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Mendeley readers
Attention Score in Context
| Title |
Encapsulation of the HSP-90 Chaperone Inhibitor 17-AAG in Stable Liposome Allow Increasing the Therapeutic Index as Assessed, in vitro, on Leishmania (L) amazonensis Amastigotes-Hosted in Mouse CBA Macrophages
|
|---|---|
| Published in |
Frontiers in Cellular and Infection Microbiology, August 2018
|
| DOI | 10.3389/fcimb.2018.00303 |
| Pubmed ID | |
| Authors |
Antonio Luis de Oliveira Almeida Petersen, Thiers A. Campos, Diana Angélica dos Santos Dantas, Juliana de Souza Rebouças, Juliana Cruz da Silva, Juliana P. B. de Menezes, Fábio R. Formiga, Janaina V. de Melo, Giovanna Machado, Patrícia S. T. Veras |
| Abstract |
The current long-term treatment for leishmaniasis causes severe side effects and resistance in some cases. An evaluation of the anti-leishmanial potential of an HSP90-inhibitor, 17-allylamino-17-demethoxygeldanamycin (17-AAG), demonstrated its potent effect against Leishmania spp. in vitro and in vivo. We have previously shown that 17-AAG can kill L. (L) amazonensis promastigotes with an IC50 of 65 nM and intracellular amastigote at concentrations as low as 125 nM. As this compound presents low solubility and high toxicity in human clinical trials, we prepared an inclusion complex containing hydroxypropyl-β-cyclodextrin and 17-AAG (17-AAG:HPβCD) to improve its solubility. This complex was characterized by scanning electron microscopy, and X-ray diffraction. Liposomes-containing 17-AAG:HPβCD was prepared and evaluated for encapsulation efficiency (EE%), particle size, polydispersity index (PDI), pH, and zeta potential, before and after accelerated and long-term stability testing. An evaluation of leishmanicidal activity against promastigotes and intracellular amastigotes of L. (L) amazonensis was also performed. The characterization techniques utilized confirmed the formation of the inclusion complex, HPβCD:17-AAG, with a resulting 33-fold-enhancement in compound water solubility. Stability studies revealed that 17-AAG:HPβCD-loaded liposomes were smaller than 200 nm, with 99% EE. Stability testing detected no alterations in PDI that was 0.295, pH 7.63, and zeta potential +22.6, suggesting liposome stability, and suitability for evaluating leishmanicidal activity. Treatment of infected macrophages with 0.006 nM of 17-AAG:HPβCD or 17-AAG:HPβCD-loaded liposomes resulted in almost complete amastigote clearance inside macrophages after 48 h. This reduction is similar to the one observed in infected macrophages treated with 2 μM amphotericin B. Our results showed that nanotechnology and drug delivery systems could be used to increase the antileishmanial efficacy and potency of 17-AAG in vitro, while also resulting in reduced toxicity that indicates these formulations may represent a potential therapeutic strategy against leishmaniasis. |
X Demographics
The data shown below were collected from the profiles of 2 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Switzerland | 1 | 50% |
| Unknown | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 2 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 45 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 45 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 10 | 22% |
| Student > Bachelor | 7 | 16% |
| Student > Master | 5 | 11% |
| Researcher | 4 | 9% |
| Student > Doctoral Student | 2 | 4% |
| Other | 3 | 7% |
| Unknown | 14 | 31% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 6 | 13% |
| Pharmacology, Toxicology and Pharmaceutical Science | 5 | 11% |
| Agricultural and Biological Sciences | 4 | 9% |
| Biochemistry, Genetics and Molecular Biology | 3 | 7% |
| Medicine and Dentistry | 3 | 7% |
| Other | 6 | 13% |
| Unknown | 18 | 40% |
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 01 September 2019.
All research outputs
#18,648,325
of 23,102,082 outputs
Outputs from Frontiers in Cellular and Infection Microbiology
#4,963
of 6,567 outputs
Outputs of similar age
#257,143
of 334,790 outputs
Outputs of similar age from Frontiers in Cellular and Infection Microbiology
#72
of 95 outputs
Altmetric has tracked 23,102,082 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,567 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 5.5. This one is in the 6th percentile – i.e., 6% of its peers scored the same or lower than it.
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We're also able to compare this research output to 95 others from the same source and published within six weeks on either side of this one. This one is in the 3rd percentile – i.e., 3% of its contemporaries scored the same or lower than it.