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Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery

Overview of attention for article published in AAPS PharmSciTech, November 2014
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  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (80th percentile)
  • Good Attention Score compared to outputs of the same age and source (72nd percentile)

Mentioned by

news
1 news outlet

Citations

dimensions_citation
3 Dimensions

Readers on

mendeley
7 Mendeley
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Title
Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery
Published in
AAPS PharmSciTech, November 2014
DOI 10.1208/s12249-014-0240-6
Pubmed ID
Authors

Vijay Pawar, Rushabh Thosani, Ashish Kanhed, Rajani Giridhar, Mange Ram Yadav

Abstract

Piperazinylalkyl ester prodrugs (4a-5d) of 6-methoxy-2-naphthylacetic acid (6-MNA) (1) were synthesized and evaluated in vitro for the purpose of percutaneous drug delivery. These ionizable prodrugs exhibited varying aqueous solubilities and lipophilicities depending on the pH of the medium. The prodrugs (4a-5c) showed higher aqueous solubility and similar lipophilicity at pH 5.0 and lower aqueous solubility and higher lipophilicity at pH 7.4 in comparison to 6-MNA. The chemical and enzymatic hydrolyses of the prodrugs was investigated in aqueous buffer solutions (pH 5.0 and 7.4) and in 80% human serum (pH 7.4) at 37°C. The prodrugs showed moderate chemical stability (t 1/2 = 6-60 h) but got readily hydrolyzed enzymatically to 6-MNA with half-life ranging from 10-60 min. In the in vitro permeation study using rat skin, the flux of 6-MNA and the prodrugs was determined in aqueous buffers of pH 5.0 and 7.4. The prodrug (5b) showed 7.9- and 11.2-fold enhancement in skin permeation compared to 6-MNA (1) at pH 5.0 and 7.4, respectively. It was concluded that the parent NSAIDs having favorable pharmacokinetic and pharmacodynamic properties coupled with increased skin permeability of their prodrugs could give better options for the treatment of rheumatic diseases.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 7 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 7 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 3 43%
Student > Ph. D. Student 1 14%
Student > Master 1 14%
Unknown 2 29%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 2 29%
Agricultural and Biological Sciences 1 14%
Chemistry 1 14%
Medicine and Dentistry 1 14%
Unknown 2 29%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 7. 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 06 November 2014.
All research outputs
#4,167,289
of 22,769,322 outputs
Outputs from AAPS PharmSciTech
#156
of 1,468 outputs
Outputs of similar age
#49,174
of 262,797 outputs
Outputs of similar age from AAPS PharmSciTech
#3
of 18 outputs
Altmetric has tracked 22,769,322 research outputs across all sources so far. Compared to these this one has done well and is in the 80th percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 1,468 research outputs from this source. They receive a mean Attention Score of 4.0. This one has done well, scoring higher than 86% of its peers.
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 262,797 tracked outputs that were published within six weeks on either side of this one in any source. This one has done well, scoring higher than 80% of its contemporaries.
We're also able to compare this research output to 18 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 72% of its contemporaries.