Impact of lipid dynamic behavior on physical stability, in vitro release and skin permeation of genistein-loaded lipid nanoparticles

Andrade, Lígia Marquez; Reis, Carolina de Fátima; Maione-Silva, Lorena; Anjos, Jorge Luiz Vieira dos; Alonso, Antônio; Serpa, Rafael Caixeta; Marreto, Ricardo Neves; Lima, Eliana Martins; Taveira, Stephânia Fleury

doi:10.1016/j.ejpb.2014.04.015

Cited by 73 publications

(32 citation statements)

References 44 publications

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“…However, depending on the drug some potential problems can occur, such as drug leakage during storage and insufficient total drug load. Despite these statements, controversial results have been found in the literature about the differences between SLN and NLC (26). Comparing all nanoparticle formulations indicated that in the present study, the SP-NLCs are better than SP-SLNs in terms of dissolution rates, entrapment efficiency and physical stability.…”

Section: Resultsmentioning

confidence: 49%

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

et al. 2016

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Abstract.Stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) formulations to enhance the dissolution rates of poorly soluble drug spironolactone (SP) were being developed. Probe ultra-sonication method was used to prepare SLNs and NLCs. All NLCs contained stearic acid (solid lipid carrier) and oleic acid (liquid lipid content), whereas, SLNs were prepared and optimised by using the solid lipid only. The particles were characterised in terms of particle size analysis, thermal behaviour, morphology, stability and in vitro release. The zeta sizer data revealed that the increase in the concentration of oleic acid in the formulations reduced the mean particle size and the zeta potential. The increase in concentration of oleic acid from 0 to 30% (w/w) resulted in a higher entrapment efficiency. All nanoparticles were almost spherically shaped with an average particle size of about ∼170 nm. The DSC traces revealed that the presence of oleic acid in the NLC formulations resulted in a shift in the melting endotherms to a higher temperature. This could be attributed to a good long-term stability of the nanoparticles. The stability results showed that the particle size remained smaller in NLC compared to that of SLN formulations after 6 months at various temperatures. The dissolution study showed about a 5.1-to 7.2-fold increase in the release of the drug in 2 h compared to the raw drug. Comparing all nanoparticle formulations indicated that the NLC composition with a ratio of 70:30 (solid:liquid lipid) is the most suitable formulation with desired drug dissolution rates, entrapment efficiency and physical stability.

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Section: Resultsmentioning

confidence: 49%

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

et al. 2016

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“…The participation of liquid lipid creates an imperfect crystal matrix, resulting in high drug loading and physical stability. 19 Of note, lipolysis of lipid-based formulations, including NLCs, is an ineluctable process when they transport through the harsh gastrointestinal tract, which tends to give rise to erratic drug release and absorption. 20 Intensification of NLCs stability can diminish the in vivo transport variation and thus lead to a controllable drug release and high absorption percentage.…”

Section: Introductionmentioning

confidence: 99%

Selenium-coated nanostructured lipid carriers used for oral delivery of berberine to accomplish a synergic hypoglycemic effect

Yin¹,

Hou²,

Yin³

et al. 2017

IJN

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Diabetes mellitus is an incurable metabolic disorder that seriously threatens human health. At present, there is no effective medication available to defeat it. This work intended to develop selenium-coated nanostructured lipid carriers (SeNLCs) for enhancing the oral bioavailability and the curative effect of berberine, an antidiabetic phytomedicine. Berberine-loaded SeNLCs (BB-SeNLCs) were prepared by hot-melt dispersion/homogenization procedure followed by in situ reduction. BB-SeNLCs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Pharmacokinetics of berberine solution, berberine-loaded NLCs (BB-NLCs) and BB-SeNLCs were studied in Sprague Dawley rats administered by oral gavage. The prepared BB-SeNLCs were around 160 nm in particle size with an EE of 90%. In addition, BB-SeNLCs exhibited a better sustained release of berberine compared to the plain NLCs. After oral administration, BB-SeNLCs greatly enhanced the oral bioavailability of berberine, which was approximately 6.63 times as much as that of berberine solution. The hypoglycemic effect of BB-SeNLCs was also significantly superior to that of BB-NLCs and berberine solution. It turned out that sustained drug release and good intestinal absorption, plus the synergy of selenium, were basically responsible for enhanced oral bioavailability and hypoglycemic effect. Our findings show that SeNLCs are promising nanocarriers for oral delivery of berberine to strengthen the antidiabetic action.

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“…The addition of oil increased superficial fluidity, which would indicate that the oil (capric and caprylic triglycerides) could probably be accommodated in this region. In fact, recent studies undertaken by our research group with unloaded SLN and NLC (with the same lipid and surfactant mixture as described here) have also demonstrated that SLN are slightly more rigid than the NLC with low oil content (12.5 %), due to a 1.5 G reduction in 2A // values (Andrade et al 2014). In addition, 2A // values of PAC-loaded SLN and NLC1 were higher than the values of unloaded nanoparticles (Andrade et al 2014), suggesting that PAC has a certain effect on lipid matrix fluidity.…”

Section: Stability Studiesmentioning

confidence: 56%

“…In an earlier study undertaken by our research group, the presence of 12.5 % of oil in lipid matrices increased nanoparticle flexibility as well as drug (genistein) skin permeation (Andrade et al 2014). So with a view to verifying the influence of increasing amounts of oil on matrix fluidity and PAC skin permeation, this present study was carried out.…”

Section: Resultsmentioning

confidence: 96%

“…The ethanol concentration (less than 2 %) did not significantly alter the fluidity of the lipid nanoparticles. In order to remove the excess surfactant micelles, before the spin labeling process, the samples of SLN and NLC dispersions were diluted in ultra-pure water at a ratio of 1:25, and the initial volume of the samples was recovered by ultrafiltration (Andrade et al 2014). Finally, the dispersions were introduced into a capillary tube, which was sealed by flame for EPR measurements.…”

Section: Electron Paramagnetic Resonance (Epr) Spectroscopy Measurementsmentioning

confidence: 99%

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Paclitaxel-loaded lipid nanoparticles for topical application: the influence of oil content on lipid dynamic behavior, stability, and drug skin penetration

et al. 2014

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Paclitaxel (PAC) has shown potential for regulating hyperkeratosis in skin diseases and its encapsulation in lipid nanoparticles could improve topical treatments. So, solid lipid nanoparticles (SLN) and nanostructured lipid carriers with 12.5 % (NLC1) and 25 % (NLC2) oil content were obtained and characterized. Lipid dynamic behavior was investigated through electron paramagnetic resonance spectroscopy (EPR) and comparative evaluations of EPR, and stability and skin permeation studies were performed. High entrapment efficiency was obtained for all formulations (over 90 %). The absence (SLN) or addition of 12.5 % oil (NLC1) did not significantly alter nanoparticle mean diameter, but 25 % oil (NLC2) produced smaller particles (270.6 ± 13.5 nm). EPR studies showed that 12.5 % oil increased NLC1 fluidity at the surface. Surprisingly, more oil increased NLC2 superficial rigidity, due to the decrease in nanoparticle mean diameter and additional PAC accumulation in the superficial environment. The oil in lipid matrices improved the physicochemical stability of NLC formulations, and drug-oil chemical affinity prevented PAC expulsion during storage time. NLC2 improved PAC skin penetration and was the only formulation capable of enhancing PAC penetration to deeper skin layers (about 6.48 ± 1.39 lg/cm 2 ). PAC-NLC2 seemed to be very promising nanocarriers for the topical delivery of PAC.Keywords Paclitaxel Á Solid lipid nanoparticles Á Nanostructured lipid carriers Á Skin permeation Á Lipid dynamic behavior and electron paramagnetic resonance spectroscopy

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Impact of lipid dynamic behavior on physical stability, in vitro release and skin permeation of genistein-loaded lipid nanoparticles

Cited by 73 publications

References 44 publications

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

Selenium-coated nanostructured lipid carriers used for oral delivery of berberine to accomplish a synergic hypoglycemic effect

Paclitaxel-loaded lipid nanoparticles for topical application: the influence of oil content on lipid dynamic behavior, stability, and drug skin penetration

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