Effect of 3-Carene and the micellar formulation on 'Leishmania (Leishmania) amazonensis'

Leishmaniases are neglected tropical diseases caused by obligate intracellular 'protozoa' of the genus 'Leishmania'. The drugs used in treatment have a high financial cost, a long treatment time, high toxicity, and variable efficacy. 3-Carene (3CR) is a hydrocarbon monoterpene th...

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Published in:Tropical medicine and infectious disease 2023-06, Vol.8 (6), p.1-15
Main Authors: Silva, Audrey Rouse Soares Tavares, Costa, Amanda Mendonça Barros, Scher, Ricardo, Andrade-Neto, Valter Viana, Sarmento, Victor Hugo Vitorino, Santos, Adriana de Jesus, Torres-Santos, Eduardo Caio, Jain, Sona, Nunes, Rogéria de Souza, Menna-Barreto, Rubem Figueiredo Sadok, Dolabella, Silvio Santana
Format: Article
Language:English
Subjects:
Amastigotes
antileishmanial
Cytotoxicity
Drug delivery systems
Drugs
Experiments
Fibroblasts
Leishmaniasis
monoterpene
Monoterpenes
nanostructure
Parasites
Parasitic diseases
Penicillin
Rheology
Rheology (Biology)
Transmission
Triblock copolymers
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Summary:Leishmaniases are neglected tropical diseases caused by obligate intracellular 'protozoa' of the genus 'Leishmania'. The drugs used in treatment have a high financial cost, a long treatment time, high toxicity, and variable efficacy. 3-Carene (3CR) is a hydrocarbon monoterpene that has shown in vitro activity against some 'Leishmania' species; however, it has low water solubility and high volatility. This study aimed to develop Poloxamer 407 micelles capable of delivering 3CR (P407-3CR) to improve antileishmanial activity. The micelles formulated presented nanometric size, medium or low polydispersity, and Newtonian fluid rheological behavior. 3CR and P407-3CR inhibited the growth of 'L'. ('L'.) 'amazonensis' promastigote with IC50/48h of 488.1 ± 3.7 and 419.9 ± 1.5 mM, respectively. Transmission electron microscopy analysis showed that 3CR induces multiple nuclei and kinetoplast phenotypes and the formation of numerous cytosolic invaginations. Additionally, the micelles were not cytotoxic to L929 cells or murine peritoneal macrophages, presenting activity on intracellular amastigotes. P407-3CR micelles (IC50/72 h = 0.7 ± 0.1 mM) increased the monoterpene activity by at least twice (3CR: IC50/72 h >1.5 mM). These results showed that P407 micelles are an effective nanosystem for delivering 3CR and potentiating antileishmanial activity. More studies are needed to evaluate this system as a potential therapeutic option for leishmaniases.
ISSN:2414-6366
2414-6366
DOI:10.3390/tropicalmed8060324