The Impact of Aqueous Solubility and Dose on the Pharmacokinetic Profiles of Resveratrol

Das, Surajit; Lin, Hai‐Shu; Ho, Paul C.; Ng, Ka‐Yun

doi:10.1007/s11095-008-9677-1

Cited by 184 publications

(134 citation statements)

References 26 publications

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“…30 Our RL-FNPs showed curves of liberation with an initial burst, reaching resveratrol saturation of the aqueous medium in 3-4 hours and maintaining a resveratrol concentration higher than 15 mg/L in PBS medium over a period of 80 hours. Considering a volume of 25 mL of PBS, 0.5 mg of resveratrol was released initially until medium saturation was reached.…”

Section: Release Of Resveratrol From Rl-fnpsmentioning

confidence: 73%

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats

Lozano-Pérez¹,

Rodríguez-Nogales²,

Ortiz-Cullera³

et al. 2014

IJN

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Purpose We aimed to evaluate the intestinal anti-inflammatory properties of silk fibroin nanoparticles, around 100 nm in size, when loaded with the stilbene compound resveratrol, in an experimental model of rat colitis. Methods Nanoparticles were loaded with resveratrol by adsorption. The biological effects of the resveratrol-loaded nanoparticles were tested both in vitro, in a cell culture of RAW 264.7 cells (mouse macrophages), and in vivo, in the trinitrobenzenesulfonic acid model of rat colitis, when administered intracolonically. Results The resveratrol liberation in 1× phosphate-buffered saline (PBS; pH 7.4) was characterized by fast liberation, reaching the solubility limit in 3 hours, which was maintained over a period of 80 hours. The in vitro assays revealed immunomodulatory properties exerted by these resveratrol-loaded nanoparticles since they promoted macrophage activity in basal conditions and inhibited this activity when stimulated with lipopolysaccharide. The in vivo experiments showed that after evaluation of the macroscopic symptoms, inflammatory markers, and intestinal barrier function, the fibroin nanoparticles loaded with resveratrol had a better effect than the single treatments, being similar to that produced by the glucocorticoid dexamethasone. Conclusion Silk fibroin nanoparticles constitute an attractive strategy for the controlled release of resveratrol, showing immunomodulatory properties and intestinal anti-inflammatory effects.

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Section: Release Of Resveratrol From Rl-fnpsmentioning

confidence: 73%

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats

Lozano-Pérez¹,

Rodríguez-Nogales²,

Ortiz-Cullera³

et al. 2014

IJN

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“…Due to its different physicochemical properties such as molecular weight, number of hydrogen bond donor and acceptor, rotatable bond, clogP, and polar surface area, resveratrol has poor biomembrane permeability. The poor oral bioavailability [14] considerably less than 1% would attribute to different the metabolic issue [44], such as very short half-life in rat liver microsomes. Furthermore, poor oral bioavailability is due to the first-pass metabolism in intestine [45,46], while increased dose and repeated dose escalation would not affect the bioavailibity.…”

Section: Resultsmentioning

confidence: 99%

The Influence of Energy of Consciousness Healing Treatment on Low Bioavailable Resveratrol in Male Sprague Dawley Rats

Branton¹

2017

IJCDA

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Abstract:Resveratrol is a natural dietary antioxidant polyphenol that believed to be effective in improving overall health.The biological activity of resveratrol is limited by its poor absorption and first-pass metabolism that lead to have very low plasma concentrations following oral administration. Therefore, the present study was performed to determine the effects of The Trivedi Effect ® -Energy of Consciousness Healing Treatment by a renowned Biofield Energy Healer, Alice Branton on resveratrol and rats through the measurement of plasma concentrations after oral administration of resveratrol. The test item, resveratrol was divided into two parts. One part was denoted as the control, while the other part was defined as the Biofield Energy Treated sample. Additionally, one group of animals also received Biofield Energy Treatment under similar conditions. Resveratrol oral formulations were administrated by oral gavage at a dose of 150 mg/kg in groups viz. G1 (untreated resveratrol), G2 (Biofield Treated resveratrol) and G3 (Biofield Treated animals received untreated resveratrol) group. The results showed that resveratrol had a very low oral plasma exposure of 91.71 ng/mL in control group. The Biofield Treatment significantly enhanced the relative oral exposure (AUC 0-t ) of resveratrol by 23.35% in G2 group compared to the control group. The Biofield Treatment also improved plasma peak concentration (C max ) of resveratrol by 125% and 28.5% in G2 and G3 groups, respectively compared with the control group. Plasma concentrations of resveratrol in G1 was declined with a rapid elimination half-life (T 1/2 , 1.48 hours), followed by sudden increases in plasma concentrations 12 to 24 hours after the test item administration. These plasma concentrations resulted in a significant prolongation of the terminal elimination half-life of resveratrol. The oral elimination T 1/2 of resveratrol in G2 and G3 were 4.67 and 9.0 hours, respectively as compared to the G1. The apparent oral plasma clearance of resveratrol decreased significantly by 54%, and 17.5% in G2 group and G3 group, respectively as compared to the control group. The mean residence time (MRT last ) of resveratrol significantly increased in G2 group (6.45 hours) and G3 group (7.70 hours), as compared to the control group. These data demonstrates greater bioavailability and total plasma level of resveratrol in rats which might be translated into better in vivo biological activity. Hence, The Trivedi Effect ® -Energy of Consciousness Healing Treatment could be considered as an innovative strategy which opens new avenues to overcome poorly absorbed nutraceuticals/pharmaceuticals and can also improve the therapeutic performance of orally active molecules.

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“…It is worth noting that pre-clinical studies using the same resveratrol concentration as ours have previously demonstrated mood lifting effects, not just following intraperitoneal administration (acute or chronic regimen, respectively; Samardzic et al, 2013;Wang et al, 2013), but also after intra-gastric administration (acute or chronic regimen, respectively; Xu et al, 2010;Yu et al, 2012), thereby alleviating some of the concerns surrounding first-pass effects. In contrast to these studies, we used both (ethanol and 2-Hydroxypropyl)-b-cyclodextrin to increase the aqueous solubility and stability of resveratrol, an approach that, while not likely to be effective at enhancing the extent of the oral bioavailability, can nonetheless enhance its rate (Amri et al, 2012;Das et al, 2008). Future investigations may address issues of optimization of oral bioavailability by considering alternative formulations (Amri et al, 2012), the use of resveratrol derivatives with higher oral availability, such as pterostilbene (e.g.…”

Section: Discussionmentioning

confidence: 99%

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Poirier

Imamura

Zanoletti

et al. 2014

Journal of Psychiatric Research

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a b s t r a c tAdolescence is increasingly recognized as a critical period for the development of the social system, through the maturation of social competences and of their underlying neural circuitries. The present study sought to test the utility of resveratrol, a dietary phenol recently reported to have mood lifting properties, in modulating social interaction that is deficient following early life adversity. The main aims were to 1) pharmacologically restore normative social investigation levels dampened by peripubertal stress in rats and 2) identify neural pathways engaged by this pharmacological approach. Following peripubertal (P28e42) stress consisting of unpredictable exposures to fearful experiences, at adulthood the subjects' propensity for social exploration was examined in the three-chamber apparatus, comparing time invested in social or non-social investigation. Administered intraperitoneally 30 min before testing, resveratrol (20 mg/kg) normalized the peripubertal stress-induced social investigation deficit seen in the vehicle group, selectively altering juvenile but not object exploration. Examination of prefrontal cortex subregion protein samples following acute resveratrol treatment in a separate cohort revealed that while monoamine oxidase A (MAOA) enzymatic activity remained unaltered, nuclear AKT activation was selectively increased in the infralimbic cortex, but not in the prelimbic or anterior cingulate cortex. In contrast, androgen receptor nuclear localization was increased in the prelimbic cortex, but not in the infralimbic or anterior cingulate cortex. This demonstration that social contact deficits are reversed by resveratrol administration emphasizes a prosocial role for this dietary phenol, and evokes the possibility of developing new treatments for social dysfunctions.

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The Impact of Aqueous Solubility and Dose on the Pharmacokinetic Profiles of Resveratrol

Abstract: Aqueous solubility barrier might affect the speed but not the extent of resveratrol absorption. Further, dose manipulation (up to 50 mg kg(-1)) did not have a significant impact on the oral bioavailability of resveratrol.

Cited by 184 publications

References 26 publications

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats

The Influence of Energy of Consciousness Healing Treatment on Low Bioavailable Resveratrol in Male Sprague Dawley Rats

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

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The Impact of Aqueous Solubility and Dose on the Pharmacokinetic Profiles of Resveratrol

Abstract: Aqueous solubility barrier might affect the speed but not the extent of resveratrol absorption. Further, dose manipulation (up to 50 mg kg(-1)) did not have a significant impact on the oral bioavailability of resveratrol.

Cited by 184 publications

References 26 publications

Silk fibroin nanoparticles constitute a&nbsp;vector for controlled release of resveratrol in&nbsp;an&nbsp;experimental model of inflammatory bowel&nbsp;disease in rats

Silk fibroin nanoparticles constitute a&nbsp;vector for controlled release of resveratrol in&nbsp;an&nbsp;experimental model of inflammatory bowel&nbsp;disease in rats

The Influence of Energy of Consciousness Healing Treatment on Low Bioavailable Resveratrol in Male Sprague Dawley Rats

Social deficits induced by peripubertal stress in rats are reversed by resveratrol

Contact Info

Product

Resources

About

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats

Silk fibroin nanoparticles constitute a vector for controlled release of resveratrol in an experimental model of inflammatory bowel disease in rats