Optimized PLGA nanoparticle platform for orally dosed<i>trans</i>-resveratrol with enhanced bioavailability potential

Singh, Gurinder; Pai, Roopa S

doi:10.1517/17425247.2014.890588

Cited by 103 publications

(53 citation statements)

References 35 publications

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“…68,175 PLGA-coated resveratrol nanoparticles enhance the bioavailability of resveratrol for up to 4 days in a rat model. 176 Their research group also studied sustained release of trans-resveratrol in vitro and found higher solubility and dissolubility of trans-resveratrol. 68,175,176 In addition, a combination of one or two nanosized bioactive compounds has multiple health beneficial effects for certain diseases, which further reduces the multiple drug load.…”

Section: Nanoresveratrolmentioning

confidence: 99%

“…176 Their research group also studied sustained release of trans-resveratrol in vitro and found higher solubility and dissolubility of trans-resveratrol. 68,175,176 In addition, a combination of one or two nanosized bioactive compounds has multiple health beneficial effects for certain diseases, which further reduces the multiple drug load. Curcumin and resveratrol encapsulated nanoliposomes have an antitumor effect against prostate cancer.…”

Section: Nanoresveratrolmentioning

confidence: 99%

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Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Ganesan¹,

Ko²,

Kim³

et al. 2015

IJN

102

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Oxidative stress plays a very critical role in neurodegenerative diseases, such as Parkinson’s disease (PD), which is the second most common neurodegenerative disease among elderly people worldwide. Increasing evidence has suggested that phytobioactive compounds show enhanced benefits in cell and animal models of PD. Curcumin, resveratrol, ginsenosides, quercetin, and catechin are phyto-derived bioactive compounds with important roles in the prevention and treatment of PD. However, in vivo studies suggest that their concentrations are very low to cross blood–brain barrier thereby it limits bioavailability, stability, and dissolution at target sites in the brain. To overcome these problems, nanophytomedicine with the controlled size of 1–100 nm is used to maximize efficiency in the treatment of PD. Nanosizing of phytobioactive compounds enhances the permeability into the brain with maximized efficiency and stability. Several nanodelivery techniques, including solid lipid nanoparticles, nanostructured lipid carriers, nanoliposomes, and nanoniosomes can be used for controlled delivery of nanobioactive compounds to brain. Nanocompounds, such as ginsenosides (19.9 nm) synthesized using a nanoemulsion technique, showed enhanced bioavailability in the rat brain. Here, we discuss the most recent trends and applications in PD, including 1) the role of phytobioactive compounds in reducing oxidative stress and their bioavailability; 2) the role of nanotechnology in reducing oxidative stress during PD; 3) nanodelivery systems; and 4) various nanophytobioactive compounds and their role in PD.

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Section: Nanoresveratrolmentioning

confidence: 99%

Section: Nanoresveratrolmentioning

confidence: 99%

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Ganesan¹,

Ko²,

Kim³

et al. 2015

IJN

102

View full text Add to dashboard Cite

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“…However, there was no double peaks phenomenon in rats by administration of GNA-NS. As the literature reported, nanoparticulate drug delivery system can overcome the enterohepatic recirculation phenomena (Singh et al, 2014). For example, Hong et al (2014) prepared myricetin NS and the enterohepatic recirculation of myricetin crude drug in rats was subdued by administration of NS formulation.…”

Section: In Vivo Evaluation Of Gna-nsmentioning

confidence: 99%

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Yuan

Zhang

et al. 2015

Drug Delivery

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Nanosuspensions (NS) can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. PEG as a non-ionic surfactant plays an important role in surface modification of nanoparticles for prolonging in vivo circulation. In this study, anti-solvent precipitation method was introduced to prepare gambogenic acid nanosuspensions (GNA-NS) with PVPK30 and PEG2000 as stabilizers to settle the disadvantages of GNA. The obtained nanoparticles were spherical with a mean particle size of 183.7 nm and a zeta potential of À22.8 mV.The entrapment efficiency and drug loading of the resultant formulation were 97.3 and 29.73%. X-ray diffraction analysis confirmed the amorphous phase of GNA in NS. Fourier transform infrared indicated there may be hydrogen bond interaction between the drug and excipients. After lyophilization of GNA-NS, the freeze-dried powder displayed sufficient longterm physical stability at 4 and 25 C. In comparison to GNA solution, in vitro studies of GNA-NS showed much slower release and higher cytotoxicity in HepG2 cells. What's more, the pharmacokinetic study in rats revealed that the AUC 0-1 and t 1/2 of GNA-NS were increased 2.63-and 1.77-fold than that of the reference formulation. Taken together, in vitro/in vivo evaluations showed NS would be an effectively strategy to change the poor aqueous solubility and prolong the half-life for GNA. The GNA-NS with enhanced bioavailability and drug efficacy provided a promising delivery system for the application of GNA. KeywordsCytotoxicity, gambogenic acid, in vivo pharmacokinetics, in vitro release, nanosuspensions History

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“…Besides these, it undergoes rapid first-pass metabolism by CYP3A4 in the liver and suffers enterohepatic recirculation, eventually leading to a marked reduction in the drug's oral bioavailable fraction (almost zero) in humans and animals like rats, etc. (Amri et al 2012, Marier et al 2002, Singh and Pai 2014a, 2014b.…”

Section: Introductionmentioning

confidence: 99%

“…All these formulations were able to increase the solubility and/or dissolution performance only. We recently reported the use of PLGA nanoparticles for improvement in absorption and subsequent oral bioavailability of t-RVT (Singh and Pai 2014a). Amri et al (2013) reported the self-emulsifying resveratrol drug delivery system, wherein they were able to achieve both the uptake by endothelial cells and improved protection against oxidative stress-mediated death.…”

Section: Introductionmentioning

confidence: 99%

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

Singh

Pai

2014

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

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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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Optimized PLGA nanoparticle platform for orally dosedtrans-resveratrol with enhanced bioavailability potential

Abstract: The studies, therefore, could provide another useful tool for successful development of t-RVT NPs and an in vivo approach to designate nanoparticulate system of t-RVT with distinctly improved bioavailability and to overcome enterohepatic recirculation.

Cited by 103 publications

References 35 publications

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

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

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Optimized PLGA nanoparticle platform for orally dosedtrans-resveratrol with enhanced bioavailability potential

Abstract: The studies, therefore, could provide another useful tool for successful development of t-RVT NPs and an in vivo approach to designate nanoparticulate system of t-RVT with distinctly improved bioavailability and to overcome enterohepatic recirculation.

Cited by 103 publications

References 35 publications

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson&rsquo;s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson&rsquo;s disease models

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

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

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Product

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Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models