Nanostructures for Improved Antimonial Therapy of Leishmaniasis

Frézard, Frédéric; Demicheli, Cynthia; Silva, Sydnei M. Da; Azevedo, Erly G.; Ribeiro, Raul Rio

doi:10.1016/b978-0-323-52727-9.00022-4

Cited by 7 publications

(8 citation statements)

References 112 publications

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“…The mechanism of action of pentavalent antimonials has remained essentially unknown. Evidence suggests that pentavalent antimony Sb(V) is a prodrug which is reduced in vivo into trivalent antimony Sb(III) [63,64]. Sb(III) is the active/toxic form that exhibits antileishmanial activity.…”

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

“…The reduction of Sb(V) to Sb(III) is favored by slightly elevated temperature and acidic pH. This suggests that Sb(V) drugs may act as a molecular carrier releasing the active Sb(III) form in the acidic intracellular compartments where the Leishmania parasites reside [64,65]. The antileishmanial activity of Sb(III) involves multiple pathways, such as: interaction with thiol metabolism of parasites resulting in deoxyribonucleic acid (DNA) fragmentation; inhibition of Leishmania type I DNA topoisomerase which promote adenosine triphosphate (ATP) and guanosine triphosphate (GTP) depletion resulting in the reduction or depletion of parasites energy; promotion the production of proinflammatory cytokines that can increase the release of reactive oxygen species [63].…”

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

“…Even though pentavalent antimonial drugs are still the first-line medication in several developing countries, they have several limitations due to the toxicity of Sb(III) [64]. These drugs require daily parenteral administration which causes local pain.…”

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

“…Systemic side effects such as hepatotoxicity, nephrotoxicity, pancreatitis, cardiac toxicity, myalgia, abdominal colic, nausea, vomiting, diarrhea are common during treatment [63,64]. In addition, the development of drug resistance decreases the effectiveness of these compounds [63,64,65]. The use of pentamidine is limited due to toxicity and drug resistance [47].…”

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

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Future Prospects in the Treatment of Parasitic Diseases: 2-Amino-1,3,4-Thiadiazoles in Leishmaniasis

Şerban

2019

Molecules

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Neglected tropical diseases affect the lives of a billion people worldwide. Among them, the parasitic infections caused by protozoan parasites of the Trypanosomatidae family have a huge impact on human health. Leishmaniasis, caused by Leishmania spp., is an endemic parasitic disease in over 88 countries and is closely associated with poverty. Although significant advances have been made in the treatment of leishmaniasis over the last decade, currently available chemotherapy is far from satisfactory. The lack of an approved vaccine, effective medication and significant drug resistance worldwide had led to considerable interest in discovering new, inexpensive, efficient and safe antileishmanial agents. 1,3,4-Thiadiazole rings are found in biologically active natural products and medicinally important synthetic compounds. The thiadiazole ring exhibits several specific properties: it is a bioisostere of pyrimidine or benzene rings with prevalence in biologically active compounds; the sulfur atom increases lipophilicity and combined with the mesoionic character of thiadiazoles imparts good oral absorption and good cell permeability, resulting in good bioavailability. This review presents synthetic 2-amino-1,3,4-thiadiazole derivatives with antileishmanial activity. Many reported derivatives can be considered as lead compounds for the synthesis of future agents as an alternative to the treatment of leishmaniasis.

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Section: Kinetoplastea Parasitesmentioning

confidence: 99%

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

Section: Kinetoplastea Parasitesmentioning

confidence: 99%

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Future Prospects in the Treatment of Parasitic Diseases: 2-Amino-1,3,4-Thiadiazoles in Leishmaniasis

Şerban

2019

Molecules

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“…Accordingly, the World Health Organization has encouraged the development of new drugs to counter this disease. However, drug development is a time-consuming and expensive process 6 . Promising alternatives include the use of pharmaceutical technology in combination with different nanocarriers to minimize side effects and improve efficacy and bioavailability.…”

mentioning

confidence: 99%

Use of pharmaceutical nanotechnology for the treatment of leishmaniasis

Marques

Júnior

Andrade

et al. 2019

Rev. Soc. Bras. Med. Trop.

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Introduction: Leishmaniasis is a global public health concern. Currently available treatments are associated with considerable side effects. The use of nanotechnology has shown promise for improving efficacy and bioavailability and minimizing side effects. Methods: This study investigated available literature, including patents and scientific articles, to identify advances in the use of nanotechnology for the treatment of leishmaniasis. Results: Our findings revealed a stable number of patents and scientific articles published over the past five years. Conclusions: There is a need to intensify research on the use of nanotechnology for the treatment of leishmaniasis.

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Chitosan-based particulate systems for drug and vaccine delivery in the treatment and prevention of neglected tropical diseases

Şenel

Yüksel

2020

Drug Deliv. and Transl. Res.

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Nanostructures for Improved Antimonial Therapy of Leishmaniasis

Cited by 7 publications

References 112 publications

Future Prospects in the Treatment of Parasitic Diseases: 2-Amino-1,3,4-Thiadiazoles in Leishmaniasis

Future Prospects in the Treatment of Parasitic Diseases: 2-Amino-1,3,4-Thiadiazoles in Leishmaniasis

Use of pharmaceutical nanotechnology for the treatment of leishmaniasis

Chitosan-based particulate systems for drug and vaccine delivery in the treatment and prevention of neglected tropical diseases

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