In vitro activity of amphotericin B cochleates against Leishmania chagasi

Sesana, Aretha Molina; Monti-Rocha, Renata; Vinhas, Solange Alves; Morais, Carlos Gustavo; Dietze, Reynaldo; Lemos, Elenice Moreira

doi:10.1590/s0074-02762011000200022

Cited by 28 publications

(17 citation statements)

References 11 publications

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“…When comparing the EC 50 of our compounds with amphotericin B (EC 50 : 0,022 mM), it is noted that the latter has lower EC 50 , ad is more effective when compared to the number of compounds used. This point is crucial, since amphotericin B has been shown as one of the most active antileishmanial drugs ever described (Sesana et al, 2011;Lucero et al, 2015;Yesilova et al, 2015), but other drugs with lower antileishmanial activity are widely used in the treatment of leishmaniasis, such as miltefosine (Kaur et al, 2015;Sundar et al, 2015;Vakil et al, 2015).…”

Section: Discussionmentioning

confidence: 99%

Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes

Silva

Palace-Berl

Tavares

et al. 2016

Experimental Parasitology

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Leishmaniasis is an overlooked tropical disease affecting approximately 1 million people in several countries. Clinical manifestation depends on the interaction between Leishmania and the host's immune response. Currently available treatment options for leishmaniasis are limited and induce severe side effects. In this research, we tested nitro-heterocyclic compounds (BSF series) as a new alternative against Leishmania. Its activity was measured in Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes using MTT colorimetric assay. Additionally, we assessed the phosphatidylserine exposure by promastigotes, measured by flow cytometry, as well as nitric oxide production, measured by Griess' method. The nitro-heterocyclic compounds (BSF series) showed activity against L. (L.) infantum promastigotes, inducting the phosphatidylserine exposition by promastigotes, decreasing intracellular amastigotes and increasing oxide nitric production. The selectivity index was more prominent to Leishmania than to macrophages. Compared to amphotericin b, our compounds presented higher IC50, however the selectivity index was more specific to parasite than to amphotericin b. In conclusion, these nitro-heterocyclic compounds showed to be promising as an anti-Leishmania drug, in in vitro studies.

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Section: Discussionmentioning

confidence: 99%

Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes

Silva

Palace-Berl

Tavares

et al. 2016

Experimental Parasitology

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“…Precipitates of phosphatidylserine and calcium incorporating amphotericin B were prepared by Sesana et al [75] and demonstrated to have in vitro activity against Leishmania chagasi. However, further development of amphotericin B lipid cochleates has been limited, perhaps in part due to the low bioavailability of the cochleate formulation [76].…”

Section: Oral Anticancer Drugsmentioning

confidence: 99%

Review and analysis of FDA approved drugs using lipid-based formulations

Savla

Browne

Plassat³

et al. 2017

Drug Development and Industrial Pharmacy

165

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Lipid-based drug delivery systems (LBDDS) are one of the most studied bioavailability enhancement technologies and are utilized in a number of U.S. Food and Drug Administration (FDA) approved drugs. While researchers have used several general rules of thumb to predict which compounds are likely to benefit from LBDDS, formulation of lipid systems is primarily an empiric endeavor. One of the challenges is that these rules of thumb focus in different areas and are used independently of each other. The Developability Classification System attempts to link physicochemical characteristics with possible formulation strategies. Although it provides a starting point, the formulator still has to empirically develop the formulation. This article provides a review and quantitative analysis of the molecular properties of these approved drugs formulated as lipid systems and starts to build an approach that provides more directed guidance on which type of lipid system is likely to be the best for a particular drug molecule. ARTICLE HISTORY

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“…Nanocochleates containing AmpB or AmpB deoxycholate were in vitro tested against L. chagasi, and results showed similar activity. 83,84 Lipid cochleates containing both AmpB and MF were also produced, and the incorporation stability was estimated. 85 Some clinical trials for VL were initiated on the basis of the results obtained with an oral nanocochleate formulation of AmpB (Bioral ® Amphotericin B), which reached Phase I development in the USA for the treatment of mycoses, but nowadays, the research appears to be discontinued.…”

Section: Lipid Cochleatesmentioning

confidence: 99%

Nanostructured delivery systems with improved leishmanicidal activity: a critical review

Bruni¹,

Stella²,

Giraudo³

et al. 2017

IJN

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Leishmaniasis is a vector-borne zoonotic disease caused by protozoan parasites of the genus Leishmania , which are responsible for numerous clinical manifestations, such as cutaneous, visceral, and mucocutaneous leishmaniasis, depending on the site of infection for particular species. These complexities threaten 350 million people in 98 countries worldwide. Amastigotes living within macrophage phagolysosomes are the principal target of antileishmanial treatment, but these are not an easy target as drugs must overcome major structural barriers. Furthermore, limitations on current therapy are related to efficacy, toxicity, and cost, as well as the length of treatment, which can increase parasitic resistance. Nanotechnology has emerged as an attractive alternative as conventional drugs delivered by nanosized carriers have improved bioavailability and reduced toxicity, together with other characteristics that help to relieve the burden of this disease. The significance of using colloidal carriers loaded with active agents derives from the physiological uptake route of intravenous administered nanosystems (the phagocyte system). Nanosystems are thus able to promote a high drug concentration in intracellular mononuclear phagocyte system (MPS)-infected cells. Moreover, the versatility of nanometric drug delivery systems for the deliberate transport of a range of molecules plays a pivotal role in the design of therapeutic strategies against leishmaniasis. This review discusses studies on nanocarriers that have greatly contributed to improving the efficacy of antileishmaniasis drugs, presenting a critical review and some suggestions for improving drug delivery.

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In vitro activity of amphotericin B cochleates against Leishmania chagasi

Cited by 28 publications

References 11 publications

Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes

Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes

Review and analysis of FDA approved drugs using lipid-based formulations

Nanostructured delivery systems with improved leishmanicidal activity: a critical review

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