↓ Skip to main content

Dove Medical Press

Paracellular permeation-enhancing effect of AT1002 C-terminal amidation in nasal delivery

Overview of attention for article published in Drug Design, Development and Therapy, March 2015
Altmetric Badge

About this Attention Score

  • In the top 25% of all research outputs scored by Altmetric
  • High Attention Score compared to outputs of the same age (82nd percentile)
  • High Attention Score compared to outputs of the same age and source (81st percentile)

Mentioned by

patent
3 patents

Citations

dimensions_citation
13 Dimensions

Readers on

mendeley
21 Mendeley
Title
Paracellular permeation-enhancing effect of AT1002 C-terminal amidation in nasal delivery
Published in
Drug Design, Development and Therapy, March 2015
DOI 10.2147/dddt.s79383
Pubmed ID
Authors

Keon-Hyoung Song, Sang-Bum Kim, Chang-Koo Shim, Suk-Jae Chung, Dae-Duk Kim, Sang-Ki Rhee, Guang J Choi, Chul-Hyun Kim, Kiyoung Kim

Abstract

The identification of permeation enhancers has gained interest in the development of drug delivery systems. A six-mer peptide, H-FCIGRL-OH (AT1002), is a tight junction modulator with promising permeation-enhancing activity. AT1002 enhances the transport of molecular weight markers or agents with low bioavailability with no cytotoxicity. However, AT1002 is not stable in neutral pH or after incubation under physiological conditions, which is necessary to fully uncover its permeation-enhancing effect. Thus, we increased the stability or mitigated the instability of AT1002 by modifying its terminal amino acids and evaluated its subsequent biological activity. C-terminal-amidated (FCIGRL-NH2, Pep1) and N-terminal-acetylated (Ac-FCIGRL, Pep2) peptides were analyzed by liquid chromatography-mass spectrometry. We further assessed cytotoxicity on cell monolayers, as well as the permeation-enhancing activity following nasal administration of the paracellular marker mannitol. Pep1 was nontoxic to cell monolayers and showed a relatively low decrease in peak area compared to AT1002. In addition, administration of mannitol with Pep1 resulted in significant increases in the area under the plasma concentration-time curve and peak plasma concentration at 3.63-fold and 2.68-fold, respectively, compared to mannitol alone. In contrast, no increase in mannitol concentration was shown with mannitol/AT1002 or mannitol/Pep2 compared to the control. Thus, Pep1 increased the stability or possibly reduced the instability of AT1002, which resulted in an increased permeation-enhancing effect of AT1002. These results suggest the potential usefulness of C-terminal-amidated AT1002 in enhancing nasal drug delivery, which may lead to the development of a practical drug delivery technology for drugs with low bioavailability.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 21 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 21 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 5 24%
Student > Master 3 14%
Professor 3 14%
Student > Bachelor 2 10%
Student > Doctoral Student 1 5%
Other 3 14%
Unknown 4 19%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 6 29%
Chemistry 3 14%
Agricultural and Biological Sciences 2 10%
Psychology 1 5%
Materials Science 1 5%
Other 1 5%
Unknown 7 33%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 9. 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 07 May 2020.
All research outputs
#3,838,613
of 25,576,801 outputs
Outputs from Drug Design, Development and Therapy
#252
of 2,254 outputs
Outputs of similar age
#46,276
of 271,477 outputs
Outputs of similar age from Drug Design, Development and Therapy
#13
of 70 outputs
Altmetric has tracked 25,576,801 research outputs across all sources so far. Compared to these this one has done well and is in the 83rd percentile: it's in the top 25% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 2,254 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.3. This one has done well, scoring higher than 88% 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 271,477 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 82% of its contemporaries.
We're also able to compare this research output to 70 others from the same source and published within six weeks on either side of this one. This one has done well, scoring higher than 81% of its contemporaries.