Delivery Of Polyphenols Research Articles

Layer by layer self-assembled hyaluronic acid nanoarmor for the treatment of ulcerative colitis

Natural compound-based treatments provide innovative ways for ulcerative colitis therapy. However, poor targeting and rapid degradation curtail its application, which needs to be addressed. Inspired by biomacromolecule-based materials, we have developed an orally administrated nanoparticle (GBP@HA NPs) using bovine serum albumin as a carrier for polyphenol delivery. The system synergizes galactosylated bovine serum albumin with two polyphenols, epigallocatechin gallate and tannic acid, which is then encased in “nanoarmor” of ε-Polylysine and hyaluronic acid to boost its stability and targeting. Remarkably, the nanoarmor demonstrated profound therapeutic effects in both acute and chronic mouse models of ulcerative colitis, mitigating disease symptoms via multiple mechanisms, regulating inflammation related factors and exerting a modulatory impact on gut microbiota. Further mechanistic investigations indicate that GBP@HA NPs may act through several pathways, including modulation of Keap1-Nrf2 and NF-κB signaling, as well as Caspase-1-dependent pyroptosis. Consequently, this novel armored nanotherapy promotes the way for enhanced polyphenol utilization in ulcerative colitis treatment research.

Alginate edible films as delivery systems for green tea polyphenols

This study investigated the potential of alginate edible films to act as vehicles for the delivery of polyphenols to the intestinal tract. Sodium alginate (0.5–2% w/v) and green tea extract (GTE, 25–50% w/w) were combined to form films with different microstructural properties via the casting method, where their physical, mechanical and barrier properties were analysed. Release studies into a 50% ethanol (v/v) food simulant and under simulated in vitro digestion were also conducted, and the resulting kinetics of polyphenols release was investigated. Composite alginate films with 25% w/w GTE (E∼2500 MPa; EAB∼14%; k∼0.04) showed significantly enhanced mechanical properties and slower rates of polyphenol release than samples with 50% w/w GTE (E∼6000 MPa; EAB∼6%; k∼0.18). Polyphenols entrapped within the 2% alginate – GTE films were successfully released during digestion (∼54%), demonstrating their bioaccessibility and availability for absorption by the gastrointestinal tract. The bioaccessibility of green tea polyphenols was significantly enhanced by films with good sustained-release effect (2% alginate – GTE, C/C0 = 54.41 ± 0.75%) respect to the free GTE (C/C0 = 33.73 ± 6.57%). These findings highlight the versatility of bioactive alginate edible films and create a blueprint for the design of sustainable active packaging alternatives with dual functionality.

Oral fast dissolving films made with alginate and whey protein for resveratrol delivery

Resveratrol is a natural polyphenol with low bioavailability because of poor hydro-solubility and extensive first-pass effect. The delivery to oral mucosa via oral fast dissolving films (OFDFs) is a useful administration route to bypass the first-pass metabolism through direct adsorption into the systemic circulation. In this study, the OFDFs was fabricated with loading of excessive and soluble resveratrol in various ratios of whey protein isolate (WPI) and alginate. The solubility of resveratrol was improved in the presence of WPI and/or alginate, which was further affected by glycerol. The OFDFs were characterized in term of thickness, disintegration time, intermolecular interaction, structure, mechanical properties and thermal degradation. At a glycerol/biopolymer ratio of 1:2 and the WPI/alginate ratios between 5:1 and 1:1, the OFDFs disintegrated within 30 s and completely dissolved within 60 s, containing 30–50 μg/cm2 dissolved resveratrol in water. The permeation percentage of 89% was the most at the WPI/alginate ratio of 3:1. Oral mucosa permeation of resveratrol in OFDFs was significantly greater than that in the corresponding film solution. The films exhibited fast disintegration and promotion of resveratrol permeation. These results demonstrate that WPI and alginate were effective in the preparation of OFDFs for enhancing the permeability of resveratrol. It is thus suggested that biopolymer-based OFDFs are potential carriers for oral delivery of polyphenols.

Quercetin-Loaded Nanocarriers as Effective Inhibitors for Copper Metal Ion-Induced γD-Crystallin Aggregation.

Cataract is one of the leading causes of blindness worldwide. Till date, the only solution for cataracts is surgery, which is a resource-intensive solution. A much simpler solution is to find a potential drug that could inhibit aggregation. It is well established that nonamyloid aggregates of eye lens protein result in cataract. γD-Crystallin, a thermodynamically stable protein, is one of the most abundant proteins in the core of the eye lens and is found to aggregate under stress conditions, leading to the cataract. It has also been found that in cataractous lens, the concentration of metals like copper is elevated significantly as compared to healthy eye lens, suggesting their role in inducing aggregation. In our present study, aggregation of γD-Crystallin was carried out in the presence of Cu (II). Using techniques like turbidity assay, CD spectroscopy, ANS binding assay, and microscopic studies like TEM, it could be confirmed that protein aggregates in the presence of Cu (II) and the nature of aggregates is amorphous. Various polyphenols were tested to suppress aggregation of the protein. Quercetin was observed to be the most efficient. To overcome the problems associated with the delivery of polyphenols, such as solubility and bioavailability, quercetin was encapsulated in two types of nanocarriers. Their characterization was done using TEM, DLS, and other techniques. The potency of quercetin-loaded CS-TPP/CS-PLGA NPs as inhibitors of γD-Crystallin aggregation was confirmed by various experiments.

Modulation of long noncoding RNAs by polyphenols as a novel potential therapeutic approach in lung cancer: A comprehensive review.

Lung cancer stands as a formidable global health challenge, necessitating innovative therapeutic strategies. Polyphenols, bioactive compounds synthesized by plants, have garnered attention for their diverse health benefits, particularly in combating various cancers, including lung cancer. The advent of whole-genome and transcriptome sequencing technologies has illuminated the pivotal roles of long noncoding RNAs (lncRNAs), operating at epigenetic, transcriptional, and posttranscriptional levels, in cancer progression. This review comprehensively explores the impact of polyphenols on both oncogenic and tumor-suppressive lncRNAs in lung cancer, elucidating on their intricate regulatory mechanisms. The comprehensive examination extends to the potential synergies when combining polyphenols with conventional treatments like chemotherapy, radiation, and immunotherapy. Recognizing the heterogeneity of lung cancer subtypes, the review emphasizes the need for the integration of nanotechnology for optimized polyphenol delivery and personalized therapeutic approaches. In conclusion, we collect the latest research, offering a holistic overview of the evolving landscape of polyphenol-mediated modulation of lncRNAs in lung cancer therapy. The integration of polyphenols and lncRNAs into multidimensional treatment strategies holds promise for enhancing therapeutic efficacy and navigating the challenges associated with lung cancer treatment.

Preparation of a curcumin oil bodies delivery system based on pH-Shift treatment: Physicochemical properties, protein structure, and digestive properties

Curcumin (Cur) was encapsulated in oil bodies (OBs) using pH-shift treatment. The physicochemical properties, surface protein structure, stability, and in vitro digestion of the prepared composite emulsion (COB) were characterized. The results showed a fading of Cur crystallization peak in COB. Besides, the highest encapsulation rate, largest particle size and zeta potential were observed at pH 0.5. Compared to OBs, the hydrophilic groups of COB surface proteins were unfolded and the central hydrophobic region remained relatively stable, with reduced COB storage stability and good oxidative stability. In vitro simulated digestion revealed that Cur was released in a sustained manner. The highest bioaccessibility (57.5%) and stability (67.3%) of COB were observed at pH 0.5. The present study suggested that pH-shift treatment is a viable method for the preparation of COB carriers. This information may provide new ideas for the preparation of lipophilic polyphenol delivery systems such as Cur, which can contribute to the application of OBs in a variety of food processing applications, including plant-based milk, fortified foods, etc.

Novel, engineered fusogenic liposome-based anti-oxidant delivery system improves the blood-brain barrier integrity in aging

Vascular dysfunction plays a pivotal role in age-related cognitive decline and neurodegeneration. The aging process often leads to a loss of integrity in the blood-brain barrier (BBB), initiating neuroinflammation and contributing to a decline in cognitive function. In previous research, we demonstrated the potential of resveratrol (RSV), a natural polyphenol, to target cerebromicrovascular endothelial cells (CMVECs), effectively countering age-related oxidative stress and improving vascular function, both in vitro and in vivo. However, the limited bioavailability of resveratrol raised questions about its effectiveness concerning the BBB and neuroinflammation. Our study aimed to address this challenge by introducing a novel drug delivery system designed to enhance the effciency of polyphenol delivery. This innovative approach involved the use of fusogenic liposomes (FL) integrated with a bioengineered protein corona (PC) featuring specific apolipoprotein E (ApoE). Our central hypothesis posited that PC formation could be harnessed to directly target CMVECs and enhance liposomal uptake, with the ultimate objective of effectively delivering RSV to the brain's microvessels in aging subjects (ApoE-FL-RSV). Our investigation encompassed the characterization of ApoE-FL uptake by CMVECs, along with an analysis of its biodistribution and pharmacokinetics in vivo. Remarkably, our findings revealed a significant increase in ApoE-FL-RSV accumulation within CMVECs in vivo, compared to control FL uptake. We employed advanced in vivo multiphoton imaging to longitudinally monitor the effects of ApoE-FL-RSV on the BBB, which demonstrated a significant rejuvenation of the endothelial barrier function in aged mice treated with ApoE-FL-RSV. In light of these results, we concluded that the fusogenic liposomal delivery system holds promise as a viable pharmacological intervention for addressing age-related vascular cognitive impairment. AHA834339, RF1AG072295, R01AG055395, R01AG068295; R01AG070915, K01AG073614, R01NS100782, R01CA255840, and Presbyterian Health Foundation. This is the full abstract presented at the American Physiology Summit 2024 meeting and is only available in HTML format. There are no additional versions or additional content available for this abstract. Physiology was not involved in the peer review process.

Supramolecular assembly of dual crosslinked nanocomposite polysaccharides hydrogel: Integration of injectable, self-healing, and pH-responsive platform for sustained delivery of polyphenols

This study introduces an innovative approach in the field of biomaterials through the development of a multifunctional, printable scaffold designed for the advanced delivery of polyphenols. Addressing challenges of burst-release, poor compounds solubility and bioavailability, we engineered a supramolecular-assembled dual crosslinked hydrogel combining fucoidan (F) and chitosan (CS) encapsulating nanoliposomes. The novel integration of dibenzaldehyde-terminated PEG (DB) within the hydrogel, created a synergistic crosslinking through the formation of the covalent Schiff base bonds and physical interactions which enhanced the hydrogel's overall characteristics. Tailoring F content (DBCS-F), allowed the crosslinking density modulation, yielding a robust gel network structure with enhanced mechanical properties, evidenced by a remarkable compressive stress resistance of 1.73 MPa at 60% strain, coupled with high compressive resilience (79.31% stress recovery after 6 cycles), surpassing single crosslinked hydrogel (DBCS). The rheological analysis further confirmed the hydrogel's improved viscoelasticity, stable network structure, and shear-thinning behavior, affirming its excellent injectability and suitability for 3D printing applications. Most notably, the incorporation of catechin/juglone-loaded nanoliposomes contributed to a pH-responsive sustained release of polyphenols in simulated gastrointestinal conditions. The developed dual crosslinked hydrogel, integrating injectability, self-healing, and pH-responsiveness presents a significant advancement in biomaterials and holds a promising approach for the fabrication of personalized 3D printed scaffolds aimed for sustained and targeted polyphenols release.

Encapsulated phenolic compounds: clinical efficacy of a novel delivery method

AbstractEncapsulation is a drug or food ingredient loaded-delivery system that entraps active components, protecting them from decomposition/degradation throughout the processing and storage stages and facilitates their delivery to the target tissue/organ, improving their bioactivities. The application of this technology is expanding gradually from pharmaceuticals to the food industry, since dietary bioactive ingredients, including polyphenols, are susceptible to environmental and/or gastrointestinal conditions. Polyphenols are the largest group of plants' secondary metabolites, with a wide range of biological effects. Literature data have indicated their potential in the prevention of several disorders and pathologies, ranging from simpler allergic conditions to more complex metabolic syndrome and cardiovascular and neurodegenerative diseases. Despite the promising health effects in preclinical studies, the clinical use of dietary polyphenols is still very limited due to their low bioaccessibility and/or bioavailability. Encapsulation can be successfully employed in the development of polyphenol-based functional foods, which may improve their bioaccessibility and/or bioavailability. Moreover, encapsulation can also aid in the targeted delivery of polyphenols and may prevent any possible adverse events. For the encapsulation of bioactive ingredients, several techniques are applied such as emulsion phase separation, emulsification/internal gelation, film formation, spray drying, spray-bed-drying, fluid-bed coating, spray-chilling, spray-cooling, and melt injection. The present review aims to throw light on the existing literature highlighting the possibility and clinical benefits of encapsulated polyphenols in health and disease. However, the clinical data is still very scarce and randomized clinical trials are needed before any conclusion is drawn. Graphical abstract

Polyphenol-based polymer nanoparticles for inhibiting amyloid protein aggregation: recent advances and perspectives.

Polyphenols are a group of naturally occurring compounds that possess a range of biological properties capable of potentially mitigating or preventing the progression of age-related cognitive decline and Alzheimer's disease (AD). AD is a chronic neurodegenerative disease known as one of the fast-growing diseases, especially in the elderly population. Moreover, as the primary etiology of dementia, it poses challenges for both familial and societal structures, while also imposing a significant economic strain. There is currently no pharmacological intervention that has demonstrated efficacy in treating AD. While polyphenols have exhibited potential in inhibiting the pathological hallmarks of AD, their limited bioavailability poses a significant challenge in their therapeutic application. Furthermore, in order to address the therapeutic constraints, several polymer nanoparticles are being explored as improved therapeutic delivery systems to optimize the pharmacokinetic characteristics of polyphenols. Polymer nanoparticles have demonstrated advantageous characteristics in facilitating the delivery of polyphenols across the blood-brain barrier, resulting in their efficient distribution within the brain. This review focuses on amyloid-related diseases and the role of polyphenols in them, in addition to discussing the anti-amyloid effects and applications of polyphenol-based polymer nanoparticles.

Metal-Infused Polyphenol-enriched Phyto-fabricated Nanoparticles: an In-depth Review of their Potent Prebiotic Properties

In light of its potential health benefits, including as improved gut health and management of the gut microbiota, herbal extracts have witnessed a major increase in demand as prebiotics in recent years. Many studies have demonstrated that polyphenolrich herbal extracts can work as prebiotics by encouraging the growth of beneficial gut flora. Unfortunately, the limited solubility and stability of these herbal extracts, as well as their susceptibility to breakdown in the gastrointestinal system, can limited their bioavailability and efficiency. To address these limitations, the integration of metal nanoparticles has emerged as a promising strategy for the efficient delivery of herbal extracts, affording heightened bioavailability and precise targeting of the gut microbiota. In this paper, we present current breakthrough in metal infused nanoparticle-based assessment of herbal extracts as efficient prebiotics, with an emphasis on formulation, characterization, and biological activity. The integration of metal nanoparticles into polyphenol-rich herbal extracts represents a cutting-edge approach to enhancing the prebiotic properties of these compounds. Metal-infused polyphenol-enriched phyto-fabricated nanoparticles hold great promise for improving gut health and modulating the gut microbiota, offering innovative solutions to address the limitations associated with traditional polyphenol delivery. Furthermore, extracts of polyphenol-rich medicinal herbs such as rosehip flower, hibiscus flower, mango bark, bamboo stem, green tea, pomegranate, and dhataki flower have been investigated to assess the viability of employing these phyto generated metal infused nanoparticles as a potential prebiotic

Electrospray alginate-Konjac glucomannan microgel as efficient colon-targeted delivery vehicle for quercetin

Colon targeted delivery of polyphenols is a promising approach in reducing the risks of colonic diseases. In this study, alginate microgels were fabricated by an electrospray method. Native Konjac glucomannan (KGM) or degraded KGM (DKGM: hydrothermal decomposition for 20 min (KMG20) or 60 min (KMG60)) were incorporated as filling material, while chitosan was added as a protective coating after microgel formation. Quercetin was encapsulated at two formulation levels to study the properties of the loaded microgels. During electrospraying, DKGM, which had lower viscosities, produced microgels with smaller average particle sizes compared to KGM, and both KGM and DKGM microgels had narrower size distribution compared to alginate-only microgels. All microgels achieved encapsulation efficient (EE) up to 100% at low quercetin formulation level (0.2% w/w), and > 75% EE at high quercetin formulation level (0.4% w/w). Loading at 125.2–191.9 mg/g freeze-dried microgel was achieved with 0.4% w/w quercetin level. FTIR confirmed the successful encapsulation of KGM/KGM20/KGM60 and quercetin into the gel matrix. Zeta potential analysis indicated that KGM/KGM20/KGM60 affected the chitosan coating and particle swelling ratio depending on quercetin loading levels. During in vitro sequential oral-gastric-intestinal digestion, KGM/DKGM retarded release compared to alginate-only microgels at low loading, but KGM and KGM20 increased release significantly at high loading. Only KGM60 maintained low release (<10%) regardless of the quercetin loading, making it a promising filling material among the tested formulations for colon-targeted delivery of quercetin.

Stability of a novel glycosylated peanut protein isolate delivery system loaded with gallic acid

To overcome the shortcomings of gallic acid (GA) application, a novel glycosylated PPI delivery system was prepared for the first time in this study using the interaction between peanut protein isolate (PPI) and GA. The effects of glycosylation on the structural and functional properties of PPI and the functional properties of nanoparticles were investigated. The optimal nanoparticles were prepared at a mass ratio 1:3 of glycosylated PPI to GA with a particle size of 338.351 ± 18.823 nm and a PDI of 0.222 ± 0.039. Hydrophobic interactions were the main force maintaining the nanoparticle structure. The nanoparticles remained stable when exposed to different environmental factors. In addition, the DPPH and ABTS radical scavenging activities of nanoparticle-embedded GA were 35.94 ± 3.24 % and 62.59 ± 5.07 % after 108 h, which were significantly higher than those of the free GA group (P < 0.05). This study is important for developing GA and hydrophilic polyphenol delivery systems.

Release study of polyphenols from polyvinyl alcohol/chitosan active films supplemented with Sonneratia ovata extract and Piper betel (L.) essential oil

In present work, the delivery kinetics of polyphenols from active films based on polyvinyl alcohol (PVOH) and chitosan (CS) enriched with Sonneratia ovata extract (SOE) and Piper betel (L.) essential oil (PBLO) in different food simulants were studied. SOE-added PVOH/CS films showed the slowest delivery rate and released amount of polyphenols. Co-supplementation with PBLO provided SOE-added PVOH/CS film with outstanding antioxidant property and thermo-stability. However, the swell and solubility properties of as-prepared films increased as PBLO concentration surged likely lying on the existence of oil droplets at internal and external surface, which affect to polyphenols delivery from active films in food simulants. The release rate of polyphenols of SOE and PBLO from as-prepared active films to several food simulants was evaluated by Peleg, Korsmeyer-Peppas, Kopcha model, and Fick's second law. The resulting parameters suggested that the release process was occurred due to the diffusion mechanism.

Colon-Targeted Release of Turmeric Nonextractable Polyphenols and Their Anticolitis Potential via Gut Microbiota-Dependent Alleviation on Intestinal Barrier Dysfunction in Mice.

Solid evidence has emerged supporting the role of nonextractable polyphenols (NEPs) and dietary fibers (DFs) as gut microbiota modulators. This study aims to elucidate gut microbiota-dependent release of turmeric NEPs and examine the possible anti-inflammatory mechanism in the dextran sulfate sodium-induced ulcerative colitis (UC) model. 1.5% DSS drinking water-induced C57BL/6J mice were fed a standard rodent chow supplemented with or without 8% extractable polyphenols (EPs), NEPs, or DFs for 37 days. The bound curcumin, demethoxycurcumin, and bisdemethoxycurcumin in NEPs were released up to 181.5 ± 10.6, 65.2 ± 6.0, and 69.5 ± 7.6 μg/mL by in vitro gut microbiota-simulated fermentation and released into the colon of NEP-supplemented mice by 5.7-, 11.0-, and 7.8-fold higher than pseudo germ-free mice, respectively (p < 0.05). NEPs also enhanced the colonic microbiota-dependent production of short-chain fatty acids in vitro and in vivo (p < 0.05). Interestingly, NEP feeding significantly improved the DSS-caused gut microbiota disorder, epithelial barrier damage, and inflammation of UC mice better than EPs or DFs (p < 0.05). Meanwhile, the pseudo germ-free mice supplemented with NEPs failed to ameliorate UC symptoms. These findings manifest that turmeric NEPs as macromolecular carriers exert the target delivery of polyphenols into the colon for regulating gut microbiota to restore the impaired gut barrier function for alleviation of inflammation.

Simulated Gastrointestinal Digestion of Chestnut (Castanea sativa Mill.) Shell Extract Prepared by Subcritical Water Extraction: Bioaccessibility, Bioactivity, and Intestinal Permeability by In Vitro Assays.

Chestnut shells (CSs) are an appealing source of bioactive molecules, and constitute a popular research topic. This study explores the effects of in vitro gastrointestinal digestion and intestinal permeability on the bioaccessibility and bioactivity of polyphenols from CS extract prepared by subcritical water extraction (SWE). The results unveiled higher phenolic concentrations retained after gastric and intestinal digestion. The bioaccessibility and antioxidant/antiradical properties were enhanced in the following order: oral < gastric ≤ intestinal digests, attaining 40% of the maximum bioaccessibility. Ellagic acid was the main polyphenol in the digested and undigested extract, while pyrogallol-protocatechuic acid derivative was only quantified in the digests. The CS extract revealed potential mild hypoglycemic (<25%) and neuroprotective (<75%) properties before and after in vitro digestion, along with upmodulating the antioxidant enzymes' activities and downregulating the lipid peroxidation. The intestinal permeation of ellagic acid achieved 22.89% after 240 min. This study highlighted the efficacy of the CS extract on the delivery of polyphenols, sustaining its promising use as nutraceutical ingredient.

Toward function starch nanogels by self-assembly of polysaccharide and protein: From synthesis to potential for polyphenol delivery

Nanogels formed by self-assembly of natural proteins and polysaccharides have attracted great interest as potential carriers of bioactive molecules. Herein, we reported that carboxymethyl starch-lysozyme nanogels (CMS-Ly NGs) were prepared using carboxymethyl starch and lysozyme by green and facile electrostatic self-assembly, and the nanogels served as epigallocatechin gallate (EGCG) delivery systems. The dimensions and structure of the prepared starch-based nanogels (i.e., CMS-Ly NGs) were characterized by dynamic light scattering (DLS), ζ-potential, Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD) and thermal gravimetric analyzer (TGA). FT-IR and 1H NMR spectra together confirmed the formation of CMS; FT-IR spectra confirmed the formation of CMS-Ly NGs; XRD spectra confirmed the disruption of the crystal structure of lysozyme after electrostatic self-assembly with CMS, and further confirmed the formation of nanogels. TGA demonstrated the thermal stability of nanogels. More importantly, the nanogels showed a high EGCG encapsulation rate of 80.0 ± 1.4 %. The CMS-Ly NGs encapsulated with EGCG exhibited regular spherical structure and stable particle size. Under the simulated gastrointestinal environmental conditions, CMS-Ly NGs encapsulated with EGCG showed the controlled release potential, which increased its utilization. Additionally, anthocyanins can also be encapsulated in CMS-Ly NGs and showed slow-release properties during gastrointestinal digestion in the same way. Cytotoxicity assay also demonstrated good biocompatibility between CMS-Ly NGs and CMS-Ly NGs encapsulated with EGCG. The findings of this research suggested the potential application of protein and polysaccharides-based nanogels in the delivery system of bioactive compounds.

Polyphenol-based Nanosystems for Next-generation Cancer Therapy: Multifunctionality, Design, and Challenges.

With the continuous updating of cancer treatment methods and the rapid development of precision medicine in recent years, there are higher demands for advanced and versatile drug delivery systems. Scientists are committed to create greener and more effective nanomedicines where the carrier is no longer limited to a single function of drug delivery. Polyphenols, which can act as both active ingredients and fundamental building blocks, are being explored as potential multifunctional carriers that are efficient and safe for design purposes. Due to their intrinsic anticancer activity, phenolic compounds have shown surprising expressiveness in ablation of tumor cells, overcoming cancer multidrug resistance, and enhancing immunotherapeutic efficacy. This review provides an overview of recent advances in the design, synthesis, and application of versatile polyphenol-based nanosystems for cancer therapy in various modes. Moreover, the merits of polyphenols and the challenges for their clinical translation are also discussed, and it is pointed out that the novel polyphenol delivery system requires further optimization and validation. This article is protected by copyright. All rights reserved.

Development and Characterization of Nanovesicles Containing Phenolic Compounds of &lt;i&gt;Carissa spinarum&lt;/i&gt;: Encapsulation, Release Kinetics, Antimicrobial Activity and Mathematical Modeling

The aim of this study was to develop and characterize a delivery system for polyphenols from an extract of Carissa spinarum leaves, based on liposomes. Liposomes loaded with Carissa spinarum polyphenols (nanoliposomal CsP) were prepared by ethanol-solvent injection method and characterized in terms of zeta potential, size, and polydipersity index by using Zeta sizer and Fourier Transform Infrared spectrum analysis. Total Phenolic content was measured by using Folin-Ciocalteu method and entrapment efficiency was evaluated. The release behavior was conducted in Phosphate Buffer Saline (PBS) solution at pH, 7.4 and Kinetic model fitted to evaluate mechanism of release. Disc diffusion sensitivity test was used to evaluate antimicrobial activity of free extract and nanoliposomal CsP. The mean diameter of nanoliposomal CsP was 181 ± 1.02 nm and had 0.345 ± 0.014 polydipersity index. Zeta potential value for nanoliposomal CsP was-45.6 ± 8.84 mV. Entrapment efficiency under the optimum conditions was 66.11 ± 1.11%. and the nanoliposomal CsP was stable over 30 days. The antibacterial activity of nanoliposomal CsP exhibited inhibition zone diameter of 14.33 ± 1.53 mm and 12.00 ± 1.23 mm against S. aureus and E. coli respectively The results reveal the Carrisa spinarum liposome can be applied as potential carrier for delivery of polyphenols to improves therapeutic action against bacterial strain.

Biosorption of bioactive compounds in bacterial nanocellulose: Mechanisms and physical-chemical properties

Bacterial cellulose (BC) is a biomaterial produced by Gluconacetobacter xylinus, with wide applicability in different areas, such as biomedical, pharmaceutical, and food. BC production is usually carried out in a medium containing phenolic compounds (PC), such as teas, however, the purification process leads to the loss of such bioactive. Thus, the innovation of this research consists of the reincorporation of PC after the purification of the BC matrices through the biosorption process. In this context, the effects of the biosorption process in BC were evaluated to maximize the incorporation of phenolic compounds from a ternary mixture of hibiscus (Hibiscus sabdariffa), white tea (Camellia sinensis), and grape pomace (Vitis labrusca). The biosorbed membrane (BC-Bio) showed a great concentration of total phenolic compounds (TPC = 64.89 mg L−1) and high antioxidant capacity through different assays (FRAP: 130.7 mg L−1, DPPH: 83.4 mg L−1, ABTS: 158.6 mg L−1, TBARS: 234.2 mg L−1). The physical tests also indicated that the biosorbed membrane presented high water absorption capacity, thermal stability, low permeability to water vapor and improved mechanical properties compared to BC-control. These results indicated that the biosorption of phenolic compounds in BC efficiently increases bioactive content and improves physical membrane characteristics. Also, PC release in a buffered solution suggests that BC-Bio can be used as a polyphenol delivery system. Therefore, BC-Bio is a polymer with wide application in different industrial segments.