encapsulation of bioactive compounds in nanoemulsion- based delivery systems

Procedia Food Science, 2011

Encapsulation into nanoemulsion-based delivery systems of bioactive compounds characterized by low solubility in aqueous phase, represents an effective approach to improve the dispersion of the bioactives into food products, to protect them against degradation or interaction with other ingredients, to reduce the impact on organoleptic properties of the food and to improve their bioavailability. The aim of the present work is the fabrication of nanoemulsions, based on natural food ingredients, to be used as delivery systems of two different bioactive compounds, resveratrol and curcumin, with the ultimate goal of improving the antioxidant and/or antimicrobial activities of the encapsulated compounds. A preliminary screening study of the optimal emulsion ingredients was carried out through the construction of a pseudo-ternary phase diagram of kinetic stability. The formation of very fine emulsions in the nanometric range (< 200 nm) was achieved by high pressure homogenization treatment, choosing those formulations containing small amounts of emulsifier, in order to minimize the impact on the organoleptic properties. Resveratrol (0.01% wt) was encapsulated in peanuts oil-based nanoemulsions, using different emulsifiers, such as soy lecithin and sugar esters. Curcumin was encapsulated in stable solid fat nanoemulsions, using stearic acid as lipid phase, up to 0.1% wt concentration. The nanoemulsions were characterized in terms of physical stability of the mean droplet size (dynamic light scattering) and chemical stability of the encapsulated bioactive compounds (HPLC and UV-Vis spectra analysis) upon accelerated ageing conditions. The effectiveness of the delivery systems was evaluated in terms of antioxidant activity of the encapsulated compounds.

Physicochemical Characterization of Chrysin-Derivative-Loaded Nanostructured Lipid Carriers with Special Reference to Anticancer Activity

Journal of Surfactants and Detergents, 2018

Homologues long-chain chrysin derivatives (LCD, C n : 8-18) were synthesized and incorporated into nanostructured lipid carriers (NLC) with the aim to treat human neuroblastoma. Mutual miscibility and attractive interactions among the NLC components, namely tripalmitin (TP), cetyl palmitate (CP), oleic acid (OA), and the chrysin (CHR) derivatives (LCD) at the air-water interface were assessed by the Langmuir monolayer approach. Optimum combination for the NLC formulations was found to be 2:2:1 (M/M/M) for TP/CP/OA, respectively. NLC formulations, both in the absence and presence of LCD, were characterized by combined dynamic light scattering, electron microscopy, atomic force microscopy, and differential scanning calorimetry. The size and zeta potential of the NLC formulations were found in the range 200-350 nm and −12 to −18 mV, respectively. Encapsulation efficiency and release kinetics of CHR and LCD when loaded into NLC were also evaluated. LCD exhibited maximum incorporation, drug-loading capacity, and sustained release because of its enhanced hydrophobicity. Superior incorporation efficiency and sustained-release profile of LCD were able to enhance their anticancer activity against human neuroblastoma cell lines, compared to CHR, making them promising agents in combating cancer.

Nanoemulsion-based delivery systems for poorly water-soluble bioactive compounds: Influence of formulation parameters on polymethoxyflavone crystallization

Food Hydrocolloids, 2012

Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures.

Encapsulation and Delivery of Crystalline Hydrophobic Nutraceuticals using Nanoemulsions: Factors Affecting Polymethoxyflavone Solubility

Food biophysics, 2012

Polymethoxyflavones (PMF) isolated from citrus peel have potent anti-cancer activity, however their utilization as functional ingredients in foods is currently limited because of their high melting point and poor water-solubility. The influence of oil type and concentration, hydrophilic polymer addition, and simulated intestinal conditions on PMF (5-hydroxytangeretin) solubility in solutions and nanoemulsions was examined. The saturation concentration of PMF in water was relatively low (0.93 µM), but could be increased appreciably by adding certain hydrophilic polymers: polyethylene glycol (PEG) and β-cyclodextrin (CD) were ineffective at increasing solubility, but poly(vinyl alcohol) (PVA) and hydroxypropyl methylcellulose (HPMC) greatly enhanced solubility (e.g., > 6 µM for 0.5 % polymer). PMF was more soluble in medium chain triglycerides (MCT, 6.1 mM) than long chain triglycerides (LCT, 4.2 mM). The encapsulation efficiency of PMF in oil-in-water nanoemulsions was higher when...

Encapsulation of Lipid-Soluble Bioactives by Nanoemulsions

Molecules, 2020

Lipid-soluble bioactives are important nutrients in foods. However, their addition in food formulations, is often limited by limited solubility and high tendency for oxidation. Lipid-soluble bioactives, such as vitamins A, E, D and K, carotenoids, polyunsaturated fatty acids (PUFA) and essential oils are generally dispersed in water-based solutions by homogenization. Among the different homogenization technologies available, nanoemulsions are one of the most promising. Accordingly, this review aims to summarize the most recent advances in nanoemulsion technology for the encapsulation of lipid-soluble bioactives. Modern approaches for producing nanoemulsion systems will be discussed. In addition, the challenges on the encapsulation of common food ingredients, including the physical and chemical stability of the nanoemulsion systems, will be also critically examined.

Plant-Based Colloidal Delivery Systems for Bioactives

Molecules

The supplementation of plant-based foods and beverages with bioactive agents may be an important strategy for increasing human healthiness. Numerous kinds of colloidal delivery systems have been developed to encapsulate bioactives with the goal of improving their water dispersibility, chemical stability, and bioavailability. In this review, we focus on colloidal delivery systems assembled entirely from plant-based ingredients, such as lipids, proteins, polysaccharides, phospholipids, and surfactants isolated from botanical sources. In particular, the utilization of these ingredients to create plant-based nanoemulsions, nanoliposomes, nanoparticles, and microgels is covered. The utilization of these delivery systems to encapsulate, protect, and release various kinds of bioactives is highlighted, including oil-soluble vitamins (like vitamin D), ω-3 oils, carotenoids (vitamin A precursors), curcuminoids, and polyphenols. The functionality of these delivery systems can be tailored to sp...

NC-ND license Oral delivery of fish oil in oil-in-water nanoemulsion: development, colloidal stability and modulatory effect on in vivo inflammatory induction in mice

BIOMEDICINE & PHARMACOTHERAPY, 2021

To improve the oral absorption of fish oil and test its anti-inflammatory effect, a fish oil nanoemulsion was developed using cis-4,7,10,13,16,19-docosahexaenoic fatty acid as a biomarker for oral administration. The colloidal stability tests of the fish oil nanoemulsion showed an average size of 155.44 nm ± 6.46 (4 °C); 163.04 nm ± 9.97 (25 °C) and polydispersity index 0.22 ± 0.02 (4 °C), 0.21 ± 0.02 (25 °C), indicating systems with low polydispersity and stable droplets. The fish oil nanoemulsion did not alter the cell viability of the RAW 264.7 macrophages and, at a concentration of 0.024 mg/mL, was kinetically incorporated into the cells after 18 h of contact. The nanoemulsion was maintained in the gastrointestinal region for a significantly shorter period of time (p ≤ 0.05) compared to the intake of fish oil in free form. Inflammatory tests demonstrated that nanoemulsion and fish oil showed less (p ≤ 0.05) neutrophil infiltration after 24h of sepsis induction and there was a significant reduction (p ≤ 0.05) in the volume of paw edema in female adult Balb/c mice who received the nanoemulsion diet compared to the other experimental groups (control, formalin, fish oil and sunflower oil). These results indicate that the fish oil nanoemulsion was significantly effective in the dietary conditions tested here, presenting satisfactory responses in the modulation of inflammatory disorders, demonstrating interesting and beneficial nutraceutical effects.

Review article on nanoemulsions and nanostructured lipid carriers

Records of Pharmaceutical and Biomedical Sciences, 2018

Lipid nanoparticles, including nanoemulsions (NEs) and nanostructured lipid carriers (NLCs) are colloidal carriers with a lipid matrix that is solid at body temperature. These colloidal carriers have attracted increasing interest for their use in therapeutic and cosmetic applications. The performance of lipid nanoparticle formulations is greatly influenced by their composition and structure. Lipid nanoparticles are generally composed of lipids, surfactants and co-surfactants. The lipid materials used in the production of lipid nanoparticles are usually solid at room temperature. Being well-tolerated in physiological conditions, lipid nanoparticles are typically biocompatible. Liquid lipids, or oils, are specifically used for production of NLCs. In most cases, lipid nanoparticles are produced as dispersions and surface-tailored with surfactants to improve dispersion stability. It was shown that NLCs reveal some advantages for drug therapy over conventional carriers, including increased solubility, the ability to enhance storage stability, improved permeability and bioavailability, reduced adverse effect, prolonged half-life, and tissue-targeted delivery.

Water-in-oil nanoemulsions loaded with Ardisia compressa K. bioactive compounds: evaluation of their physicochemical stability and functional activities

Journal of Dispersion Science and Technology, 2020

Ardisia compressa K. (ACK) fruits are a potential source of antioxidant compounds like phenolics and anthocyanins. ACK extracts made with aqueous ethanol (E75) yielded the highest total phenolic content (TPC) and antioxidant activity (AA) by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2 0azino-bis-3-ethylbenzothiazoline-6-sulphonic acid (ABTS) assays. Water-in-oil nanoemulsions (NE W/ O) were produced by spontaneous emulsification, in order to provide longer stability to functional activities from ACK extract, and formulated using ACK extract (10-30%wt.), rosemary essential oil (REO), and Tween 80:Span 80 (10-30% wt.). Resultant NE W/O were placed in a pseudo-ternary phase diagram and classified based on their visual performance, like phase separation, opacity, or translucent-stable systems. The latter displayed smaller hydrodynamic droplet sizes and better stability and were selected for physicochemical characterization. Physical stability through the hydrodynamic diameter, turbidity, and color attributes was monitored until 93 d at 25 C under light exposure (LE) and dark. A first-order model was used for the first two variables, with rate kinetic constants (k) from 10 À6 to 10 À8 s À1. Color index (CI) showed higher reduction when NE W/O were stored under LE, whereas total color difference (TCD) values were higher than 5.5, indicating marked differences in visual color compared to fresh NE W/O (t ¼0 d). Chemical stability from NE W/ O made with 30% w/w of ACK extract (NE30) displayed the best stability against pH changes, and TPC and AA during storage time, exhibiting also good antimicrobial susceptibility (AMS) against Gram-positive and Gram-negative bacteria with a synergistic effect of enhanced AMS than that observed in their respective individual components, even after storage time.