An Inhalable Powder Formulation Based on Micro- and Nanoparticles Containing 5-Fluorouracil for the Treatment of Metastatic Melanoma

Zatta, Kelly Cristine; Frank, Luíza Abrahão; Reolon, Luciano Antonio; Amaral-Machado, Lucas; Egito, Eryvaldo Sócrates Tabosa do; Gremião, Maria Palmira Daflon; Pohlmann, Adriana Raffin; Guterres, Sílvia Stanisçuaski

doi:10.3390/nano8020075

Cited by 20 publications

(18 citation statements)

References 72 publications

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“…The scanning electron microscopy (SEM) images obtained from the formulations DAP-LNC-CS-L1 and DAP-LNC-CS-L2 showed the presence of morphological agglomerates and an irregular surface of the particles according to Figure 6. The SEM images found in our study corroborate with other dry powder images of spray-dried nanocapsules obtained by SEM (22,23,28).…”

Section: Scanning Electron Microscopy Of the Nanocapsule Spraydried Psupporting

confidence: 90%

“…Particle size and high specific surface area provide suitable flow characteristics which are used for the purpose of improving post-dry properties (27). In this context, powders having different granulometries could be administered by means of a dry powder inhaler with an appropriate drug delivery along the respiratory tract (28). The behavior of post-dry redispersion is evaluated by the wet diffraction technique to demonstrate that the powders from a dispersion time are able to recover their nanometric characteristics (29).…”

Section: Development and Characterization Of The Nanocapsule Spray-drmentioning

confidence: 99%

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Dry-Powder of Chitosan-Coated Lipid-Core Nanocapsules Containing Dapsone: Development, Laser Diffraction Characterization and Analytical Quantification

Cé¹,

Jornada²,

Marchi³

et al. 2019

Drug Anal. Res.

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Analytical techniques are critical for ensuring physical and chemical stability of a drug both for assessing the stability of drug molecules and for quantifying and identifying the drug content in products. We proposed the development of dry-powders of lipid-core nanocapsules containing dapsone and coated with chitosan, as well as, the analytical quantification of dapsone in dry-powders with 1% and 2% (m/v) of leucine by high-performance liquid chromatography (HPLC). Size is the most relevant physicochemical property of nanoparticulated drug delivery systems. In this context, our results demonstrated that during the powders redispersion in water, could be observed that the mean particle diameters (DAP-LNC-CS-L1 and DAP-LNC-CS-L2) decreased with redispersion times increase. The spray-drying of the lipid-core nanocapsule formulations showed yields ranging from 58 ± 1.0 % (DAP-LNC-CS-L1) to 61 ± 1.5 % (DAP-LNC-CS-L2) indicating an efficient drying process. In this context, the analytical quantifications of dapsone in the dry powders of nanocapsules by HPLC showed that the dapsone content ranged from 92 ± 1.4% (DAP-LNC-CS-L2) to 95 ± 0.8% (DAP-LNC-CS-L1). Can be concluded that spray-drying process of DAP-LNC-CS-L1 and DAP-LNC-CS-L2 formulations showed an efficient aqueous dispersion of nanocapsule powders and the analytical quantification of dapsone in spray-dryed powders were higher than 90%.

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Section: Scanning Electron Microscopy Of the Nanocapsule Spraydried Psupporting

confidence: 90%

Section: Development and Characterization Of The Nanocapsule Spray-drmentioning

confidence: 99%

Dry-Powder of Chitosan-Coated Lipid-Core Nanocapsules Containing Dapsone: Development, Laser Diffraction Characterization and Analytical Quantification

Cé¹,

Jornada²,

Marchi³

et al. 2019

Drug Anal. Res.

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“…A flow rate of 1.0 mL/min and injection volume 20 μl at ambient temperature were maintained while detection was performed at wavelength of 268 nm 41 . Prior to analysis, reverse phase column was equilibrated with mobile phase made up of methanol 5 mM sodium phosphate buffer in ratio of 595, and pH adjusted to 5 42 .…”

Section: Characterization Of Sln Formulations Transmission Electron mentioning

confidence: 99%

Application of smart solid lipid nanoparticles to enhance the efficacy of 5-fluorouracil in the treatment of colorectal cancer

Smith

Affram

Nottingham

et al. 2020

Sci Rep

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5-Fluorouracil (5-FU) is a standard treatment option for colorectal cancer (CRC) but its rapid metabolism and systemic instability (short half-life) has hindered its therapeutic efficacy. The objective of this study was to develop a novel drug delivery system, solid lipid nanoparticle (SLN), capable of delivering high payload of 5-FU to treat CRC. The rational was to improve 5FU-nanocarrier compatibility and therapeutic efficacy. The SLN-loaded 5-FU was developed by utilizing a Strategic and unique Method to Advance and Refine the Treatment (SMART) of CRC through hot and cold homogenization approach. The SLN was made of unique PEGylated lipids and combination of the surfactants. Cytotoxicity studies, clonogenic assay, flow cytometry and confocal imaging were conducted to evaluate the effectiveness and cellular uptake of 5FU-SLN4 in HCT-116 cancer cells. Pharmacokinetic (PK) parameters and receptor expressions were determined while tumor efficacy studies were conducted on mouse bearing subcutaneous HCT-116 cancer. Among the all the formulations, 5FU-SLN4 was the most effective with particle size of was 263 ± 3 nm, zeta potential was 0.1 ± 0.02 and entrapment efficiency of 81 ± 10%. The IC50 value of 5FU-SLN4 (7.4 ± 0.02 µM) was 2.3 fold low compared with 5-FU (17.7 ± 0.03 µM). For tumor efficacy studies, 5FU-SLN4 significantly inhibited tumor growth in comparison to 5-FU while area-under plasma concentration-time curve (AUC) of 5FU-SLN4 was 3.6 fold high compared with 5-FU. HER2 receptors expression were markedly reduced in 5-FU-SLN4 treated mice compared with 5FU and liver and kidney tissues showed no toxicity at dose of 20 mg/kg. 5FU-SLN4 was highly cytotoxic against HCT-116 cells and significantly inhibited subcutaneous tumor growth in mice compared with 5-FU. This emphasizes the significance of developing a smart nano-delivery system to optimize the delivery efficiency of anticancer drugs to tumors.

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“…A wide variety of drug carriers have been developed to enhance the pharmacokinetic performance and biodistribution of drugs; however, the carrier is generally just an excipient for delivery goal where only the drug molecule is the therapeutically relevant compound . Natural compound‐based nanoparticles are a minimally explored area of drug delivery with significant promise for cancer therapy.…”

mentioning

confidence: 99%

Targeted Therapy against Metastatic Melanoma Based on Self‐Assembled Metal‐Phenolic Nanocomplexes Comprised of Green Tea Catechin

et al. 2019

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The targeted therapy of metastatic melanoma is an important yet challenging goal that has received only limited attention to date. Herein, green tea polyphenols, (–)‐epigallocatechin‐3‐gallate (EGCG), and lanthanide metal ions (Sm 3+ ) are used as building blocks to engineer self‐assembled Sm III ‐EGCG nanocomplexes with synergistically enhanced tumor inhibitory properties. These nanocomplexes have negligible systemic toxic effects on healthy cells but cause a significant reduction in the viability of melanoma cells by efficiently regulating their metabolic pathways. Moreover, the wound‐induced migration of melanoma cells can be efficiently inhibited by Sm III ‐EGCG, which is a key criterion for metastatic melanoma therapy. In a mouse melanoma tumor model, Sm III ‐EGCG is directly compared with a clinical anticancer drug, 5‐fluorouracil and shows remarkable tumor inhibition. Moreover, the targeted therapy of Sm III ‐EGCG is shown to prevent metastatic lung melanoma from spreading to main organs with no adverse side effects on the body weight or organs. These in vivo results demonstrate significant advantages of Sm III ‐EGCG over its clinical counterpart. The results suggest that these green tea‐based, self‐assembled nanocomplexes possess all of the key traits of a clinically promising candidate to address the challenges associated with the treatment of advanced stage metastatic melanoma.

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An Inhalable Powder Formulation Based on Micro- and Nanoparticles Containing 5-Fluorouracil for the Treatment of Metastatic Melanoma

Cited by 20 publications

References 72 publications

Dry-Powder of Chitosan-Coated Lipid-Core Nanocapsules Containing Dapsone: Development, Laser Diffraction Characterization and Analytical Quantification

Dry-Powder of Chitosan-Coated Lipid-Core Nanocapsules Containing Dapsone: Development, Laser Diffraction Characterization and Analytical Quantification

Application of smart solid lipid nanoparticles to enhance the efficacy of 5-fluorouracil in the treatment of colorectal cancer

Targeted Therapy against Metastatic Melanoma Based on Self‐Assembled Metal‐Phenolic Nanocomplexes Comprised of Green Tea Catechin

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