Nanosuspension of quercetin: preparation, characterization and effects against Aedes aegypti larvae

Pessoa, Leticie Zulmira da Silva; Duarte, Jonatas Lobato; Ferreira, Ricardo Marcelo dos Anjos; Oliveira, Anna Eliza Maciel de Faria Mota; Cruz, Rodrigo Alves Soares; Faustino, Silvia Maria Mathes; Carvalho, José Carlos Tavares; Fernandes, Caio P.; Souto, Raimundo Nonato Picanço; Araújo, Raquel Silva

doi:10.1016/j.bjp.2018.07.003

Cited by 28 publications

(8 citation statements)

References 39 publications

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“…Previously, several formulation technologies for nanosuspension have been developed, i.e., nanocrystals using high-pressure homogenization [ 41 ], nanosuspensions by high-pressure homogenization [ 42 ], and nanosuspension by a solvent displacement method followed by solvent evaporation [ 43 ]. In this study, quercetin nanosuspension was successfully developed to improve the solubility and stability of natural quercetin molecules using an acid-base nanoprecipitation method ( Figure 2 and Table 1 ).…”

Section: Resultsmentioning

confidence: 99%

Anti-Inflammatory, Antioxidative, and Nitric Oxide-Scavenging Activities of a Quercetin Nanosuspension with Polyethylene Glycol in LPS-Induced RAW 264.7 Macrophages

et al. 2022

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Quercetin (Qu) is a dietary antioxidant and a member of flavonoids in the plant polyphenol family. Qu has a high ability to scavenge reactive oxygen species (ROS) and reactive nitrogen species (RNS) molecules; hence, exhibiting beneficial effects in preventing obesity, diabetes, cancer, cardiovascular diseases, and inflammation. However, quercetin has low bioavailability due to poor water solubility, low absorption, and rapid excretion from the body. To address these issues, the usage of Qu nanosuspensions can improve physical stability, solubility, and pharmacokinetics. Therefore, we developed a Qu and polyethylene glycol nanosuspension (Qu-PEG NS) and confirmed its interaction by Fourier transform infrared analysis. Qu-PEG NS did not show cytotoxicity to HaCaT and RAW 264.7 cells. Furthermore, Qu-PEG NS effectively reduced the nitrogen oxide (NO) production in lipopolysaccharide (LPS)-induced inflammatory RAW 264.7 cells. Additionally, Qu-PEG NS effectively lowered the levels of COX-2, NF-κB p65, and IL-1β in the LPS-induced inflammatory RAW 264.7 cells. Specifically, Qu-PEG NS exhibited anti-inflammatory properties by scavenging the ROS and RNS and mediated the inhibition of NF-κB signaling pathways. In addition, Qu-PEG NS had a high antioxidant effect and antibacterial activity against Escherichia coli and Bacillus cereus. Therefore, the developed novel nanosuspension showed comparable antioxidant, anti-inflammatory, and antibacterial functions and may also improve solubility and physical stability compared to raw quercetin.

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Section: Resultsmentioning

confidence: 99%

Anti-Inflammatory, Antioxidative, and Nitric Oxide-Scavenging Activities of a Quercetin Nanosuspension with Polyethylene Glycol in LPS-Induced RAW 264.7 Macrophages

et al. 2022

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“…In the final step, we used AutoDockVina to generate nine docking positions for each ligand interacting with the OBP active site and to return energy affinity values (kcal/mol). All docking position results were analyzed using PyMOL 2.0 [ 42 ] and Discovery Studio 4.5 [ 43 ] to select the best position for each ligand inside the AaegOBP1 receptor. For this, we considered the receptor-ligand affinity energies, ligand interactions with the amino acids from the active site, and the route mean square deviation (RMSD) between the initial and subsequent ligand structures.…”

Section: Methodsmentioning

confidence: 99%

Methanolic Extracts of Chiococca alba in Aedes aegypti Biorational Management: Larvicidal and Repellent Potential, and Selectivity against Non-Target Organisms

Borges

Haddi

Valbon

et al. 2022

Plants

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The use of formulations containing botanical products for controlling insects that vector human and animal diseases has increased in recent years. Plant extracts seem to offer fewer risks to the environment and to human health without reducing the application strategy’s efficacy when compared to synthetic and conventional insecticides and repellents. Here, we evaluated the potential of extracts obtained from caninana, Chiococca alba (L.) Hitchc. (Rubiaceae), plants as a tool to be integrated into the management of Aedes aegypti, one of the principal vectors for the transmission of arborviruses in humans. We assessed the larvicidal and repellence performance against adult mosquitoes and evaluated the potential undesired effects of the extracts on non-target organisms. We assessed the susceptibility and predatory abilities of the nymphs of Belostoma anurum, a naturally occurring mosquito larva predator, and evaluated the C. alba extract’s cytotoxic effects in mammalian cell lines. Our chromatographic analysis revealed 18 compounds, including rutin, naringin, myricetin, morin, and quercetin. The methanolic extracts of C. alba showed larvicidal (LC50 = 82 (72–94) mg/mL) activity without killing or affecting the abilities of B. anurum to prey upon mosquito larvae. Our in silico predictions revealed the molecular interactions between rutin and the AeagOBP1 receptor to be one possible mechanism for the repellent potential recorded for formulations containing C. alba extracts. Low cytotoxicity against mammalian cell lines reinforces the selectivity of C. alba extracts. Collectively, our findings highlight the potential of C. alba and one of its constituents (rutin) as alternative tools to be integrated into the management of A. aegypti mosquitoes.

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“…Strategies employed to improve formulation stability and effectiveness include nanoformulation and microencapsulation ( Werdin González et al, 2014 ; Pessoa et al, 2018 ; Campos et al, 2020 ; Shahzad and Manzoor, 2021 ). The impregnation of zedoary oil in sand granules also remarkably prolonged activity from 5 days to 3 weeks ( Champakaew et al, 2007 ; Sutthanont et al, 2019 ).…”

Section: Strategies To Improve Insecticide Residualitymentioning

confidence: 99%

Challenges, Advances and Opportunities in Exploring Natural Products to Control Arboviral Disease Vectors

Demarque

Espindola

2021

Front. Chem.

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Natural products constitute an important source of molecules for product development. However, despite numerous reports of compounds and active extracts from biodiversity, poor and developing countries continue to suffer with endemic diseases caused by arboviral vectors, including dengue, Zika, chikungunya and urban yellow fever. Vector control remains the most efficient disease prevention strategy. Wide and prolonged use of insecticides has resulted in vector resistance, making the search for new chemical prototypes imperative. Considering the potential of natural products chemistry for developing natural products-based products, including insecticides, this contribution discusses the general aspects and specific characteristics involved in the development of drug leads for vector control. Throughout this work, we highlight the obstacles that need to be overcome in order for natural products compounds to be considered promising prototypes. Moreover, we analyze the bottlenecks that should be addressed, together with potential strategies, to rationalize and improve the efficiency of the drug discovery process.

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Nanosuspension of quercetin: preparation, characterization and effects against Aedes aegypti larvae

Cited by 28 publications

References 39 publications

Anti-Inflammatory, Antioxidative, and Nitric Oxide-Scavenging Activities of a Quercetin Nanosuspension with Polyethylene Glycol in LPS-Induced RAW 264.7 Macrophages

Anti-Inflammatory, Antioxidative, and Nitric Oxide-Scavenging Activities of a Quercetin Nanosuspension with Polyethylene Glycol in LPS-Induced RAW 264.7 Macrophages

Methanolic Extracts of Chiococca alba in Aedes aegypti Biorational Management: Larvicidal and Repellent Potential, and Selectivity against Non-Target Organisms

Challenges, Advances and Opportunities in Exploring Natural Products to Control Arboviral Disease Vectors

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