Polysorbate 80-coated PLGA nanoparticles improve the permeability of acetylpuerarin and enhance its brain-protective effects in rats

Sun, Deqing; Xue, Aiying; Zhang, Bin; Lou, Haiyan; Shi, Hui; Zhang, Xiumei

doi:10.1111/jphp.12481

Cited by 30 publications

(16 citation statements)

References 49 publications

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“…Besides, the measurement of PDI is employed to understand the range of droplet size in ME system, and its value closer to zero suggests greater uniformity of the formed dispersion. It has been reported that nanoscale-sized particles with homogeneous distribution can provide a large surface area, improve drug absorption (Mohsin et al., 2016), as well as making it easier to cross the BBB (Sun et al., 2015). Therefore, the optimized LME was a monodispersed system and appropriate for delivery.…”

Section: Discussionmentioning

confidence: 99%

Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution

et al. 2019

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Lycopene is considered as a promising neuroprotector with multiple bioactivities, while its therapeutic use in neurological disorders is restricted due to low solubility, instability and limited bioavailability. Our work aimed to develop lycopene-loaded microemulsion (LME) and investigate its potentials in improving bioavailability and brain-targeting efficiency following oral administration. The blank microemulsion (ME) excipients were selected based on orthogonal design and pseudo-ternary phase diagrams, and LME was prepared using the water titration method and characterized in terms of stability, droplet size distribution, zeta potential, shape and lycopene content. The optimized LME encompassed lycopene, (R)-(þ)-limonene, Tween 80, Transcutol HP and water and lycopene content was 463.03 ± 8.96 mg/mL. This novel formulation displayed transparent appearance and satisfactory physical and chemical stabilities. It was spherical and uniform in morphology with an average droplet size of 12.61 ± 0.46 nm and a polydispersity index (PDI) of 0.086 ± 0.028. The pharmacokinetics and tissue distributions of optimized LME were evaluated in rats and mice, respectively. The pharmacokinetic study revealed a dramatic 2.10-fold enhancement of relative bioavailability with LME against the control lycopene dissolved in olive oil (LOO) dosage form in rats. Moreover, LME showed a preferential targeting distribution of lycopene toward brain in mice, with the value of drug targeting index (DTI) up to 3.45. In conclusion, the optimized LME system demonstrated excellent physicochemical properties, enhanced oral bioavailability and superior brain-targeting capability. These findings provide a basis for the applications of ME-based strategy in brain-targeted delivery via oral route, especially for poorly water-soluble drugs.

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Section: Discussionmentioning

confidence: 99%

Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution

et al. 2019

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“…Thus, mitochondria do not normally produce and supply energy (ATP) . After destroying the cell wall, the nanoparticles could more readily enhance the cells penetration and the fungicides ability to act on the target site . Above all, pyraclostrobin formulations inhibited the growth of F. oxysporum to some extent, and the antifungal activity of the solid nanodispersion was greater than that of the traditional WDG formulation.…”

Section: Resultsmentioning

confidence: 99%

Preparation, characterization and antifungal activity of pyraclostrobin solid nanodispersion by self‐emulsifying technique

Wang

Guo

Yao

et al. 2019

Pest Management Science

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BACKGROUND Pathogenic fungi are the causal agents of 70–80% of plant diseases. Therefore, it is imperative to explore new and high effective fungicides. Constructing nanoscale fungicides using nanomaterial and nanotechnology has attracted wide attention in recent years. RESULTS In this research, a pyraclostrobin solid nanodispersion (PSND) was prepared using the self‐emulsifying method. The solid nanodispersion had a mean particle size of 20 nm and a zeta potential of ‐29.3 mV. The solubility and dissolution rate of the PSND increased owing to the decrease in particle size and the actions of the surfactants. The contact angle and retention volumes of the PSND on cucumber and cabbage leaf surfaces were greater than those of the commercial water dispersible granule. In addition, the median lethal concentration against Fusarium oxysporum was 0.7 43 µg mL−1. The toxicity of the nanoparticles was 4.5 times that of the water dispersible granule (WDG). The high fungicidal activity of PSND promoted the production of excess reactive oxygen species (ROS). The activity levels of the antioxidant enzymes containing superoxide dismutase (SOD) and catalase (CAT) decreased in F. oxysporum. CONCLUSION The research introduced a new method for preparing insoluble pyraclostrobin solid nanoformulation for fungicides to enhance the fungicidal activity and reduce environmental pollution. © 2019 Society of Chemical Industry

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“…In some studies it was proved that up to (2 % w/w) P80 concentration is effective or brain targeting of nanoparticles [83,84] . In most of the studies, for coating 1 % w/v of P80 was added to nanoparticle suspensions and incubated for 30 min with constant stirring and finally lyophilized [85,86] .…”

Section: Surfactant-based Approach To Prolong Brain Retention Of Polymentioning

confidence: 99%

Effect of Surfactant Coating on Brain Targeting Polymeric Nanoparticles; a Review

Chacko¹,

Palanisamy²,

Gowrishankar³

et al. 2018

pharmaceutical-sciences

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Chacko, et al.: Surfactant Coating on Brain Targeting NanoparticlesTargeting of drugs to brain is one of the most challenging issues for pharmaceutical research as bloodbrain barrier acts as an insurmountable obstacle for the passage of systemically delivered therapeutics and the brain extracellular matrix attributes to poor distribution of locally delivered drugs. Amongst various invasive or non-invasive methods to warrant blood-brain barrier, nanoparticle is one of promising ways to administer central nervous system drugs. The concept of nanoparticle-based drug targeting make a tremendous progress and gigantic era to overcome the above limitations with improved drug efficacy and reduced drug toxicity. In recent years, new strategies of surfactant coating of biodegradable polymeric nanoparticles, which differ from conventional methodologies of brain targeting, have emerged at the forefront of medical science. The non-ionic surfactant, polysorbate 80 as a coating material promises an unparalleled opportunity for enhancement of brain targeting of colloidal particles. The aim of this review is to evaluate the potential application of surfactant-coated nanoparticles as drug carrier system for various central nervous system diseases.

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Polysorbate 80-coated PLGA nanoparticles improve the permeability of acetylpuerarin and enhance its brain-protective effects in rats

Abstract: Polysorbate 80-coated PLGA-NPs can improve the permeability of AP cross the BBB and enhance its brain-protective effects in rats.

Cited by 30 publications

References 49 publications

Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution

Oral delivery of lycopene-loaded microemulsion for brain-targeting: preparation, characterization, pharmacokinetic evaluation and tissue distribution

Preparation, characterization and antifungal activity of pyraclostrobin solid nanodispersion by self‐emulsifying technique

Effect of Surfactant Coating on Brain Targeting Polymeric Nanoparticles; a Review

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