Encapsulation Of Epigallocatechin Gallate Research Articles

Nano-encapsulation of epigallocatechin gallate using starch nanoparticles: Characterization and insights on in vitro micellar cholesterol solubility.

The present work investigates the in vitro cholesterol reduction bioactivity of epigallocatechin gallate (EGCG) prior to and after nano-encapsulation using potato starch nanoparticle (SNP) as wall material. EGCG encapsulation in potato SNPs was achieved through a green inclusion complexation method. The encapsulated EGCG was characterized for its morphology, thermal, and crystalline properties using FESEM, DSC, XRD, and Fourier transform infrared (FTIR) studies. The bioactivity of EGCG to reduce gut cholesterol was studied using in vitro micellar cholesterol solubility study. The encapsulated EGCG exhibited enhanced thermal and crystalline properties. The FESEM results indicated successful nano-encapsulation of EGCG at 20-120nm diameter. The melting point enhanced from 225.7°C in EGCG to 282.9°C in encapsulated EGCG. The crystallinity also enhanced and could be observed through the increased intensity in the encapsulated EGCG. The FTIR results affirmed a shifting of peaks at 3675, 2927, 1730, and 1646cm-1, which corresponds to formation of new H bonds and confirms successful encapsulation of EGCG in SNPs. Further, EGCG had significantly reduced the cholesterol concentration by 91.63% as observed through the in vitro micellar inhibition study. The encapsulated EGCG was not able to reduce cholesterol as observed in the in vitro micellar cholesterol solubility study. This effect occurred due to the unavailability of EGCG after it formed a complex with SNPs. PRACTICAL APPLICATION: This study first investigates the utilization of newly synthesized potato starch nanoparticles as a coating material for nano-encapsulation of EGCG. The enhanced thermal and crystalline properties of these nanoparticles contribute to improved attributes in the nano-encapsulated EGCG. Such properties hold promise for applications in functional food matrices subjected to high-temperature processing, including functional cookies, bread, and cakes. Furthermore, this research explores the bioactivity of EGCG concerning its capacity to reduce gut cholesterol levels. It also examines the potential application of nano-encapsulated EGCG in lowering gut cholesterol through a micellar solubility study.

Encapsulation of EGCG by Zein-Gum Arabic Complex Nanoparticles and In Vitro Simulated Digestion of Complex Nanoparticles.

Epigallocatechin gallate (EGCG) has many excellent qualities such as its antitumor, antiradiation and anti-oxidation properties, but its application is limited because its oral bioavailability is low and stability is poor. In this paper, zein and gum arabic (GA) were used as wall materials to prepare Zein-GA complex nanoparticles for encapsulating and protecting the EGCG. The particle size of Zein-GA-EGCG complex nanoparticles ranged from 128.03–221.23 nm, and the EGCG encapsulation efficiency reached a maximum of 75.23% when the mass ratio of zein to GA was 1:1. The FTIR and XRD results illustrated that the components of the Zein-GA-EGCG complex nanoparticles interacted by electrostatic, hydrogen bonding, and hydrophobic interactions. The EGCG release rate of Zein-GA-EGCG nanoparticles (16.42%) was lower than that of Zein-EGCG (25.52%) during gastric digestion, and a large amount of EGCG was released during intestinal digestion, suggesting that the Zein-GA-EGCG nanoparticles could achieve the sustained release of EGCG during in vitro digestion. Hence, using Zein-GA complexes to encapsulate EGCG effectively increased the encapsulation efficiency of EGCG and realized the purpose of sustained release during simulated gastrointestinal digestion.

Nano-enabled delivery of EGCG ameliorates silica-induced pulmonary fibrosis in rats

Silicosis is the most serious occupational pulmonary fibrosis caused by excessive inhalation of silica particles, whereas viable therapeutic choices are constrained. Epigallocatechin gallate (EGCG) presents massive health benefits, but unfortunately with stability absence. Here, encapsulation of EGCG in poly(n-butylcyanoacrylate) nanoparticles (EGCG/PBCA-NPs) were fabricated by self-polymerization for gastrointestinal delivery in silicosis fibrosis treatment. The obtained nano-enabled delivery of EGCG was produced using a medical adhesive approved by FDA as carrier, and presented spherical particles with approximate diameter of 160 nm, a narrow PDI value of 0.2, Zeta potential value of 30 mV as well as a high EGCG incorporation (90 %) and loading efficiency (20 %). In evaluating the protect effects of nano-formulations, EGCG/PBCA-NPs shown excellent stability in gastric fluid with pH-triggered release in intestine and strong EGCG gastrointestinal retention against degradation. After daily gastrointestinal administration, EGCG/PBCA-NPs exhibited the superior anti-fibrosis efficacy in silicosis model rats induced by silica, involving lung index decline, hydroxyproline content decrease, histological improvement, collagen accumulation reduction and α-SMA down-regulation in comparison with naked EGCG. These results strongly demonstrated that PBCA-based NPs may be a promising nano-enabled delivery carrier for enhancing the gastrointestinal stability and anti-fibrotic effects of EGCG.

The potency of PLGA-Encapsulated Epigallocatechin Gallate (EGCG) as adjuvant therapy for chronic kidney disease

Chronic kidney disease (CKD) prevalence keeps increasing worldwide and being particular concern due to its morbidity and mortality. However, current CKD therapy are known to be economically costly and not necessarily provide better outcomes. Epigallocatechin gallate (EGCG) is one of the substances that widely studied as perspective therapeutic agents of CKD due to its anti-inflammatory, antioxidant, and enhancing mitochondrial function ability. However, the use of EGCG is limited to low bioavailability and poor pharmacokinetic profile. Encapsulation of EGCG with PLGA is expected to increase the efficacy of EGCG especially for its use as the kidney protective agent and optimize therapy of CKD. Thus, this study aims to analyze the potency of PLGA-encapsulated EGCG as the adjuvant therapy for CKD. This study was a narrative review summarizes studies related to current adjuvant therapy of CKD. EGCG has beneficial effects in reducing pro-inflammatory cytokines among chronic kidney disease. EGCG also can increase scavenging of free radicals to decrease reactive oxygen species. EGCG is known to enhance mitochondrial function and increase mitochondrial protection to prevent apoptosis in various kidney diseases. Combination of PLGA encapsulation with EGCG has a beneficial effect in improving the delivery, bioavailability, stability, and the pharmacokinetic profile of EGCG. PLGA-encapsulated EGCG also provides a better therapeutic effect on preventing and decreasing progression of kidney damage. Finally, this study concluded that combination of PLGA-encapsulated EGCG has a potency as the adjuvant therapy of CKD.

Vine Cane Compounds to Prevent Skin Cells Aging through Solid Lipid Nanoparticles.

The long lifespan of the world’s population has been raising interest in the research for new solutions to delay the aging process. With the aim of skin aging prevention, solid lipid nanoparticles (SLNs) were developed in this work for the encapsulation of three lipophilic natural compounds extracted from vine cane—epigallocatechin gallate (EGCG), resveratrol and myricetin. The developed loaded-SLNs proved to be stable, maintaining their adequate physicochemical characteristics for 30 days. In addition, the loaded-SLNs formulations exhibited high encapsulation efficiencies and loading capacities and high intracellular antioxidant activity. The mixture of EGCG-loaded SLNs with resveratrol-loaded SLNs proved to have the highest protection against induced oxidative stress. The in vitro cytotoxicity of the loaded SLNs was also evaluated, showing that the developed formulations are biocompatible for concentrations up to 50 µg/mL and could be safe for use in cosmetics. The encapsulation of EGCG, resveratrol and myricetin in SLNs seems to be a suitable strategy for the delivery of these antioxidants to the skin, improving their bioavailability.

Epigallocatechin gallate/L-ascorbic acid–loaded poly-γ-glutamate microneedles with antioxidant, anti-inflammatory, and immunomodulatory effects for the treatment of atopic dermatitis

Epigallocatechin gallate (EGCG) is a potential therapeutic agent for treatment of atopic dermatitis (AD) due to its antioxidant and anti-inflammatory activities. However, inherent instability of EGCG greatly limits its bioavailability and clinical efficacy. In this study, we developed a poly-γ-glutamate (γ-PGA)–based microneedle (MN) formulation capable of maintaining EGCG's stability and efficiently delivering EGCG into the skin to ameliorate AD symptoms. The γ-PGA MN can not only protect EGCG from oxidation, but also serve as an immunomodulator to downregulate T helper type 2 (Th2)-type immune responses. Encapsulation of EGCG into the γ-PGA MN and utilization of L-ascorbic acid (AA) as a stabilizer preserved 95% of its structural stability and retained 93% of its initial antioxidant activity after 4 weeks of storage. Once-weekly administration of EGCG/AA-loaded MNs to an Nc/Nga mouse model of AD for 4 weeks significantly ameliorated skin lesions and epidermal hyperplasia by reducing serum IgE (from 12156 ± 1344 to 5555 ± 1362 ng/mL) and histamine levels (from 81 ± 18 to 40 ± 5 pg/mL) and inhibiting IFN-γ (from 0.10 ± 0.01 to 0.01 pg/mg total protein) and Th2-type cytokine production, when compared to the AD (no treatment) group (p < 0.05). Notably, once-weekly MN therapy was at least as effective as the daily topical application of an EGCG + AA solution but markedly reduced the administration frequency and required dose. These results show that EGCG/AA-loaded γ-PGA MNs may be a convenient and promising therapeutic option for AD treatment. Statement of significanceThis study describes epigallocatechin gallate (EGCG)/L-ascorbic acid (AA)-loaded poly-γ-glutamate (γ-PGA) microneedles (MN) capable of providing antioxidant, anti-inflammatory, and immunomodulatory effects on inflamed skin for ameliorating atopic dermatitis (AD) symptoms in Nc/Nga mice. After skin insertion, the γ-PGA MN can be quickly dissolved in the skin and remain in the dermis for sustained release of encapsulated active ingredients for 6 days. We demonstrated that once-weekly MN therapy effectively alleviated skin lesions and modulated immune response to relieve Th2-polarized allergic response in mice. Once-weekly MN dosing regimen may provide patients with a more convenient, therapeutically equivalent option to daily topical dosing, and may increase compliance and long-term persistence with AD therapy.

Life under Extreme Conditions: Aeropyrum pernix and Pernisine

Life under Extreme Conditions: Aeropyrum pernix and Pernisine

Encapsulation of EGCG and esterified EGCG derivatives in double emulsions containing Whey Protein Isolate, Bacterial Cellulose and salt

Double (W1/O/W2) emulsions of 0.8 %wt PGPR-0.25 %wt BC-1 %wt WPI and NaCl (1.6–8 %wt) were characterized regarding their microstructure, droplet size, stability and viscosity. Droplet size increased with salt concentration. Salt addition at 4–5% wt limited the instability rate. Viscosity increased with NaCl concentration up to 4.8 %wt, above which it decreased. Eventually, the emulsion with 4.3 %wt salt was selected for catechin incorporation. In order to increase its antioxidant activity, Epigallocatechin Gallate (EGCG) was esterified with stearic acid. Esterification was partial and a mixture of esters was obtained. Both EGCG and its esterified derivatives were incorporated in the double emulsion. Storage reduced encapsulation. Encapsulation efficiency was reduced in the order “EGCG in the W1 phase” emulsion > “EGCG in the O phase” emulsion > “esterified EGCG in the W1 phase” emulsion. The presence of both catechins did not have a great effect on retarding emulsion oxidation.

Encapsulation of epigallocatechin gallate in zein/chitosan nanoparticles for controlled applications in food systems

The objective of this study was to prepare chitosan nanoparticles (CS NPs) coated with zein as a promising encapsulation and delivery system for epigallocatechin gallate (EGCG). The factors influencing the nanoparticle fabrication, including zein concentration, zein/chitosan weight ratio and EGCG encapsulation percentage, were systematically investigated. The physicochemical and structural analysis showed that the electrostatic interactions and hydrogen bonds were the major forces responsible for nanoparticles formation. The transmission electron microscopy study revealed the spherical nature with smooth surface of obtained nanoparticles. The release profile of EGCG showed a burst effect, followed by slow release. EGCG release was relatively higher from zein/chitosan nanoparticles (zein/CS NPs) with higher DPPH scavenging activity, than that of NPs without zein coating in 95% ethanol fatty simulant. These results indicated that controlled-release of EGCG from zein/CS NPs and its corresponding antioxidant activities in 95% ethanol fatty simulant may provide long-term protection against oxidation for fatty foods.

Therapeutic Potential of Epigallocatechin Gallate Nanodelivery Systems.

Nowadays, the society is facing a large health problem with the rising of new diseases, including cancer, heart diseases, diabetes, neurodegenerative diseases, and obesity. Thus, it is important to invest in substances that enhance the health of the population. In this context, epigallocatechin gallate (EGCG) is a flavonoid found in many plants, especially in tea. Several studies support the notion that EGCG has several benefits in fighting cancer, heart diseases, diabetes, and obesity, among others. Nevertheless, the poor intestinal absorbance and instability of EGCG constitute the main drawback to use this molecule in prevention and therapy. The encapsulation of EGCG in nanocarriers leads to its enhanced stability and higher therapeutic effects. A comprehensive review of studies currently available on the encapsulation of EGCG by means of nanocarriers will be addressed.

Zein-based colloidal particles for encapsulation and delivery of epigallocatechin gallate

Zein, a water insoluble plant protein from a renewable natural source, has been identified as a highly promising material for the production of protein-based colloidal particles for the encapsulation of lipophilic compounds. However, the encapsulation of hydrophilic, water-soluble, bioactive molecules within zein colloidal particles is still unexplored. We show that the encapsulation of epigallocatechin gallate (EGCG) is strongly limited by the weak physical interactions occurring with the zein matrix during the precipitation phase. We demonstrate that the use of sodium caseinate, as a colloidal stabilizer to coat the zein particles, enables the modulation of the encapsulation efficiency and functionality of zein colloidal particles for EGCG delivery. In particular, coated zein particles exhibit a larger size, opposite surface charge and significantly different antioxidant activity, owing to the localization of EGCG affected by the different extent of interaction of EGCG with zein and sodium caseinate. Remarkably, particle formulation also tunes the release rate of EGCG during in vitro digestion and modulates the rate of fat digestion, through the combination of the Pickering emulsion stabilization effect and EGCG interaction with lipase enzyme. Zein-based colloidal particles constitute hence remarkable systems for the tunable and multi-functional delivery of EGCG.

Stability and bioaccessibility of EGCG within edible micro-hydrogels. Chitosan vs. gelatin, a comparative study

Micro-hydrogels are very promising systems for the protection and controlled delivery of sensitive bioactives, but limited knowledge exists regarding the impact of this encapsulation on their bioaccessibility. In this work, two different hydrogel-forming biopolymers (gelatin and chitosan) were compared as wall materials for the microencapsulation of a model flavonoid, (−)-epigallocatechin gallate (EGCG). Results showed that gelatin was more adequate as wall material for the encapsulation of EGCG than chitosan, achieving higher encapsulation efficiencies (95% ± 6%), being more effective in delaying EGCG release and degradation in aqueous solution and exhibiting a 7 times higher bioaccessibility of the bioactive compound (in terms of antioxidant activity) after in-vitro gastrointestinal digestion. A very low bioaccessibility of EGCG in chitosan was observed, due to the neutralization of the carbohydrate in the basic simulating salivary conditions, thus precluding subsequent flavonoid release. Moreover, gelatin micro-hydrogels also hindered dimer formation during in-vitro digestion, thus suggesting greater bioavailability when compared with free EGCG.

Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation

The encapsulation of epigallocatechin gallate (EGCG) in lipid nanoparticles (LNs) could be a suitable approach to avoid drug oxidation and epimerization, which are common processes that lead to low bioavailability of the drug limiting its therapeutic efficacy. The human health benefits of EGCG gained much interest in the pharmaceutical field, and so far there are no studies reporting its encapsulation in LNs. The purpose of this study has been the development of an innovative system for the ocular delivery of EGCG using LNs as carrier for the future treatment of several diseases, such as dry eye, age-related macular degeneration (AMD), glaucoma, diabetic retinopathy and macular oedema. LNs dispersions have been produced by multiple emulsion technique and previously optimized by a factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, two distinct cationic lipids were used, namely, cetyltrimethylammonium bromide (CTAB) and dimethyldioctadecylammonium bromide (DDAB). EGCG has been successfully loaded in the LNs dispersions and the nanoparticles analysis over 30 days of storage time predicted a good physicochemical stability. The particles were found to be in the nanometer range (<300nm) and all the evaluated parameters, namely pH, osmolarity and viscosity, were compatible to the ocular administration. The evaluation of the cationic lipid used was compared regarding physical and chemical parameters, lipid crystallization and polymorphism, and stability of dispersion during storage. The results show that different lipids lead to different characteristics mainly associated with the acyl chain composition, i.e. double lipid shows to have influence in the crystallization and stability. Despite the recorded differences between DTAB and DDAB, both cationic LNs seem to fit the parameters for ocular drug delivery.

(−)-Epigallocatechin gallate/gelatin layer-by-layer assembled films and microcapsules

A new type of protein/polyphenol microcapsules on the basis of naturally occurring polyphenol (−)-epigallocatechin gallate (EGCG) and gelatin, type A, was obtained using the layer-by-layer (LbL) assembly method. The microcapsules show a more pronounced dependence of permeability on molecular weight of permeating substances than commonly used polyallylamine/polystyrene sulfonate capsules. The regularities of EGCG adsorption in alternation with type A and B gelatins have been investigated using quartz crystal microbalance and electrophoretic mobility measurements on microparticles and found to be dependent on gelatin properties. EGCG in the LbL assemblies retains its antioxidant activity. The kinetics of the reaction of 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) cation-radicals with films consisting of 1–10 gelatin/EGCG bilayers is affected by film structure. The EGCG content in the protein/polyphenol film material is as high as 30% w/w. Encapsulation of EGCG via its alternated adsorption with gelatins can be a perspective way to new formulations containing the polyphenol for drug delivery applications.