Recent advances of resveratrol in nanostructured based delivery systems and in the management of HIV/AIDS

Singh, Gurinder; Pai, Roopa S

doi:10.1016/j.jconrel.2014.09.002

Cited by 66 publications

(47 citation statements)

References 86 publications

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“…Resveratrol offers pleiotropic health beneficial effects, including antioxidant and anti-83 aging effects 3 , cardioprotective 4 , anticancer 1 , neuroprotective 5 and HIV/AIDS 84 activities 6 . 85…”

mentioning

confidence: 99%

Zein-Based Nanoparticles Improve the Oral Bioavailability of Resveratrol and Its Anti-inflammatory Effects in a Mouse Model of Endotoxic Shock

Peñalva

Esparza

Larrañeta

et al. 2015

J. Agric. Food Chem.

164

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27Resveratrol offers pleiotropic health beneficial effects including its reported capability to 28 inhibit lipopolysaccharide (LPS) induced cytokine production. The aim of this work was 29 to prepare, characterize and evaluate a resveratrol nanoparticulate formulation based 30 on zein. For this purpose the oral bioavailability of the encapsulated polyphenol as well 31 as its anti-inflammatory effect in a mouse model of endotoxic shock were studied. 32Resveratrol-loaded nanoparticles displayed sizes around 300 nm with a negative zeta 33 potential (-51 mV) and a polyphenol loading close to 80 μg/mg. In vitro, the release of 34 resveratrol from the nanoparticles was found to be pH-independent and adjusted well 35 to the Peppas-Salin kinetic model, suggesting a mechanism based on the combination 36 between diffusion and erosion of the nanoparticle matrix. Pharmacokinetic studies 37 demonstrated that zein-based nanoparticles provided high and prolonged plasma 38 levels of the polyphenol for at least 48 h. The oral bioavailability of resveratrol when 39 administered in these nanoparticles increased up to 50% (20-fold higher than for the 40 control solution of the polyphenol). Furthermore, nanoparticles administered daily for 7 41 days at 15 mg/kg, were able to diminish the endotoxic symptoms induced in mouse by 42 the ip administration of LPS (i.e. hypothermia, piloerection and stillness). In addition, 43 serum TNF-α levels were slightly lower (about 15%) of those observed for the control. 44 45

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confidence: 99%

Zein-Based Nanoparticles Improve the Oral Bioavailability of Resveratrol and Its Anti-inflammatory Effects in a Mouse Model of Endotoxic Shock

Peñalva

Esparza

Larrañeta

et al. 2015

J. Agric. Food Chem.

164

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show abstract

“…Several types of research have been conducted in last two decades; that demonstrate that resveratrol possesses anti-inflammatory, anticancer, antiviral, anti-arthritic and anti-oxidant properties [34]. Its poor absorption, bioavailability and low selectivity have limited its clinical use.…”

Section: Resveratrolmentioning

confidence: 99%

Liposomes Containing Phytochemicals for Cancer Treatment-an Update

Khan

Suvarna

2016

Int J Curr Pharm Sci

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Many phytochemicals exhibit promising effects in treatment and prevention of various cancers, but due to their poor water solubility, stability, bioavailability and target specificity make administering them at therapeutic doses impractical. This is especially true for curcumin, quercetin, resveratrol and berberine. There is rising activity in developing nano drug delivery systems for these phytochemicals. These nano drug delivery systems mainly include liposomes, micelles, solid lipid nanoparticles, nanoemulsions, which are biocompatible and biodegradable nanoparticles. These nanoparticles can increase the stability and aqueous solubility of phytochemicals. They can also be used as sustained drug delivery systems. Much work has also proven that they enhance the absorption and bioavailability of the phytochemicals, protect them from premature enzymatic degradation or metabolism, hence prolonging their circulation time. Besides these parameters, in this review, we have also mentioned the improved target specificity of phytochemicals to cancer cells or tumours via passive or targeted delivery. Hence, nanotechnology cleared the way for developing phytochemical-loaded nanoparticles for prevention and treatment of cancer.

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“…A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. The parent compound and its conjugated metabolite undergo enterohepatic recirculation, resulting in multiple peaks in the plasma concentration-time profile (Singh and Pai 2014c). Marked enhancement in the effective permeability, a direct measure of absorption of the S-SNEDDS across the intestine, clearly demonstrates that the S-SNEDDS formulation was able to augment drug absorption in rats.…”

Section: In Vivo Pharmacokinetic Studies In Ratsmentioning

confidence: 99%

In vitro and in vivo performance of supersaturable self-nanoemulsifying system of trans-resveratrol

Singh

Pai

2014

Artificial Cells, Nanomedicine, and Biotechnology

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To develop an optimized supersaturable self-nanoemulsifying drug delivery system (S-SNEDDS) in order to improve the oral bioavailability of trans-resveratrol (t-RVT), together with surmounting poor aqueous solubility, enterohepatic recirculation and controlling drug precipitation, by employing a precipitation inhibitor (PPI) that is, hydroxypropyl methylcellulose (HPMC). The long-term stability of a previously reported formulation optimized long chain triglycerides (OPT LCT-SNEDDS), consisting of Lauroglycol FCC and Transcutol P, indicated rapid precipitation of trans-resveratrol. Following incorporation of the selected PPI, the precipitates were differentiated using the X-ray diffraction (XRD) technique. An in vitro supersaturation test was carried out for the S-SNEDDS formulation. The S-SNEDDS formulation was appraised for pharmacokinetic and in situ perfusion studies. In vitro dilution of the S-SNEDDS formulation resulted in the formation of a nanoemulsion, followed by a slow precipitation of t-RVT in the S-SNEDDS formulation vis-à-vis SNEDDS formulated with OPT-LCT, where it undergoes rapid precipitation, yielding a low t-RVT concentration. The pharmacokinetic study indicated that the AUC(0-8h) of the S-SNEDDS formulation increased by nearly 1.33-fold in the presence of HPMC vis-à-vis the OPT LCT-SNEDDS, at a drug dose of 20 mg/kg. The in situ perfusion parameters, viz., fraction absorbed and effective permeability, demonstrated significant improvement in the rate and extent of absorption from the S-SNEDDS formulation. This case demonstrates that the supersaturatable approach is effective in delivering and in improving the oral bioavailability of t-RVT.

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Recent advances of resveratrol in nanostructured based delivery systems and in the management of HIV/AIDS

Cited by 66 publications

References 86 publications

Zein-Based Nanoparticles Improve the Oral Bioavailability of Resveratrol and Its Anti-inflammatory Effects in a Mouse Model of Endotoxic Shock

Zein-Based Nanoparticles Improve the Oral Bioavailability of Resveratrol and Its Anti-inflammatory Effects in a Mouse Model of Endotoxic Shock

Liposomes Containing Phytochemicals for Cancer Treatment-an Update

In vitro and in vivo performance of supersaturable self-nanoemulsifying system of trans-resveratrol

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