| Title |
Polarity-sensitive nanocarrier for oral delivery of Sb(V) and treatment of cutaneous leishmaniasis
|
|---|---|
| Published in |
International Journal of Nanomedicine, May 2016
|
| DOI | 10.2147/ijn.s105952 |
| Pubmed ID | |
| Authors |
Juliane S Lanza, Flaviana R Fernandes, José D Corrêa-Júnior, José MC Vilela, Rogério Magalhães-Paniago, Lucas AM Ferreira, Margareth S Andrade, Cynthia Demicheli, Maria N Melo, Frédéric Frézard |
| Abstract |
There is a great need for orally active drugs for the treatment of the neglected tropical disease leishmaniasis. Amphiphilic Sb(V) complexes, such as 1:3 Sb-N-octanoyl-N-methylglucamide complex (SbL8), are promising drug candidates. It has been previously reported that SbL8 forms kinetically stabilized nanoassemblies in water and that this simple dispersion exhibits antileishmanial activity when given by oral route to a murine model of visceral leishmaniasis. The main objective of the present work was to interfere in the structural organization of these nanoassemblies so as to investigate their influence on the oral bioavailability of Sb, and ultimately, optimize an oral formulation of SbL8 for the treatment of cutaneous leishmaniasis. The structural organization of SbL8 nanoassemblies was manipulated through addition of propylene glycol (PG) to the aqueous dispersion of SbL8. The presence of 50% (v/v) PG resulted in the loss of hydrophobic microenvironment, as evidenced by fluorescence probing. However, nanostructures were still present, as demonstrated by dynamic light scattering, small-angle X-ray scattering, and atomic force microscopy (AFM). A remarkable property of these nanoassemblies, as revealed by AFM analysis, is the flexibility of their supramolecular organization, which showed changes as a function of the solvent and substrate polarities. The formulation of SbL8 in 1:1 water:PG given orally to mice promoted significantly higher and more sustained serum levels of Sb, when compared to SbL8 in water. The new formulation, when given as repeated doses (200 mg Sb/kg/day) to BALB/c mice infected with Leishmania amazonensis, was significantly more effective in reducing the lesion parasite burden, compared to SbL8 in water, and even, the conventional drug Glucantime(®) given intraperitoneally at the same dose. In conclusion, this work introduces a new concept of polarity-sensitive nanocarrier that was successfully applied to optimize an oral formulation of Sb(V) for treating cutaneous leishmaniasis. |
X Demographics
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Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 2 | 100% |
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 % |
|---|---|---|
| Brazil | 1 | 2% |
| Unknown | 44 | 98% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Researcher | 6 | 13% |
| Student > Ph. D. Student | 5 | 11% |
| Student > Master | 4 | 9% |
| Student > Bachelor | 3 | 7% |
| Student > Doctoral Student | 3 | 7% |
| Other | 7 | 16% |
| Unknown | 17 | 38% |
| Readers by discipline | Count | As % |
|---|---|---|
| Pharmacology, Toxicology and Pharmaceutical Science | 7 | 16% |
| Immunology and Microbiology | 6 | 13% |
| Veterinary Science and Veterinary Medicine | 3 | 7% |
| Medicine and Dentistry | 3 | 7% |
| Agricultural and Biological Sciences | 3 | 7% |
| Other | 6 | 13% |
| Unknown | 17 | 38% |
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 17 June 2016.
All research outputs
#19,944,091
of 25,373,627 outputs
Outputs from International Journal of Nanomedicine
#2,971
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#217,274
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Outputs of similar age from International Journal of Nanomedicine
#110
of 120 outputs
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