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Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge 

Overview of attention for article published in International Journal of Nanomedicine, July 2015
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Citations

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129 Mendeley
Title
Niosomal carriers enhance oral bioavailability of carvedilol: effects of bile salt-enriched vesicles and carrier surface charge 
Published in
International Journal of Nanomedicine, July 2015
DOI 10.2147/ijn.s84703
Pubmed ID
Authors

Simin Dadashzadeh, Azadeh Haeri, Marjan Daeihamed, Gelareh Arzani, Hamid Bakhtiari Kaboutaraki

Abstract

Carvedilol (CRV) is an antihypertensive drug with both alpha and beta receptor blocking activity used to preclude angina and cardiac arrhythmias. To overcome the low, variable oral bioavailability of CRV, niosomal formulations were prepared and characterized: plain niosomes (without bile salts), bile salt-enriched niosomes (bilosomes containing various percentages of sodium cholate or sodium taurocholate), and charged niosomes (negative, containing dicetyl phosphate and positive, containing hexadecyl trimethyl ammonium bromide). All formulations were characterized in terms of encapsulation efficiency, size, zeta potential, release profile, stability, and morphology. Various formulations were administered orally to ten groups of Wistar rats (n=6 per group). The plasma levels of CRV were measured by a validated high-performance liquid chromatography (HPLC) method and pharmacokinetic properties of different formulations were characterized. Contribution of lymphatic transport to the oral bioavailability of niosomes was also investigated using a chylomicron flow-blocking approach. Of the bile salt-enriched vesicles examined, bilosomes containing 20% sodium cholate (F2) and 30% sodium taurocholate (F5) appeared to give the greatest enhancement of intestinal absorption. The relative bioavailability of F2 and F5 formulations to the suspension was estimated to be 1.84 and 1.64, respectively. With regard to charged niosomes, the peak plasma concentrations (Cmax) of CRV for positively (F7) and negatively charged formulations (F10) were approximately 2.3- and 1.7-fold higher than after a suspension. Bioavailability studies also revealed a significant increase in extent of drug absorption from charged vesicles. Tissue histology revealed no signs of inflammation or damage. The study proved that the type and concentration of bile salts as well as carrier surface charge had great influences on oral bioavailability of niosomes. Blocking the lymphatic absorption pathway significantly reduced oral bioavailability of CRV niosomes. Overall twofold enhancement in bioavailability in comparison with drug suspension confers the potential of niosomes as suitable carriers for improved oral delivery of CRV.

Mendeley readers

The data shown below were compiled from readership statistics for 129 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
United Kingdom 1 <1%
India 1 <1%
Unknown 127 98%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 19 15%
Student > Master 19 15%
Professor > Associate Professor 12 9%
Student > Doctoral Student 8 6%
Student > Bachelor 8 6%
Other 28 22%
Unknown 35 27%
Readers by discipline Count As %
Pharmacology, Toxicology and Pharmaceutical Science 38 29%
Agricultural and Biological Sciences 10 8%
Medicine and Dentistry 10 8%
Biochemistry, Genetics and Molecular Biology 5 4%
Chemistry 4 3%
Other 16 12%
Unknown 46 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 30 July 2015.
All research outputs
#15,340,815
of 22,818,766 outputs
Outputs from International Journal of Nanomedicine
#2,236
of 3,816 outputs
Outputs of similar age
#153,934
of 263,416 outputs
Outputs of similar age from International Journal of Nanomedicine
#85
of 124 outputs
Altmetric has tracked 22,818,766 research outputs across all sources so far. This one is in the 22nd percentile – i.e., 22% of other outputs scored the same or lower than it.
So far Altmetric has tracked 3,816 research outputs from this source. They receive a mean Attention Score of 4.3. This one is in the 28th percentile – i.e., 28% 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 263,416 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 32nd percentile – i.e., 32% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 124 others from the same source and published within six weeks on either side of this one. This one is in the 19th percentile – i.e., 19% of its contemporaries scored the same or lower than it.