Brain-targeted delivery of resveratrol using solid lipid nanoparticles functionalized with apolipoprotein E

Neves, Ana Rute; Queiroz, Joana Fontes; Reis, Salette

doi:10.1186/s12951-016-0177-x

Cited by 182 publications

(106 citation statements)

References 52 publications

(65 reference statements)

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“…Formulations of resveratrol have also been used for several other clinical conditions . For example, micronized resveratrol is reported to reduce blood pressure in hypertensive patients when coadministered with standard antihypertensive medication.…”

Section: Completed Clinical Trialsmentioning

confidence: 99%

Health benefits of resveratrol: Evidence from clinical studies

Singh

Verma

et al. 2019

Medicinal Research Reviews

367

238

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Resveratrol is a polyphenolic nutraceutical that exhibits pleiotropic activities in human subjects. The efficacy, safety, and pharmacokinetics of resveratrol have been documented in over 244 clinical trials, with an additional 27 clinical trials currently ongoing. Resveretrol is reported to potentially improve the therapeutic outcome in patients suffering from diabetes mellitus, obesity, colorectal cancer, breast cancer, multiple myeloma, metabolic syndrome, hypertension, Alzheimer's disease, stroke, cardiovascular diseases, kidney diseases, inflammatory diseases, and rhinopharyngitis. The polyphenol is reported to be safe at doses up to 5 g/d, when used either alone or as a combination therapy. The molecular basis for the pleiotropic activities of resveratrol are based on its ability to modulate multiple cell signaling molecules such as cytokines, caspases, matrix metalloproteinases, Wnt, nuclear factor‐κB, Notch, 5′‐AMP‐activated protein kinase, intercellular adhesion molecule, vascular cell adhesion molecule, sirtuin type 1, peroxisome proliferator‐activated receptor‐γ coactivator 1α, insulin‐like growth factor 1, insulin‐like growth factor‐binding protein 3, Ras association domain family 1α, pAkt, vascular endothelial growth factor, cyclooxygenase 2, nuclear factor erythroid 2 like 2, and Kelch‐like ECH–associated protein 1. Although the clinical utility of resveratrol is well documented, the rapid metabolism and poor bioavailability have limited its therapeutic use. In this regard, the recently produced micronized resveratrol formulation called SRT501, shows promise. This review discusses the currently available clinical data on resveratrol in the prevention, management, and treatment of various diseases and disorders. Based on the current evidence, the potential utility of this molecule in the clinic is discussed.

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Section: Completed Clinical Trialsmentioning

confidence: 99%

Health benefits of resveratrol: Evidence from clinical studies

Singh

Verma

et al. 2019

Medicinal Research Reviews

367

238

View full text Add to dashboard Cite

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“…Furthermore, this poor bioavailability will also affect the concentration of resveratrol in the brain after crossing the blood brain barrier (BBB). However, the most encouraging aspect is that resveratrol reaches the brain both during short term and acute treatments [75, 76] and significant efforts are ongoing to increase the concentration of resveratrol in the brain using various delivery system [77, 78]. …”

Section: Discussionmentioning

confidence: 99%

Resveratrol inhibits phorbol ester-induced membrane translocation of presynaptic Munc13-1

Pany

Ghosh

You

et al. 2017

Biochimica et Biophysica Acta (BBA) - General Subjects

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Background Resveratrol (1) is a naturally occurring polyphenol that has been implicated in neuroprotection. One of resveratrol’s several biological targets is Ca2+-sensitive protein kinase C alpha (PKCα). Resveratrol inhibits PKCα by binding to its activator-binding C1 domain. Munc13-1 is a C1 domain-containing Ca2+-sensitive SNARE complex protein essential for vesicle priming and neurotransmitter release. Methods To test if resveratrol could also bind and inhibit Munc13-1, we studied the interaction of resveratrol and its derivatives, (E)-1,3-dimethoxy-5-(4-methoxystyryl)benzene, (E)-5,5’-(ethene-1,2-diyl)bis(benzene-1,2,3-triol), (E)-1,2-bis(3,4,5-trimethoxyphenyl)ethane, and (E)-5-(4-(hexadecyloxy)-3,5-dihydroxystyryl)benzene-1,2,3-triol with Munc13-1 by studying its membrane translocation from cytosol to plasma membrane in HT22 cells and primary hippocampal neurons. Results Resveratrol, but not the derivatives inhibited phorbol ester-induced Munc13-1 translocation from cytosol to membrane in HT22 cells and primary hippocampal neurons, as evidenced by immunoblot analysis and confocal microscopy. Resveratrol did not show any effect on Munc13-1H567K, a mutant which is not sensitive to phorbol ester. Binding studies with Munc13-1 C1 indicated that resveratrol competes with phorbol ester for the binding site. Molecular docking and dynamics studies suggested that hydroxyl groups of resveratrol interact with phorbol-ester binding residues in the binding pocket. Conclusions and significance This study characterizes Munc13-1 as a target of resveratrol and highlights the importance of dietary polyphenol in the management of neurodegenerative diseases.

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“…From solid lipidic nanoparticles (containing cetylpalmitate and Tween 80) functionalized with ApoE, permeability showed a significant increase (ca. 2 times higher) in penetration through hCMEC/D3 cells monolayers compared to non‐functionalized ones …”

Section: Overcoming Limitationsmentioning

confidence: 95%

“…Solid lipidic nanoparticles ApoE functionalized reduced ca. 1.5 times the RSV release and the initial burst effect was avoided in comparison with non‐functionalized ones after 28 h, in blood stream simulated conditions at 37 °C …”

Section: Overcoming Limitationsmentioning

confidence: 99%

“…In vitro cell viability studies of solid lipid nanoparticles modified with a chitosan derivative were performed using NIH/3T3 mouse embryonic fibroblast cells and none of the formulations showed any significant toxicity . Moreover, in vitro toxicity studies of solid lipid nanoparticles functionalized with ApoE revealed no toxicity up to 50 μM over 4 h of incubation using hCMEC/D3 cells …”

Section: Overcoming Limitationsmentioning

confidence: 99%

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Recent Strategies in Resveratrol Delivery Systems

2019

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Resveratrol, a natural polyphenolic stilbenoid widely found in grapes and wines, displays beneficial properties such as cardio‐protective, antioxidant and anti‐inflammatory activities. Trans‐resveratrol (RSV) is the most bioactive and more abundant stereoisomer found in nature. Despite the positive properties of RSV, there are various factors that limit its effectiveness, including low aqueous solubility, low oral bioavailability and chemical instability. During the last years, an increasing number of strategies such as nano and micro encapsulation have been developed in order to overcome these limitations and enhance the use of RSV in nutritional and pharmaceutical applications. This Review summarizes the advances and main properties of several RSV carriers and delivery systems reported during the last 5 years.

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Brain-targeted delivery of resveratrol using solid lipid nanoparticles functionalized with apolipoprotein E

Cited by 182 publications

References 52 publications

Health benefits of resveratrol: Evidence from clinical studies

Health benefits of resveratrol: Evidence from clinical studies

Resveratrol inhibits phorbol ester-induced membrane translocation of presynaptic Munc13-1

Recent Strategies in Resveratrol Delivery Systems

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