Optimization of LDL targeted nanostructured lipid carriers of 5-FU by a full factorial design

Andalib, Somayeh; Varshosaz, Jaleh; Hassanzadeh, Farshid; Sadeghi, Hojjat

doi:10.4103/2277-9175.100147

Cited by 25 publications

(6 citation statements)

References 14 publications

(16 reference statements)

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“…The first one is related to chemical nature and the degree of crystallinity between these lipids type and the drug used. 29 Another explanation highlights the variability of the melting point of the lipids used, since its effect on the viscosity of the lipid phase and thus on the energy required to break the emulsion particle to a smaller one, beeswax has a high melting point as compared to GMS and this means more power was needed to destruct such particle so large particle size can be predicted, a similar result was obtained by Sharifi et al 30…”

Section: Particle Size Analysismentioning

confidence: 58%

Impact of Lipid Type and Ratio in Rizatriptan Benzoate Nanostructured Lipid Carrier

Rajab¹,

Jawad²

2023

IJDDT

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Nanotechnology represents a magic wand to solve most problems related to improving drug effi ciency, one of the most important of these problems is the drug’s permeability through biological membranes. Rizatriptan benzoate was used for the treatment of acute migraine, it has poor permeability and is diffi cult to administer through the nose. This study aims to design a nanostructured lipid carrier containing rizatriptan benzoate as a trial to enhance its biological permeability. A high shear homogenization technique was utilized as a method of preparation; glyceryl monostearate and becs wax are used as solid lipids while oleic acid and castor oil were used as liquid lipids in diff erent ratios. Particle size analysis, polydispersity index, zeta potential, entrapment effi ciency, and loading effi ciency were considered the main criteria for the evaluation, meanwhile, the in-vitro release test was done for the formulas having smallest particle size. Moreover, the infrared spectroscopy and diff erential scanning calorimetry (DSC) are investigated for the selected formula. The obtained outcome revealed a signifi cant eff ect on the particle size and entrapment effi ciency upon enhancing the ratio of liquid lipid. Furthermore, changing the type of solid and liquid lipid leads to a dramatic alteration in the criteria of evaluation, also biphasic release pattern was seen. The infrared spectroscopy shows an intact rizatriptan benzoate, while DSC revealed a change of drug molecule to an amorphous state. In conclusion, a high shear homogenization can be used to formulate a successful nanostructured lipid carrier with good physical properties.

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Section: Particle Size Analysismentioning

confidence: 58%

Impact of Lipid Type and Ratio in Rizatriptan Benzoate Nanostructured Lipid Carrier

Rajab¹,

Jawad²

2023

IJDDT

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“…Most likely, this is because of the creation of many imperfections in the NLCs structure which provides more space to the drug entrapment. 38 …”

Section: Resultsmentioning

confidence: 99%

“…A slight decrease in size was observed with longer ultrasonication times, approaching the central value. [38][39][40]…”

Section: Impact Of Independent Variables On the Particle Size (Respon...mentioning

confidence: 99%

Pentapeptide cRGDfK-Surface Engineered Nanostructured Lipid Carriers as an Efficient Tool for Targeted Delivery of Tyrosine Kinase Inhibitor for Battling Hepatocellular Carcinoma

Deepak,

Kumar,

Pandey

et al. 2023

IJN

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Background Antitumor research aims to efficiently target hepatocarcinoma cells (HCC) for drug delivery. Nanostructured lipid carriers (NLCs) are promising for active tumour targeting. Cell-penetrating peptides are feasible ligands for targeted cancer treatment. Methods In this study, we optimized gefitinib-loaded NLCs (GF-NLC) for HCC treatment. The NLCs contained cholesterol, oleic acid, Pluronic F-68, and Phospholipon 90G. The NLC surface was functionalized to enhance targeting with the cRGDfK-pentapeptide, which binds to the αvβ3 integrin receptor overexpressed on hepatocarcinoma cells. Results GF-NLC formulation was thoroughly characterized for various parameters using differential scanning calorimetry and X-ray diffraction analysis. In-vitro and in-vivo studies on the HepG2 cell line showed cRGDfK@GF-NLC’s superiority over GF-NLC and free gefitinib. cRGDfK@GF-NLC exhibited significantly higher cytotoxicity, growth inhibition, and cellular internalization. Biodistribution studies demonstrated enhanced tumour site accumulation without organ toxicity. The findings highlight cRGDfK@GF-NLC as a highly efficient carrier for targeted drug delivery, surpassing non-functionalized NLCs. These functionalized NLCs offer promising prospects for improving hepatocarcinoma therapy outcomes by specifically targeting HCC cells. Conclusion Based on these findings, cRGDfK@GF-NLC holds immense potential as a highly efficient carrier for targeted drug delivery of anticancer agents, surpassing the capabilities of non-functionalized NLCs. This research opens up new avenues for effective treatment strategies in hepatocarcinoma.

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“…The proportion of drug and lipid was another important factor that affected the quality of nanoparticles. Larger proportions of drug to lipid resulted in increased DL%, but decreased EE% [22]. Therefore, using the weighted score of the two as the evaluation index can balance the contradiction.…”

Section: Discussionmentioning

confidence: 99%

Nanostructured lipid carriers loaded with morellic acid for enhanced anticancer efficacy: preparation, characterization, pharmacokinetics and anticancer evaluation

Jia

2024

Am J Cancer Res

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Morellic acid (MA), a typical compound found in Garcinia plants, is known for its anticancer properties. In present study, we isolated MA from resin of Garcinia hanburyi Hook. f. using preparative chromatography. We have successfully prepared MA-loaded nanostructured lipid carriers (MA-NLCs) and refined the production process via orthogonal testing. Optimization of the preparation process resulted in an average particle size of 165.50±1.70 nm with a PDI of 0.19±0.01. The EE% and DL% of MA-NLCs were 78.17±0.34% and 7.25±0.38%, respectively. The zeta potential of MA-NLCs was -21.85±0.67 mV. Comparatively, MA-NLCs showed a greater area under the curve (AUC) and an extended half-life (t1/2) than free MA. Pharmacokinetics analysis revealed that the AUC 0-t increased from 4.91±0.65 μg/mL•min (free MA) to 18.91±3.40 μg/mL•min (MA-NLCs) and the t 1/2 value for MA-NLCs was 7.93-fold longer than that of free MA. In vitro cytotoxic assessments indicated that MA formulations curtailed the proliferation of cancer cells. In vivo, MA-NLCs significantly inhibited the tumor growth in tumor-bearing mouse model. Molecular mechanism studies revealed that up-regulation of apaf-1 and activation of caspase-3, caspase-9 and GSDME by MA-NLCs may trigger to apoptosis and pyroptosis in cancer cells. Consequently, our findings support the potential of NLCs as an effective MA delivery system for the clinical management of cancer.

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Optimization of LDL targeted nanostructured lipid carriers of 5-FU by a full factorial design

Cited by 25 publications

References 14 publications

Impact of Lipid Type and Ratio in Rizatriptan Benzoate Nanostructured Lipid Carrier

Impact of Lipid Type and Ratio in Rizatriptan Benzoate Nanostructured Lipid Carrier

Pentapeptide cRGDfK-Surface Engineered Nanostructured Lipid Carriers as an Efficient Tool for Targeted Delivery of Tyrosine Kinase Inhibitor for Battling Hepatocellular Carcinoma

Nanostructured lipid carriers loaded with morellic acid for enhanced anticancer efficacy: preparation, characterization, pharmacokinetics and anticancer evaluation

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