Nitazoxanide in the treatment of chronic cutaneous leishmaniasis resistant to traditional sodium stibogluconate

Gurgen, Johnny; Hogan, Daniel J.; Grace, Edward G.; Johnson, David

doi:10.1016/j.jaad.2009.06.044

Cited by 8 publications

(4 citation statements)

References 5 publications

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“…Sodium stibogluconate was the most effective treatment and achieved the most rapid relief. However, SSG is expensive (US$160 per 100 ml) and its supply is interrupted, and moreover SSG resistance is emerging in Sri Lanka . In the present study, SSG was found to have a 4% failure rate.…”

Section: Discussionmentioning

confidence: 50%

Randomized, double‐blind, controlled, comparative study on intralesional 10% and 15% hypertonic saline versus intralesional sodium stibogluconate in Leishmania donovani cutaneous leishmaniasis

Ranawaka¹,

Weerakoon²,

Silva

2015

Int J Dermatology

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This study found 10% HS to be an effective and safe alternative to SSG. Treatment with HS at concentrations of 15% or above was not safe as a result of cutaneous necrosis. Safety was not studied for concentrations of 11-14%, and these concentrations should be avoided pending further evidence. Hypertonic saline is very cheap (< US$1 per 100 ml, whereas SSG is priced at US$160 per 100 ml), is prepared locally and has no systemic side effects and minimal local side effects.

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Section: Discussionmentioning

confidence: 50%

Randomized, double‐blind, controlled, comparative study on intralesional 10% and 15% hypertonic saline versus intralesional sodium stibogluconate in Leishmania donovani cutaneous leishmaniasis

Ranawaka¹,

Weerakoon²,

Silva

2015

Int J Dermatology

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“…É bem tolerada, tem poucos efeitos colaterais e requer um curto período de tratamento. Não há contraindicações importantes, exceto hipersensibilidade prévia (Gurgen, Hogan, Grace, & Johnson, 2011). No entanto, ela requer monitoramento quando administrada concomitantemente com medicamentos como varfarina ou fenitoína e não há dados sobre a biodisponibilidade cutânea (Zhang et al, 2010).…”

Section: Nitazoxanida: Atividades Farmacológicasunclassified

Nitazoxanida: aspectos gerais, sistemas de liberação e potencial de reposicionamento da molécula

Lira

Sousa

Brito

et al. 2021

RSD

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A nitazoxanida (NTZ) é um fármaco empregado no tratamento de infecções virais e parasitárias devido ao seu mecanismo de ação ativar processos de morte celular. Entretanto, apresenta baixa biodisponibilidade oral, restringindo a sua utilização na terapêutica, com isso, novos sistemas de liberação são necessários para melhor absorção in vivo. O objetivo desta revisão narrativa foi abordar aspectos referentes a características físico-químicas da molécula de Nitazoxanida e seu potencial de reposicionamento. Foram realizadas buscas nas bases de dados Pubmed, Lilacs e Science Direct, selecionados artigos em inglês e português, cruzando os descritores “Nitazoxanida”, “caracterização” e “formulação” combinados entre si. Evidências científicas descrevem a NTZ como uma molécula de baixo peso molecular, melhor absorvida em pH ácido, que sofre desacetilação originando seu metabólito ativo, a Tizoxanida. Estudos relatam sua aplicação frequentemente em doenças por Giardia lamblia, Entamoeba histolytica e Cryptosporidium parvum, além de infecções por protozoários, helmintos, bactérias gram negativas e positivas e possuir propriedades antivirais, estando relacionado a sua descoberta recente na COVID-19, inclusive associada a outros fármacos. Assim, sistemas como lipossomas, nanopartículas, microesferas, comprimidos de liberação controlada foram relatados como potencializadores veículos na liberação do fármaco, além de possibilitar melhoria nos seus aspectos físico-químicos. Portanto, a NTZ representa uma molécula com grande potencial de aplicação e reposicionamento, abrangendo inúmeras possibilidades.

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“…The enzyme pyruvate kinase catalyses the glycolysis process which results in the production of adenosine triphosphate (ATP). By inhibiting ATP production, NTZ may have potential to inhibit the leishmanial parasites [15].…”

Section: Introductionmentioning

confidence: 99%

“…causing the pyruvate binding to the cofactor thiamine pyrophosphate in opposition to the binding with potential substrates in the cell [16]. Moreover, it has more specific activity for Leishmania as compared to the other second-line anti-parasitic agents being more specific for bacterial or fungal infections [15]. In a previous study, the in vivo results indicated that by giving NTZ orally at the dose of 400 mg kg −1 d −1 , the liver and splenic leishmanial parasitic load was reduced by more than 90% [17].…”

Section: Introductionmentioning

confidence: 99%

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

et al. 2022

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Topical delivery is preferable over systemic delivery for cutaneous leishmaniasis, because of its easy administration, reduced systemic adverse effects and low cost. Nitazoxanide (NTZ) has broad-spectrum activity against various parasites and has the potential to avoid drug resistance developed by enzymatic mutations. NTZ oral formulation is associated with severe dyspepsia and stomach pain. Herein, NTZ-transethosomes (NTZ-TES) were prepared and loaded into chitosan gel (NTZ-TEG) for topical delivery. NTZ-TES were prepared by the thin-film hydration method and optimized statistically via the Box-Behnken method. The optimized formulation indicated excellent particle size (176 nm), polydispersity index (0.093), zeta potential (−26.4 mV) and entrapment efficiency (86%). The transmission electron microscopy analysis showed spherical-sized particles and Fourier-transform infrared spectroscopy analysis indicated no interaction among the excipients. Similarly, NTZ-TEG showed optimal pH, desirable viscosity and good spreadability. NTZ-TES and NTZ-TEG showed prolonged release behaviour and higher skin penetration and deposition in the epidermal/dermal layer of skin in comparison with the NTZ-dispersion. Moreover, NTZ-TES showed higher percentage inhibition, lower half-maximal inhibitory concentration (IC 50 ) against promastigotes and higher macrophage uptake. Additionally, skin irritation and histopathology studies indicated the safe and non-irritant behaviour of the NTZ-TEG. The obtained findings suggested the enhanced skin permeation and improved anti-leishmanial effect of NTZ when administered as NTZ-TEG.

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Nitazoxanide in the treatment of chronic cutaneous leishmaniasis resistant to traditional sodium stibogluconate

Cited by 8 publications

References 5 publications

Randomized, double‐blind, controlled, comparative study on intralesional 10% and 15% hypertonic saline versus intralesional sodium stibogluconate in Leishmania donovani cutaneous leishmaniasis

Randomized, double‐blind, controlled, comparative study on intralesional 10% and 15% hypertonic saline versus intralesional sodium stibogluconate in Leishmania donovani cutaneous leishmaniasis

Nitazoxanida: aspectos gerais, sistemas de liberação e potencial de reposicionamento da molécula

Macrophage targeting of nitazoxanide-loaded transethosomal gel in cutaneous leishmaniasis

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