Inefficacy of the association N-methyl glucamine and topical miltefosine in the treatment of experimental cutaneous leishmaniasis by Leishmania (Leishmania) amazonensis

Sampaio, Raimunda Nonata Ribeiro; Lucas, Íris Campos; Takami, Hitoshi

doi:10.1590/s1678-91992007000300004

Cited by 5 publications

(5 citation statements)

References 25 publications

(22 reference statements)

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“…In recent years, various topical formulations containing paromomycin, pentavalent antimonials, β-lapachone and amphotericin B have been developed for CL treatment [4][5][6]29 , but none were sufficiently effective or safe for clinical approval. Here, we evaluated the efficacy of a new topical nanoformulation against CL that combined the potency of a promising antileishmanial compound the nitro-chalcone CH8 11 -with the skin permeation ability of the versatile LNC 30 .…”

Section: Discussionmentioning

confidence: 99%

“…To circumvent these difficulties, an effective topical treatment is the obvious choice for CL. However, creams containing paromomycin, miltefosine and amphotericin B have shown partial or no efficacy against CL, in particularly against New World Leishmania species [4][5][6] . Failure of topical formulations is typically linked to poor skin permeation, mainly to high drug molecular size and/or inappropriate lipophilicity 7 .…”

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confidence: 99%

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Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8

Escrivani

Lopes

Poletto

et al. 2020

Nanomedicine: Nanotechnology, Biology and Medicine

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Peer-review status of attached le: eerEreviewed Citation for published item: isrivniD hougls y nd vopesD wilene l¡ eri nd olettoD pernnd nd perrriniD tel egin nd ousEftistD erine tF nd teelD trik qF nd quterresD ¡ %lvi tnis uski nd ohlmnnD edrin 0n nd ossiEfergmnnD frtir @PHPHA 9inpsultion in lipidEore nnopsules improves topil tretment with the potent ntileishmnil ompound grVF9D xnomediine X nnotehnologyD iology nd mediineFD PR F pF IHPIPIF

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Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8

Escrivani

Lopes

Poletto

et al. 2020

Nanomedicine: Nanotechnology, Biology and Medicine

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“…10 Therefore, current opinions agree that the topical treatment of CL has not reached optimal effectiveness. 11 Meanwhile, chalcones and their derivatives have been investigated as potential drug candidates for Leishmaniasis treatment, since their antileishmanial activity has been demonstrated by different authors.…”

Section: Mattos Et Almentioning

confidence: 99%

Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design

Mattos¹,

Argenta²,

Melchiades³

et al. 2015

IJN

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Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 2 2 full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant – soybean lecithin or sorbitan monooleate and type of co-surfactants – polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin. In order to evaluate the stability of the systems, the antileishmanial assay was performed against Leishmania amazonensis 24 hours and 60 days after the preparation of the nanoemulsions. The formulation composed of soybean lecithin and polysorbate 20 presented suitable physicochemical characteristics (droplet size 171.9 nm; polydispersity index 0.14; zeta potential −39.43 mV; pH 5.16; and viscosity 2.00 cP), drug content (91.09%) and the highest retention in dermis (3.03 µg·g −1 ) – the main response of interest – confirmed by confocal microscopy. This formulation also presented better stability of leishmanicidal activity in vitro against L . amazonensis amastigote forms (half maximal inhibitory concentration value 0.32±0.05 µM), which confirmed the potential of the nanoemulsion soybean lecithin and polysorbate 20 for CL treatment.

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“…The infection triggers a cluster of clinical manifestations that can lead to death, if the patient is not treated. The toxicity of drugs, the difficulties of administration and the duration of treatment, allied with their low efficacy for humans and practical inefficacy for other animals, has stimulated the research of new natural leishmanicidal compounds, such as those derived from animal venoms [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

In vitro activity of phospholipase A2 and of peptides from Crotalus durissus terrificus venom against amastigote and promastigote forms of Leishmania (L.) infantum chagasi

Barros¹,

Pereira²,

Barros³

et al. 2015

J Venom Anim Toxins Incl Trop Dis

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BackgroundAmerican visceral leishmaniasis is caused by the intracellular parasite Leishmania (L.) infantum chagasi, and transmitted by the sand fly Lutzomyia longipalpis. Since treatment is based on classical chemotherapeutics with significant side effects, the search for new drugs remains the greatest global challenge. Thus, this in vitro study aimed to evaluate the leishmanicidal effect of Crotalus durissus terrificus venom fractions on promastigote and amastigote forms of Leishmania (L.) infantum chagasi.MethodsPhospholipase A2 (PLA2) and a pool of peptide fraction (<3 kDa) were purified from Crotalus venom. Furthermore, promastigotes and peritoneal macrophages of mice infected by amastigotes were exposed to serial dilutions of the PLA2 and peptides at intervals varying between 1.5625 μg/mL and 200 μg/mL. Both showed activity against promastigotes that varied according to the tested concentration and the time of incubation (24, 48 and 72 h).ResultsMTT assay for promastigotes showed IC50 of 52.07 μg/mL for PLA2 and 16.98 μg/mL for the peptide fraction of the venom. The cytotoxicity assessment in peritoneal macrophages showed IC50 of 98 μg/mL and 16.98 μg/mL for PLA2 and peptide by MTT assay, respectively. In peritoneal macrophages infected by Leishmania (L.) infantum chagasi amastigotes, the PLA2 stimulated growth of parasites, and at higher doses reduced growth by 23 %. The peptide fraction prevented 43 % of the intracellular parasite growth at a dose of 16.98 μg/mL, demonstrating the toxicity of this dose to macrophages. Both fractions stimulated H2O2 production by macrophages but only PLA2 was able to stimulate NO production.ConclusionWe have demonstrated the in vitro leishmanicidal activity of the PLA2 and peptide fraction of Crotalus venom. The results encourage further studies to describe the metabolic pathways involved in cell death, as well as the prospecting of molecules with antiparasitic activity present in the peptide fraction of Crotalus durissus terrificus venom.

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Inefficacy of the association N-methyl glucamine and topical miltefosine in the treatment of experimental cutaneous leishmaniasis by Leishmania (Leishmania) amazonensis

Cited by 5 publications

References 25 publications

Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8

Encapsulation in lipid-core nanocapsules improves topical treatment with the potent antileishmanial compound CH8

Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design

In vitro activity of phospholipase A2 and of peptides from Crotalus durissus terrificus venom against amastigote and promastigote forms of Leishmania (L.) infantum chagasi

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