Lipid-Based Nanoformulations of Trifluralin Analogs in the Management of
            <i>Leishmania Infantum</i>
            Infections

Lopes, Rodrigo J.G.; Pereira, Joana; Esteves, M. Alexandra; Gaspar, Maria Manuela; Carvalheiro, Manuela; Eleutério, Carla; Gonçalves, Lídia; Jiménez-Ruı́z, Antonio; Almeida, António J.; Cruz, M.E.M.

doi:10.2217/nnm.15.190

Cited by 19 publications

(7 citation statements)

References 30 publications

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“…Despite the decades of research, CL management is still unsatisfactory owing to numerous challenges associated with existing therapeutics (Awanish Kumar et al, 2018a;Zulfiqar et al, 2017). Substantial anti-leishmanial activity renders TFL a suitable candidate against CL, however, due to its crystalline nature and poor aqueous solubility, its use was restrained (Lopes et al, 2016).…”

Section: Discussionmentioning

confidence: 99%

“…Repurposing of existing drugs can be an opportunistic approach to ameliorate anti-leishmanial therapy associated challenges (Jamshaid et al, 2021). A dinitroaniline compound, Trifluralin (TFL)-a herbicidal compound, is charismatic for leishmaniasis owing to its ability of inhibiting microtubules polymerization and tubulin formation (Chan et al, 1993;Lopes et al, 2016), as illustrated in Figure -1. It exhibits limited response when applied topically to tackle CL (Esteves et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

“…Nanotechnologybased techniques are valuable to improve its water solubility. Attempts have been made to design nano-delivery systems of TFL and its analogues (Lopes et al, 2016). In last decade, antileishmanial chemotherapy was merged with nanotechnology, hence, multiple anti-leishmanial nano-formulations has been designed.…”

Section: Introductionmentioning

confidence: 99%

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Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Khan

Jamshaid

Din

et al. 2022

Journal of Pharmaceutical Sciences

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This is a PDF file of an article that has undergone enhancements after acceptance, such as the addition of a cover page and metadata, and formatting for readability, but it is not yet the definitive version of record. This version will undergo additional copyediting, typesetting and review before it is published in its final form, but we are providing this version to give early visibility of the article. Please note that, during the production process, errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Khan

Jamshaid

Din

et al. 2022

Journal of Pharmaceutical Sciences

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“…According to Lopes et al (2016), the effective antileishmanial activity of lipid nanocarriers goes through an effective internalization process of these nanostructures by macrophages [69]. Therefore, Pires and collaborators (2020) evaluated macrophages' recognition of their solid lipid nanoparticles by analyzing an uptake assay with fluorescent SLN using thioglycolateelicited macrophages from male mice [70].…”

Section: Antileishmanial Activity (In Vitro)mentioning

confidence: 99%

Annatto Oil Loaded Nanostructured Lipid Carriers: A Potential New Treatment for Cutaneous Leishmaniasis

et al. 2021

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Annatto (Bixa orellana L.) is extensively used as food pigment worldwide. Recently, several studies have found it to have healing and antioxidant properties, as well as effective action against leishmaniasis. Therefore, the purpose of this study was to incorporate the oil obtained from annatto seeds into a nanostructured lipid carrier (NLC) and evaluate its physicochemical properties and biological activity against Leishmania major. Nanoparticles were prepared by the fusion-emulsification and ultrasonication method, with the components Synperonic™ PE (PL) as the surfactant, cetyl palmitate (CP) or myristyl myristate (MM) as solid lipids, annatto oil (AO) (2% and 4%, w/w) as liquid lipid and active ingredient, and ultra-pure water. Physicochemical and biological characterizations were carried out to describe the NLCs, including particle size, polydispersity index (PDI), and zeta potential (ZP) by dynamic light scattering (DLS), encapsulation efficiency (EE%), thermal behavior, X-ray diffraction (XRD), transmission electron microscopy (TEM), Electron Paramagnetic Resonance (EPR), cytotoxicity on BALB/c 3T3 fibroblasts and immortalized human keratinocyte cells, and anti-leishmaniasis activity in vitro. Nanoparticles presented an average diameter of ~200 nm (confirmed by TEM results), a PDI of less than 0.30, ZP between −12.6 and −31.2 mV, and more than 50% of AO encapsulated in NLCs. Thermal analyses demonstrated that the systems were stable at high temperatures with a decrease in crystalline structure due to the presence of AOs (confirmed by XRD). In vitro, the anti-leishmania test displayed good activity in encapsulating AO against L. major. The results indicate that the oily fraction of Bixa orellana L. in NLC systems should be evaluated as a potential therapeutic agent against leishmaniasis.

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“…Solid lipid nanoparticles (SLNs) are colloidal nanocarriers that have a size range between 50 and 100 nm, generally spherical in shape, being their structure composed of a solid lipid core (at both room and body temperatures), stabilized by an interfacial surfactant layer [188,189]. Several lipids can be used for the preparation of SLNs, including fatty acids, highly purified triglycerides, complex glyceride mixtures, or waxes.…”

Section: Nanotheranostics In Diagnosis and Treatment Of Cancermentioning

confidence: 99%

Current Trends in Cancer Nanotheranostics: Metallic, Polymeric, and Lipid-Based Systems

et al. 2019

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Theranostics has emerged in recent years to provide an efficient and safer alternative in cancer management. This review presents an updated description of nanotheranostic formulations under development for skin cancer (including melanoma), head and neck, thyroid, breast, gynecologic, prostate, and colon cancers, brain-related cancer, and hepatocellular carcinoma. With this focus, we appraised the clinical advantages and drawbacks of metallic, polymeric, and lipid-based nanosystems, such as low invasiveness, low toxicity to the surrounding healthy tissues, high precision, deeper tissue penetration, and dosage adjustment in a real-time setting. Particularly recognizing the increased complexity and multimodality in this area, multifunctional hybrid nanoparticles, comprising different nanomaterials and functionalized with targeting moieties and/or anticancer drugs, present the best characteristics for theranostics. Several examples, focusing on their design, composition, imaging and treatment modalities, and in vitro and in vivo characterization, are detailed herein. Briefly, all studies followed a common trend in the design of these theranostics modalities, such as the use of materials and/or drugs that share both inherent imaging (e.g., contrast agents) and therapeutic properties (e.g., heating or production reactive oxygen species). This rationale allows one to apparently overcome the heterogeneity, complexity, and harsh conditions of tumor microenvironments, leading to the development of successful targeted therapies.

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Lipid-Based Nanoformulations of Trifluralin Analogs in the Management of Leishmania Infantum Infections

Abstract: The modification of TFL structure to obtain active TFLA, together with their incorporation in NanoDDS, improved their in vivo performance against L. infantum infection.

Cited by 19 publications

References 30 publications

Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Designing, Optimization and Characterization of Trifluralin Transfersomal Gel to Passively Target Cutaneous Leishmaniasis

Annatto Oil Loaded Nanostructured Lipid Carriers: A Potential New Treatment for Cutaneous Leishmaniasis

Current Trends in Cancer Nanotheranostics: Metallic, Polymeric, and Lipid-Based Systems

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