A new medium-throughput screening design approach for the development of hydroxymethylnitrofurazone (NFOH) nanostructured lipid carrier for treating leishmaniasis

Souza, Aline de; Yukuyama, Megumi Nishitani; Barbosa, Eduardo José; Monteiro, Lis Marie; Faloppa, Ana Cristina Breithaupt; Calixto, Leandro Augusto; Araújo, Gabriel Lima de Barros; Fotaki, Nikoletta; Löbenberg, Raimar; Bou‐Chacra, Nádia Araci

doi:10.1016/j.colsurfb.2020.111097

Cited by 10 publications

(2 citation statements)

References 58 publications

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“…Therefore, this work performed a preformulation test to assess the solubility of magnolol in oil or oil mixtures found in the most popular commercial fat emulsions. Crystal 16 TM combines automation with integrated transmissivity technology, which is a convenient method allowing the screening of a large number of liquid lipids in a short time using a low amount of drug substances and without the use of an organic solvent [ 24 ]. Comparing oil mixtures selected for this study, corresponding to commercially available intravenous lipid emulsions, Mix 4 composed of 30% of soybean oil, 30% of MCT, 25% of olive oil, and 15% of fish oil, possessed the best solubilization capacity [ 25 ] for magnolol.…”

Section: Discussionmentioning

confidence: 99%

The Development of Magnolol-Loaded Intravenous Emulsion with Low Hepatotoxic Potential

Gostyńska,

Czerniel,

Kuźmińska

et al. 2023

Pharmaceuticals

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Intestinal failure-associated liver disease (IFALD) is a severe liver injury occurring due to factors related to intestinal failure and parenteral nutrition administration. Different approaches are studied to reduce the risk or ameliorate the course of IFALD, including providing omega-3 fatty acids instead of soybean oil-based lipid emulsion or administering active compounds that exert a hepatoprotective effect. This study aimed to develop, optimize, and characterize magnolol-loaded intravenous lipid emulsion for parenteral nutrition. The preformulation studies allowed for chosen oils mixture of the highest capacity of magnolol solubilization. Then, magnolol-loaded SMOFlipid was developed using the passive incorporation method. The Box–Behnken design and response surface methodology were used to optimize the entrapment efficiency. The optimal formulation was subjected to short-term stress tests, and its effect on normal human liver cells and erythrocytes was determined using the MTT and hemolysis tests, respectively. The optimized magnolol-loaded SMOFlipid was characterized by the mean droplet diameter of 327.6 ± 2.9 nm with a polydispersity index of 0.12 ± 0.02 and zeta potential of −32.8 ± 1.2 mV. The entrapment efficiency of magnolol was above 98%, and pH and osmolality were sufficient for intravenous administration. The magnolol-loaded SMOFlipid samples showed a significantly lower toxic effect than bare SMOFlipid in the same concentration on THLE-2 cells, and revealed an acceptable hemolytic effect of 8.3%. The developed formulation was characterized by satisfactory stability. The in vitro studies showed the reduced cytotoxic effect of MAG-SMOF applied in high concentrations compared to bare SMOFlipid and the non-hemolytic effect on human blood cells. The magnolol-loaded SMOFlipid is promising for further development of hepatoprotective lipid emulsion for parenteral nutrition.

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Section: Discussionmentioning

confidence: 99%

The Development of Magnolol-Loaded Intravenous Emulsion with Low Hepatotoxic Potential

Gostyńska,

Czerniel,

Kuźmińska

et al. 2023

Pharmaceuticals

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“…NLCs formulation also exhibited sustained and prolonged release of a drug than SLN. There are various previous work reported of NLCs for oral delivery of poorly/sparingly soluble drug for the improvement of drug load, sustained release and bioavailability i.e., NLCs delivery of ezetimibe 15 , saquinavir 16 hydroxymethyl-nitrofurazone 17 , baicalin 18 and exhibited the remarkable response. A few works were reported for DG i.e., solid self nano emulsifying system 5,19 , magnetic nanoparticle 20 , and sustained-release tablet 21 for improvement of drug delivery.…”

mentioning

confidence: 99%

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, <i>in vitro</i> Characterization and <i>ex vivo</i> Intestinal Permeation Study

Zafar

2020

J. Oleo Sci.

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IntroductionDiabetes type 2, diabetes mellitus is a group of metabolic disease in which the blood glucose level increase ≥ 200 mg/dL for a long period. Due to high blood glucose level, many other symptoms appeared simultaneously like more frequent urination, weight loss, increased hunger, dehydration, as well as the alteration in lipid profile, liver function test and kidney function test. The associated complication may occur like heart attack, kidney failure and damaged eye in chronic and serious condition. In worldwide approx. 422 million peoples were affected and about 1.6 million deaths occurred in the low and middle-income countries in every year 1 . Various oral dosage form available in the market to reduce the blood glucose level

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Niclosamide nanoemulsion for colorectal cancer: development, physicochemical characterization, and in vitro anticancer activity

Barbosa,

Fukumori,

de Araújo Sprengel

et al. 2024

J Nanopart Res

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A new medium-throughput screening design approach for the development of hydroxymethylnitrofurazone (NFOH) nanostructured lipid carrier for treating leishmaniasis

Cited by 10 publications

References 58 publications

The Development of Magnolol-Loaded Intravenous Emulsion with Low Hepatotoxic Potential

The Development of Magnolol-Loaded Intravenous Emulsion with Low Hepatotoxic Potential

Development of Oral Lipid Based Nano-formulation of Dapagliflozin: Optimization, <i>in vitro</i> Characterization and <i>ex vivo</i> Intestinal Permeation Study

Niclosamide nanoemulsion for colorectal cancer: development, physicochemical characterization, and in vitro anticancer activity

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