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Lipid-core nanocapsules increase the oral efficacy of quercetin in cutaneous leishmaniasis

Published online by Cambridge University Press:  27 June 2017

A. J. SOUSA-BATISTA ,
F. S. POLETTO ,
C. I. M. S. PHILIPON ,
S. S. GUTERRES ,
A. R. POHLMANN  and
B. ROSSI-BERGMANN
A. J. SOUSA-BATISTA
Affiliation:
Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Av Carlos Chagas Filho 373, 21941-901 Rio de Janeiro, RJ, Brazil
F. S. POLETTO
Affiliation:
Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves 9500, 91501-970 Porto Alegre, RS, Brazil
C. I. M. S. PHILIPON
Affiliation:
Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Av Carlos Chagas Filho 373, 21941-901 Rio de Janeiro, RJ, Brazil
S. S. GUTERRES
Affiliation:
Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, 90610-000 Porto Alegre, RS, Brazil
A. R. POHLMANN
Affiliation:
Instituto de Química, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves 9500, 91501-970 Porto Alegre, RS, Brazil
B. ROSSI-BERGMANN*
Affiliation:
Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Av Carlos Chagas Filho 373, 21941-901 Rio de Janeiro, RJ, Brazil
*
*Corresponding author: Instituto de Biofísica Carlos Chagas Filho, Av Carlos Chagas Filho 373, 21·9410901 Rio de Janeiro, RJ, Brazil. E-mail: bartira@biof.ufrj.br
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Summary

New oral treatments are needed for all forms of leishmaniasis. Here, the improved oral efficacy of quercetin (Qc) and its penta-acetylated derivative (PQc) was evaluated in cutaneous leishmaniasis after encapsulation in lipid-core nanocapsules (LNCs) of poly(ε-caprolactone). Leishmania amazonensis-infected BALB/c mice were given 51 daily oral doses of free drugs (16 mg kg−1) or LNC-loaded drugs (0·4 mg kg−1). While treatment with free Qc reduced the lesion sizes and parasite loads by 38 and 71%, respectively, LNC-Qc produced 64 and 91% reduction, respectively. The antileishmanial efficacy of PQc was similar but not as potently improved by encapsulation as Qc. None of the treatments increased aspartate aminotransferase, alanine aminotransferase or creatinine serum levels. These findings indicate that when encapsulated in LNC, Qc and, to a lesser extent, PQc can safely produce an enhanced antileishmanial effect even at a 40-fold lower dose, with implications for the development of a new oral drug for cutaneous leishmaniasis.

Keywords

leishmaniachemotherapyLNCdrug deliverynanoparticlenanotechnology
Type
Research Article
Information
Parasitology , Volume 144 , Issue 13 , November 2017 , pp. 1769 - 1774
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Copyright
Copyright © Cambridge University Press 2017 

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