Improved antileishmanial activity and cytotoxicity of a novel nanotherapy for N-iodomethyl-N,N-dimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide

Fernández, Maritza; Holgado, M.A.; Otero, María Dolores Cayero; Pineda, Tatiana; Yepes, Lina M.; Gaspar, Diana P.; Almeida, António J.; Robledo, Sara M.; Martín-Banderas, Lucía

doi:10.1016/j.jddst.2020.101988

Cited by 3 publications

(4 citation statements)

References 47 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The effectiveness was exclusive to the amastigote stage, with similar effects on the different Leishmania species evaluated. [7,8,12] C 6 I inhibits choline/ethanolamine kinase and phosphatidylcholine production in L. infantum but also interferes with the in vitro choline uptake in L. tarentolae. [6] TC1 and TC2 inhibited protease activity in L. braziliensis and the functioning of mitochondria, an organelle that, in Leishmania, is primarily responsible for energy metabolism since it provides 70% of ATP production.…”

Section: Validation Of the In Vitro Cytotoxicity And Leishmanicidal A...mentioning

confidence: 99%

“…In addition, the thermodynamic stability of the nanoemulsions was established under centrifugation and freeze/thaw cycles. [8] Therefore, nanoemulsions were centrifuged at 13,000 rpm for one hour; then, test tubes containing 0.5 mL of the formulation were hermetically sealed and stored upright for 24 h at −20°C and then for another 24 h at 37°C. The formulations were observed for any changes such as precipitation, phase separation, or agglutination, and this cycle was repeated six times.…”

Section: Characterization Of the Nanoemulsionmentioning

confidence: 99%

“…Besides, it also interferes with the in vitro choline uptake in Leishmania tarentolae promastigotes. [6] Furthermore, C 6 I is active against intracellular amastigotes of Leishmania panamensis [7] and Leishmania braziliensis [8] ; moreover, administered topically at a dose of 2 mg/kg/day for 15 days or formulated in precirol nanoparticles, it can cure hamsters with experimental CL caused by L. braziliensis. [9] Furthermore, TC1 and TC2 [10] compounds derived from chromon and thiochromon compounds, formulated as a 4% ointment, showed an excellent therapeutic response when administered topically in hamsters with CL caused by L. braziliensis.…”

mentioning

confidence: 99%

“…[13] The significantly moderated lipophilicity of compounds TC2, TC1, and C 6 I can make it through the media watery tissue of the skin, being the step limitation in the process of diffusion of these assets. [7,8,[10][11][12] Therefore, transportation is the only you can get by upgrading permeation efficiency. A highly lipophilic molecule tends to accumulate within the top layer of the skin, the stratum corneum, and poorly spreads to deeper strata.…”

mentioning

confidence: 99%

See 3 more Smart Citations

Nanoemulsions for increased penetrability and sustained release of leishmanicidal compounds

García

Fernández‐Culma

Upegui

et al. 2023

Archiv der Pharmazie

Self Cite

View full text Add to dashboard Cite

In the last decade, the World Health Organization has driven the development of drugs for topical use in patients with cutaneous leishmaniasis (CL), the most prevalent clinical form of leishmaniasis, a neglected tropical disease. The chemicals C 6 I, TC1, and TC2 were reported as promising antileishmanial drugs. We aimed to develop a topical nanoformulation that enhances the advantageous effect of C 6 I, TC1, and TC2, guaranteeing higher stability and bioavailability of the pharmacologically active components through the topical route. Nanoemulsions were prepared by ultrasonication based on oleic acid (0.5 g). A relation of Tween ® -80/ ethanol (1:3) and water was obtained; physicochemical characterization of all formulations was performed, and the preliminary stability and transdermal penetration of these nanoemulsions were also investigated. Newtonian-type fluids with high load capacity, 147-273 nm globule size, and −15 to −18 mV zeta potential were obtained with differential permeability rates in the first pig ear skin assay, first-order kinetics-release model for C 6 I, and Weibull for TC1 and TC2. The nanoemulsion showed good stability, high encapsulation efficiency, and higher leishmanicidal activity against Leishmania braziliensis with lower cytotoxicity in U937 macrophages. In conclusion, nanoemulsions of ethanol-oleic acid/Tween ® -80 increase the activity of compounds with leishmanicidal activity by increasing their penetration and sustained release.

show abstract

Section: Validation Of the In Vitro Cytotoxicity And Leishmanicidal A...mentioning

confidence: 99%

Section: Characterization Of the Nanoemulsionmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

See 2 more Smart Citations

Nanoemulsions for increased penetrability and sustained release of leishmanicidal compounds

García

Fernández‐Culma

Upegui

et al. 2023

Archiv der Pharmazie

Self Cite

View full text Add to dashboard Cite

show abstract

PLGA Nanoparticles as New Drug Delivery Systems in Leishmaniasis Chemotherapy: A Review of Current Practices

Valiallahi,

Vazifeh,

Gatabi

et al. 2024

CMC

View full text Add to dashboard Cite

Although leishmaniasis is one of the most common parasitic diseases, its traditional treatments suffer from some serious problems. To solve such issues, we can take advantage of the effective nanoparticle-based approaches to deliver anti-leishmanial agents into leishmania-infected macrophages either using passive targeting or using macrophage-related receptors. Despite the high potential of nanotechnology, Liposomal Amphotericin B (AmBisome®) is the only FDA-approved nanoparticle-based anti-leishmanial therapy. In an effort to find more anti-leishmanial nano-drugs, this 2011-2021 review study aimed to investigate the in-vivo and in-vitro effectiveness of poly (lactic-co-glycolic acid) nanoparticles (PLGA-NPs) in the delivery of some traditional anti-leishmanial drugs. Based on the results, PLGA-NPs could improve solubility, controlled release, trapping efficacy, bioavailability, selectivity, and mucosal penetration of the drugs, while they decreased resistance, dose/duration of administration and organotoxicity of the agents. However, none of these nano-formulations have been able to enter clinical trials so far. We summarized the data about the common problems of anti-leishmanial agents and the positive effects of various PLGA nano-formulations on reducing these drawbacks under both in-vitro and in-vitro conditions in three separate tables. Overall, this study proposes two AmB-loaded PLGA with a 99% reduction in parasite load as promising nanoparticles for further studies.

show abstract

Nanomedical research and development in Spain: improving the treatment of diseases from the nanoscale

Fernández-Gómez

Aranda

Tosat‐Bitrián

et al. 2023

Front. Bioeng. Biotechnol.

View full text Add to dashboard Cite

The new and unique possibilities that nanomaterials offer have greatly impacted biomedicine, from the treatment and diagnosis of diseases, to the specific and optimized delivery of therapeutic agents. Technological advances in the synthesis, characterization, standardization, and therapeutic performance of nanoparticles have enabled the approval of several nanomedicines and novel applications. Discoveries continue to rise exponentially in all disease areas, from cancer to neurodegenerative diseases. In Spain, there is a substantial net of researchers involved in the development of nanodiagnostics and nanomedicines. In this review, we summarize the state of the art of nanotechnology, focusing on nanoparticles, for the treatment of diseases in Spain (2017–2022), and give a perspective on the future trends and direction that nanomedicine research is taking.

show abstract

Improved antileishmanial activity and cytotoxicity of a novel nanotherapy for N-iodomethyl-N,N-dimethyl-N-(6,6-diphenylhex-5-en-1-yl)ammonium iodide

Cited by 3 publications

References 47 publications

Nanoemulsions for increased penetrability and sustained release of leishmanicidal compounds

Nanoemulsions for increased penetrability and sustained release of leishmanicidal compounds

PLGA Nanoparticles as New Drug Delivery Systems in Leishmaniasis Chemotherapy: A Review of Current Practices

Nanomedical research and development in Spain: improving the treatment of diseases from the nanoscale

Contact Info

Product

Resources

About