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Intranasal agomelatine solid lipid nanoparticles to enhance brain delivery: formulation, optimization and in vivo pharmacokinetics

Overview of attention for article published in Drug Design, Development and Therapy, June 2017
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1 tweeter

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76 Mendeley
Title
Intranasal agomelatine solid lipid nanoparticles to enhance brain delivery: formulation, optimization and in vivo pharmacokinetics
Published in
Drug Design, Development and Therapy, June 2017
DOI 10.2147/dddt.s102500
Pubmed ID
Authors

Ahmed Fatouh, Ahmed Elshafeey, Ahmed Abdelbary

Abstract

Agomelatine is a novel antidepressant drug suffering from an extensive first-pass metabolism leading to a diminished absolute bioavailability. The aim of the study is: first to enhance its absolute bioavailability, and second to increase its brain delivery. To achieve these aims, the nasal route was adopted to exploit first its avoidance of the hepatic first-pass metabolism to increase the absolute bioavailability, and second the direct nose-to-brain pathway to enhance the brain drug delivery. Solid lipid nanoparticles were selected as a drug delivery system to enhance agomelatine permeability across the blood-brain barrier and therefore its brain delivery. The optimum solid lipid nanoparticles have a particle size of 167.70 nm ±0.42, zeta potential of -17.90 mV ±2.70, polydispersity index of 0.12±0.10, entrapment efficiency % of 91.25%±1.70%, the percentage released after 1 h of 35.40%±1.13% and the percentage released after 8 h of 80.87%±5.16%. The pharmacokinetic study of the optimized solid lipid nanoparticles revealed a significant increase in each of the plasma peak concentration, the AUC(0-360 min) and the absolute bioavailability compared to that of the oral suspension of Valdoxan(®) with the values of 759.00 ng/mL, 7,805.69 ng⋅min/mL and 44.44%, respectively. The optimized solid lipid nanoparticles gave a drug-targeting efficiency of 190.02, which revealed more successful brain targeting by the intranasal route compared with the intravenous route. The optimized solid lipid nanoparticles had a direct transport percentage of 47.37, which indicates a significant contribution of the direct nose-to-brain pathway in the brain drug delivery. The intranasal administration of agomelatine solid lipid nanoparticles has effectively enhanced both the absolute bioavailability and the brain delivery of agomelatine.

Twitter Demographics

The data shown below were collected from the profile of 1 tweeter who shared this research output. Click here to find out more about how the information was compiled.

Mendeley readers

The data shown below were compiled from readership statistics for 76 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 76 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 24 32%
Researcher 11 14%
Student > Ph. D. Student 8 11%
Student > Bachelor 4 5%
Student > Postgraduate 2 3%
Other 7 9%
Unknown 20 26%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 25 33%
Biochemistry, Genetics and Molecular Biology 5 7%
Engineering 4 5%
Agricultural and Biological Sciences 4 5%
Chemistry 3 4%
Other 8 11%
Unknown 27 36%

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 09 July 2017.
All research outputs
#10,152,515
of 11,442,641 outputs
Outputs from Drug Design, Development and Therapy
#846
of 1,202 outputs
Outputs of similar age
#218,116
of 259,756 outputs
Outputs of similar age from Drug Design, Development and Therapy
#26
of 31 outputs
Altmetric has tracked 11,442,641 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,202 research outputs from this source. They receive a mean Attention Score of 3.8. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 259,756 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 31 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.