Encapsulation Of Resveratrol Research Articles

Soy lipophilic protein self-assembled by pH-shift combined with heat treatment: Structure, hydrophobic resveratrol encapsulation, emulsification, and digestion

This study evaluates the effect of pH (pH 3 and 11) and heat treatment (60 °C) in modifying the soybean lipophilic protein (LP) for the development of an encapsulation system to co-deliver resveratrol (Res) and vitamin D3. The structural and functional properties of LP after the modification will change to varying degrees. Meanwhile, Res was loaded into the hydrophobic core of LP, and the resulting Res-loaded structures have a uniform particle size distribution and a high encapsulation efficiency (78%). When the amount of Res encapsulation increases, the emulsification and oxidation resistance of the Pickering emulsion increased; the interfacial tension and interfacial protein adsorption increased to 11.21 mN/m and 97.34%, respectively. During simulated gastrointestinal digestion, the Pickering emulsion prepared with LP-Res nanoparticles at pH 11, 60 °C (pH 11, 60 °C-LP-Res) effectively protected Res and vitamin D3 from degradation or precipitation, indicating a significant increase in bioavailability.

Extraction of protein from churpi of yak milk origin: Size reduction, nutraceutical potential and as a wall material for resveratrol

Resveratrol is a known anti-oxidant and anti-cancer bioactive. The low bioavailability and poor water solubility of resveratrol is a major barrier that restricts its usage in food applications. To overcome these problems, the study presents micro and nano encapsulation of resveratrol in casein micelles extracted from Himalayan cheese (Churpi). Resveratrol loaded casein microparticles (CS-rm) were obtained using emulsion-freeze drying. Whereas, resveratrol loaded casein nanoparticles (CS-rn) were obtained using ultrasonication. Both were characterized using dynamic light scattering (DLS), scanning electron microscopy (SEM) and attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR). DLS revealed hydrodynamic diameter of 71.24 μm and 387.023 nm and zeta potential of −22.62 and −28.08 mV for CS-rm and CS-rn. FTIR confirmed the characteristic peaks of resveratrol at 965.4, 1380.86, 1586.66 and 1607 cm−1 confirmed successful micro and nanoencapsulation. CS-rm displayed high encapsulation efficiency (52.32%) and swelling power (77.90 at pH 3 and 68.65 at pH 7.5) than CS-rn. Both micro and nanoencapsulation protected resveratrol in gastric conditions, however, CS-rn showed high release of resveratrol then CS-rm in simulated intestinal conditions. The anti-oxidant and anti-cancer activity of resveratrol under simulated gastric and intestinal conditions (SGID) was significantly higher (p ≤ 0.05) for CS-rn, showing that nanoencapsulation improved release and nutraceutical profile of resveratrol. Resveratrol loaded nano and micro casein particles can be used a source of fortified protein supplement in growing food and nutraceutical industry.

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.

Resveratrol Encapsulation and Release from Pristine and Functionalized Mesoporous Silica Carriers.

Resveratrol, a naturally occurring polyphenol, has attracted significant attention due to its antioxidant, cardioprotective and anticancer potential. However, its low aqueous solubility limits resveratrol bioavailability and use. In this work, different mesoporous silica matrices were used to encapsulate the polyphenol and to increase its dissolution rate. Pristine MCM-41, MCM-48, SBA-15, SBA-16, FDU-12 and MCF silica were obtained. The influence of SBA-15 functionalized with aminopropyl, isocyanate, phenyl, mercaptopropyl, and propionic acid moieties on resveratrol loading and release profiles was also assessed. The cytotoxic effects were evaluated for mesoporous carriers and resveratrol-loaded samples against human lung cancer (A549), breast cancer (MDA-MB-231) and human skin fibroblast (HSF) cell lines. The effect on apoptosis and cell cycle were assayed for selected resveratrol-loaded carriers. The polyphenol molecules are encapsulated only inside the mesopores, mostly in amorphous state. All materials containing either pristine or functionalized silica carriers increased polyphenol dissolution rate. The influence of the physico-chemical properties of the mesoporous carriers and resveratrol–loaded supports on the kinetic parameters was identified. Resv@SBA-15-SH and Resv@SBA-15-NCO samples exhibited the highest anticancer effect against A549 cells (IC50 values were 26.06 and 36.5 µg/mL, respectively) and against MDA-MB-231 (IC50 values were 35.56 and 19.30 µg/mL, respectively), which highlights their potential use against cancer.

Folic acid-chitosan nanomaterials for delivery of dietary polyphenols

The encapsulation of antioxidant resveratrol, genistein, and curcumin by folic acid-chitosan nanoparticles was studied in aqueous solution, using multiple spectroscopic methods, TEM images and modeling. Structural analysis showed that polyphenol bindings are via hydrophilic, hydrophobic, and H-bonding contacts with resveratrol forming more stable conjugates. As chitosan size increased, the binding efficacy and stability of polyphenol-polymer adducts were increased. Polyphenol binding induced major alterations of chitosan morphology. Folic acid-chitosan nanoparticles are capable of delivering polyphenols in vitro.

Ordered hydrocolloids networks as delivery vehicles of nutraceuticals: Optimal encapsulation of curcumin and resveratrol

Nutraceutical compounds such as curcumin and resveratrol are effective for preventing and treating diabetes, cardiovascular disease, obesity and cancer. However, their unstable properties and water insolubility curtail the wholesome application as well as developing food supplements, functional foods and medicinal foods. Highly efficient and economical delivery systems are helpful to overcome this quandary. Among the several available carrier materials, hydrocolloids stand out tall due to their inbred non-toxic traits, cost-effectiveness and compatibility to humans. Herein, iota-carrageenan (IC), from the marine algae, has been chosen as the model hydrocolloid, which forms thermo-reversible gels and oriented fibers with ordered networks, and curcumin and resveratrol, as model nutraceuticals, have been encapsulated in the IC fibers for different time periods, namely for 1, 2, 3, 4 and 5 weeks to determine the optimal encapsulation time. The results demonstrate that encapsulation time dictates the overall entrapped amount in the IC network with an optimal duration of 3 weeks. The two nutraceuticals are readily protected from heat by the IC network and released in a sustained manner. The outcome offers an elegant opportunity to develop value-added delivery systems of nutraceuticals, in particular, and health promoting and disease preventing compounds, in general, based on the ordered hydrocolloid networks.

Impact of calcium ions and degree of oxidation on the structural, physicochemical, and in-vitro release properties of resveratrol-loaded oxidized gellan gum hydrogel beads

Oxidized gellan gum (OGG) hydrogel beads as delivery systems for resveratrol were fabricated by ionic cross-linking with calcium chloride (CaCl2). The degree of oxidation (DO) and CaCl2 concentration had significant influences on the formation and functional properties of hydrogel beads. The resveratrol encapsulation efficiency (66.43%–79.84%) and loading capacity (4.15%–5.05%) of OGG hydrogel beads were enhanced as DO increased. The hydrogel beads exhibited a uniform spherical shape as observed by scanning electron microscope. Fourier transform infrared spectroscopy analysis confirmed that hydrogen bonds and ionic interaction participated in the formation of hydrogel beads. X-ray diffraction analysis revealed that the physical state of resveratrol was changed from crystalline to amorphous form after encapsulation. Furthermore, the physical stability and antioxidant capacity evaluation demonstrated that the hydrogel bead fabricated with DO80 OGG and CaCl2 concentration of 1.0 M could provide high protection for resveratrol against degradation by environmental stresses and maintain its antioxidant capacity. The DO and CaCl2 concentrations could modulate the in-vitro release behaviors of hydrogel beads and obtain a good small intestinal-targeted release of resveratrol at high DO and medium CaCl2 concentration. These findings suggested that a promising delivery system for encapsulating bioactive ingredients can be fabricated by rational design.

Resveratrol‐Loaded Poly(d,l‐Lactide‐Co‐Glycolide) Microspheres Integrated in a Hyaluronic Acid Injectable Hydrogel for Cartilage Regeneration

Cartilage tissue has a relatively low regenerative capacity which leads to a need for disease‐modifying active pharmaceutical ingredients (APIs) which can stimulate its regeneration and more urgently, effective ways of introducing APIs into the cartilage defects. Herein, an integrated system is proposed in which a hyaluronic acid (HA)‐based injectable hydrogel scaffold is embedded with API‐loaded poly(d,l‐lactide‐co‐glycolide) microspheres (PLGA MPs). This new injectable drug delivery system can successfully deliver APIs locally, increase drug retention time, and promote endogenous cartilage regeneration. In this study, resveratrol (RSV), a small hydrophobic compound is introduced as the selected API. PLGAs with differing copolymer ratios and endgroups are evaluated to study their effects on particle formation, RSV encapsulation, and drug release kinetics. This system is optimized as a 1 month sustained release formulation. In addition, the long‐acting chondrogenic induction of the RSV‐loaded system is evaluated by coculturing with cartilage‐derived progenitor cells in vitro. PLGA–RSV MPs stimulated the expression of cartilage‐related genes and the production of the cartilage‐specific extracellular matrix. This integrated system shows great potential as an injectable formulation for long‐acting chondrogenesis and endogenous cartilage tissue regeneration.

Co-delivery of curcumin and resveratrol through electrosprayed core-shell nanoparticles in 3D printed hydrogel

In this study, the possibility of improving the bioavailability of two potent synergistic nutraceuticals, curcumin and resveratrol, using core-shell nanoparticles and its delivery through 3D printed gelatin hydrogel in a customized structure was examined. The co-axial electrospraying technique was adopted for core-shell nanoparticles formation co-encapsulating both the bioactives in zein core protected by polyethylene glycol (PEG) or ethyl cellulose (EC) as a shell. Biopolymer composition and electrospraying conditions were optimized for core-shell nanoparticle formation. Zein-PEG nanoparticles (∼300 nm) provided 68% and 83% and zein-EC nanoparticles (∼344 nm) provided 54% and 71% efficiency for curcumin and resveratrol encapsulation, respectively. Improved antioxidant activity and transition of both bioactives to amorphous form in the obtained nanoparticles were confirmed. The bioaccessibility of both bioactives was significantly improved in zein-PEG core-shell nanoparticles followed by zein-EC core-shell and simple zein nanoparticles, compared to native bioactives. The maximum bioaccessibility of 79% for curcumin and 82% for resveratrol was observed in zein-PEG core-shell nanoparticles, which is 3.6-fold and 1.7-fold higher than its native form. These nanoparticles also supported intestinal permeability enhancement by 3.5-fold and 2.2-fold for encapsulated curcumin and resveratrol, compared to its native form. To deliver these nanoparticles in consumer-preferred customized structures, 3D printing conditions were optimized to fabricate nanoparticle incorporated gelatin hydrogel 3D structures stable at room temperature. Comparatively, zein-PEG core-shell nanoparticles maintained their structural stability and uniform distribution in the hydrogel matrix for the effective protection of encapsulated bioactives. This 3D printed hydrogel model food loaded with nanoparticles will be a potent nutraceutical oral delivery system with the benefits of shape customization.

Treatment with ultrasound improves the encapsulation efficiency of resveratrol in zein-gum Arabic complex coacervates

The study was conducted to understand the effect of zein-gum Arabic (GA) complex coacervates prepared by ultrasound treatment on the encapsulation of resveratrol. Compared with zein, zein-GA complex coacervation largely increased the encapsulation efficiency from 26.19% to 55.85% and it was further increased to 74.2% after sonication. Also, prominent rise in the related loading capacities from 2.79% to 6.01% was noted. The increased particle size by the addition of GA and polydispersity index of the ternary complex was dramatically reduced after ultrasound treatment; the absolute values of zeta potential were increased. The hydrogen bonds, electrostatic interactions and hydrophobic effects were the main driving forces for the formation of the ternary complex particles. Ultrasound treatment strengthened the hydrogen bonding and electrostatic interactions, resulting in the formation of compact and homogeneous composite nanoparticles with smaller particle size, which was further confirmed by scanning electron microscope and atomic force microscope. These findings reveal the mechanism of ultrasound enhancing the zein-GA complex coacervation to load resveratrol, and demonstrate its promising effect in modifying protein-polysaccharide complex coacervation as a delivery carrier in the functional food and beverage industry.

Phytosomal nanocarriers for encapsulation and delivery of resveratrol- Preparation, characterization, and application in mayonnaise

Resveratrol (RES), a well-known bioactive compound, was encapsulated within nano-phytosome (RES-PHY) for application in mayonnaise. The physico-chemical, microstructure, physical stability, antioxidant activity, encapsulation efficiency (EE%) were evaluated. The particle size, polydispersity index (PDI), and zeta-potential (ζ) of the RES-PHY-nanoparticles were recorded by dynamic light scattering (DLS) as 78.7 nm, ~0.18, −15.9 mv and spherical shapes of the particles with the size under 100 nm were proved by scanning electron microscopy (SEM). The High-Performance-Liquid-Chromatography (HPLC) indicated the EE of 85%. Fourier-transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analyses showed the well-insertion and homogenous embedment of RES within PHY-nanocarrier according to the formation of new hydrogen bonds and amorphous structure of RES-PHY. During 60 days storage of RES-PHY-solution, the particles remained at ~112 nm with a unimodal distribution. The antioxidant activities of RES-PYH-enriched mayonnaise were respectively 84, 82, and 81% after 14, 30, and 60 days of storage that were higher than control samples with pure-RES (75, 62, and 60%) and citric acid (82, 80, and 79%). Overall, the results showed that RES-PHY was able to maintain the antioxidant properties of RES in mayonnaise during shelf-life and could be considered in high-fat foods to reduce oxidation and enhance their nutritional properties.

Encapsulation of resveratrol in zein-polyglycerol conjugate stabilized O/W nanoemulsions: Chemical stability, in vitro gastrointestinal digestion, and antioxidant activity

To overcome the poor water solubility, low chemical stability, and antioxidant activity in aqueous of resveratrol, it was encapsulated in the soybean oil-in-water (O/W) nanoemulsions stabilized by two zein-polyglycerol conjugates, zein-polyglycerol-6 (Zein-PG-6) and zein-polyglycerol-10 (Zein-PG-10). The nanoemulsions showed high stability over 34-day storage in terms of particle characterization and more than 90% encapsulation efficiency of resveratrol. Chemical retentions of resveratrol in nanoemulsions stabilized by Zein-PG-10 was a little better than those prepared with Zein-PG-6. Furthermore, other physicochemical properties of Zein-PG-10 stabilized nanoemulsions, including sustained release and stability against pH, ionic strength, and simulated gastrointestinal digestion, were also better than those of Zein-PG-6. O/W nanoemulsions also significantly improved the antioxidant activity of encapsulated resveratrol. Therefore, the present Zein-PG-10 stabilized O/W nanoemulsion could be used as a promising nano-delivery vehicle to encapsulate and protect resveratrol and other lipophilic bioactive compounds in food or other industries.

Improvement in storage stability and resveratrol retention by fabrication of hollow zein-chitosan composite particles

Solid and hollow particles based on zein have been prepared for the encapsulation of bioactive components. Hollow particles have many advantages over their solid counterpart, due to increased surface area, low density, and sustained release, emerged as a promising delivery system for polyphenols. It is necessary to improve the stability of zein particles for the encapsulation of bioactive components. The current work aims to prepare hollow zein particles by employing chitosan coating and explore the potential of the composite particles for the encapsulation and protection of resveratrol, a natural polyphenol. Hollow zein (HZ) and zein-chitosan (HZ-CH) particles were characterized in terms of size, surface charge, morphological structure, particle yield and antioxidant activity. Encapsulation of resveratrol in the zein matrix was studied by the help of fluorescence, infrared and X-ray diffraction techniques. The composite particles were also subjected to storage and in vitro digestion. Particle yield was greater than 90% when the concentrations of chitosan were greater than 0.02%. HZ-CH particles were positively charged and bigger in size as compare to HZ particles. Resveratrol entrapment caused an apparent increase in the size of the particles. The highest encapsulation efficiency and loading capacity of resveratrol were 91% and 14% in the hydrophobic zein shell of HZ-CH particles, respectively. The chitosan coating improved the storage and digestion stability of resveratrol-loaded hollow zein particles and the storage stability of encapsulated resveratrol and exhibited a sustained in vitro release of resveratrol. Therefore, the hollow zein composite particles could be used as an efficient delivery system for resveratrol in the development of functional foods.

Oral delivery of folate-targeted resveratrol-loaded nanoparticles for inflammatory bowel disease therapy in rats

AimsIn the current study, resveratrol-loaded PLGA nanoparticles targeted with folate were developed in order to protect resveratrol from fast degradation, modify its pharmacokinetics and increase its intestinal permeation. Then, the therapeutic efficacy of the prepared system was evaluated in suppression of colon inflammation on TNBS-induced colitis model. Main methodsIn this regard, resveratrol was encapsulated in PLGA and FA-conjugated PLGA in order to prepare non-targeted (PLGA-RSV) and targeted (PLGA-FA-RSV) platforms, respectively. Key findingsObtained results demonstrated that the prepared formulations encapsulated the resveratrol with high encapsulation efficiency of 90.7% ± 5.1% for PLGA-RSV and 59.1% ± 3.3% for PLGA-FA-RSV. In vitro release experiment showed that the prepared formulations were capable of retaining good amount of resveratrol under the simulated gastric condition (HCl 0.1 N, pH 1.2), while significant amount of resveratrol was released under simulated intestinal condition (PBS, pH 7.4). The trans-well permeability rates through Caco-2 monolayer during 180 min, was determined to be 4.5%, 61% and 99% for resveratrol, PLGA-RSV and PLGA-FA-RSV respectively. The pathological analysis of the rat intestinal sections (hematoxylin & eosin staining) at 7th day post-TNBS colonic inflammation induction illustrated that the oral administrations of FA-PLGA-RSV and PLGA-RSV were able to significantly inhibit the inflammation and reduce neutrophil and lymphocytes accumulation. It is worth noting that the folate-targeted system demonstrated highest efficacy in suppressing colon inflammation. SignificanceIt could be concluded that the encapsulation of resveratrol into biodegradable folate-targeted PLGA nanoparticles could introduce a potent platform in suppressing colonic inflammation thus offering a great capability for clinical translation.

Resveratrol encapsulation in high molecular weight chitosan-based nanogels for applications in ocular treatments: Impact on human ARPE-19 culture cells

Oxidative stress and inflammation play a pivotal role in ocular diseases. Resveratrol (RSV) is a natural bioactive that has recently attracted attention due to it potent antioxidant and anti-inflammatory properties. However, RSV presents poor aqueous solubility and chemical instability. Besides, effective drug delivery to the posterior segment of the eye is challenge. Nanotechnology emerges as a possible solution to improve both limitations. Here, we developed and characterized nanogels (NG) based on high molecular weight chitosan (HCS) crosslinked with sodium tripolyphosphate. The distribution size of NG presented a major population around 140 nm with a ζ-potential value of 32 ± 2 mV. TEM and AFM images showed that NG exhibited a rounded morphology. RSV encapsulation efficiency was 59 ± 1%. Photodegradation experiments showed that HCS by its own protects RSV from UV light-induced degradation. Biocompatibility assays revealed that NG were not cytotoxic neither inflammatory in human retinal pigment epithelial cells (ARPE-19), which constitutes the outer blood-retinal barrier. After cellular internalization, we report an endo-lysosomal escape of NG, which is crucial for efficient nanocarriers delivery systems. In conclusion, we envision that HCS based NG could constitute novel carriers for RSV, opening the possibility of its application in ocular diseases.

Resveratrol-loaded proniosomes: Formulation, characterization and fortification

Resveratrol was encapsulated into proniosomes with the aim of enhancing its applications in food. Maltodextrin, lactose monohydrate and pullulan were used as wall materials for the preparation of resveratrol-loaded proniosomes by thin-film hydration technique. The morphological, microstructural, entrapment and release properties were determined. The wall material had marked (p < 0.01) influence on the shape and hydrodynamic diameter of proniosomes. Maltodextrin-based proniosomes were smooth and spherical shaped while lactose and pullulan-based proniosomes were flaky with sharp edges. The maltodextrin-based niosomes had the lowest hydrodynamic diameter of 168.73 nm, zeta potential of −29.6 mV, entrapment efficiency of 90.11%, and release of 21.8% at 2 h and 78.2% after 8 h in gastric and intestinal conditions, respectively. Fourier-transform infrared spectroscopy and X-ray diffractometry confirmed successful encapsulation of resveratrol. The antioxidant activity of maltodextrin and lactose-based resveratrol-loaded proniosomes was comparable to that of pure resveratrol. From dynamic light scattering, FTIR, in-vitro release, and antioxidant activity studies, it could be concluded that encapsulation of resveratrol as proniosomes would considerably enhance its bioavailability. Milk and yogurt fortified with resveratrol-loaded proniosomes did not exhibit any adverse effect on organoleptic qualities.

Efficacy of resveratrol encapsulated microsponges delivered by pectin based matrix tablets in rats with acetic acid-induced ulcerative colitis

Objectives: The objective of the present work to encapsulate the resveratrol (RES) inside the chitosan-based microsponges, employing the systematic optimization by 33 Box–Behnken design for the colonic targeting. Significance: Enhanced therapeutic efficacy of RES-loaded microsponges and matrix tablets, vis-a-vis pureRES for ulcerative colitis. Methods: RES-loaded microsponges were prepared employing the systematic optimization by 33 Box–Behnken design for the colonic targeting. The best-optimizedRES-loaded microsponge was compressed in the form of a tablet, employing pectin as a matrix-forming material. The encapsulation of RES inside microsponge was confirmed by XRD, DSC and FT-IR. Further, both RES-loaded microsponges and matrix tablets were evaluated for in vitro release kinetics and further evaluated for in vivo ulcerative colitis animal model. Results: Optimization experiments was obtained as the high value of r 2 (particle size = 0.9999; %EE = 0.9652; %CDR = 0.9469) inferred excellent goodness of fit. SEM revealed nearly spherical and porous nature of RES-loaded microsponges. The in vitro release kinetic showed zero-order release for RES-loaded microsponges and Korsmeyer–Peppas model for matrix tablets. The pharmacodynamic studies, in ulcerative colitis rat model, indicated better therapeutic efficacy of drug-loaded microsponges and matrix tablets, vis-a-vis pure RES. Thus, the present study advocates the potential of RES based microsponges delivered by pectin based matrix tablet, in the treatment of various colonic disorders. Conclusion: The present study proved that RES-loaded microsponges and matrix tablets based on chitosan and pectin can be the ideal delivery system for colonic delivery of RES.

Electrohydrodynamic Encapsulation of Resveratrol Using Food-Grade Nanofibres: Process Optimization, Characterization and Fortification

Utilization of resveratrol as a nutraceutical in foods is limited due to its low bioavailability and chemical instability. Therefore, resveratrol was encapsulated into nanofibres by electrospinning at concentrations of 15, 18 and 21% TS, applied voltage of 13, 18 and 23 kV and feed rates of 0.6 and 1 mL/h using WPI-pullulan as wall material. Electrospinning conditions were optimized as 18% TS, 18 kV applied voltage and 0.6 mL/h flow rate. SEM images showed formation of clean and continuous fibres at 18 and 23 kV applied voltage, with a mean fibre diameter of 63 to 208 nm and encapsulation efficiency of 74 and 96.70%. Successful encapsulation of resveratrol was confirmed by FTIR and XRD analyses. The zeta potential of resveratrol-loaded nanofibres was in the range of − 20.5 to − 32.2 mV, suggestive of higher stability. The antioxidant property of resveratrol in nanofibres was retained. No significant physiochemical and sensorial changes were observed in resveratrol fortified milk.

Switching from Conventional to Nano-natural Phytochemicals to Prevent and Treat Cancers: Special Emphasis on Resveratrol.

Natural phytochemicals and their derivatives have been used in medicine since prehistoric times. Natural phytochemicals have potential uses against various disorders, including cancers. However, due to low bioavailability, their success in clinical trials has not been reproduced. Nanotechnology has played a vital role in providing new directions for diagnosis, prevention, and treatment of different disorders, and of cancer in particular. Nanotechnology has demonstrated the capability to deliver conventional natural products with poor solubility or a short half-life to target specific sites in the body and regulate the release of drugs. Among the natural products, the phytoalexin resveratrol has demonstrated therapeutic effects, including antioxidant, antiinflammatory, and anti-proliferative effects, as well as the potential to inhibit the initiation and promotion of cancer. However, low water solubility and extensive first-pass metabolism lead to poor bioavailability of resveratrol, hindering its potential. Conventional dosage forms of resveratrol, such as tablets, capsules, dry powder, and injections, have met with limited success. Nanoformulations are now being investigated to improve the pharmacokinetic characteristics, as well as to enhance the bioavailability and targetability of resveratrol. This review details the therapeutic effectiveness, mode of action, and pharmacokinetic limitations of resveratrol, as well as discusses the successes and challenges of resveratrol nanoformulations. Modern nanotechnology techniques to enhance the encapsulation of resveratrol within nanoparticles and thereby enhance its therapeutic effects are emphasized. To date, no resveratrol-based nanosystems are in clinical use, and this review would provide a new direction for further investigations on innovative nanodevices that could consolidate the anticancer potential of resveratrol.

Comparative Evaluation of Solubility, Cytotoxicity and Photostability Studies of Resveratrol and Oxyresveratrol Loaded Nanosponges.

Resveratrol and oxyresveratrol are natural polyphenolic stilbenes with several important pharmacological activities. However, low solubility and aqueous instability are the major limitations in their drug delivery applications. In the present work, we demonstrated the encapsulation of resveratrol and oxyresveratrol with nanosponge to improve solubility and stability. Several characterization techniques were used to confirm the encapsulation of both drug molecules within the nanosponges. The high encapsulation efficiency of resveratrol (77.73%) and oxyresveratrol (80.33%) was achieved within the nanosponges. Transmission electron microscopy suggested uniform spherical size particles of resveratrol and oxyresveratrol loaded nanosponges. Compared to free drugs, better protection against UV degradation was observed for resveratrol-loaded nanosponge (2-fold) and oxyresveratrol-loaded nanosponge (3-fold). Moreover, a higher solubilization of resveratrol- and oxyresveratrol-loaded nanosponges lead to a better antioxidant activity compared to drug molecules alone. Cytotoxicity studies against DU-145 prostate cancer cell lines further suggested improved activity of both resveratrol and oxyresveratrol-loaded nanosponges without any significant toxicity of blank nanosponges.