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Characterization and Properties of Solid Lipid Nanoparticles Modified with Polyethylene Glycol-2000-1, 2-Distearoyl-Sn-Glycero-3-Phosphoethanolamine

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To improve the physicochemical and pharmacokinetic properties, solid lipid nanoparticles (SLNs) modified with (Polyethylene glycol-2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine (PEG2000-DSPE) were prepared using glyceryl monostearate as a lipid carrier and resveratrol as a model drug. Compared to ordinary SLNs, SLNs doped with low amount of PEG2000-DSPE [m(PEG2000-DSPE):m(lipids) = 1:5, w/w] exhibited improved physicochemical and pharmacokinetic properties, including higher entrapment efficiency (above 80%), smaller particle size (approximately 100 nm), more distinguished drug release at low pH values (pH < 6.0), and longer drug circulation in vivo. According to the characterizations performed, the DSPE moiety was doped into lipid matrix to form a PEG2000-DSPE/lipid eutectic dopant, inhibiting lipid polymorphism transformation from α-form to β-form, thereby preventing drug expulsion from the lipid. The dopant contained lattice defects, allowing for the incorporation of more resveratrol. Resveratrol was released in a sustained and pH-sensitive pattern due to nanoparticles destabilization induced by partial protonation of PEG2000-DSPE. PEG chains distributed on the nanoparticle surface caused steric hindrance and “stealth” properties, thus maintaining dispersion stability and extending circulation time of nanoparticles. These results confirm that PEG2000-DSPE modification effects are attributable to the matrix and surface structures of nanoparticles, which consist of a core containing DSPEinduced lattice defects and a shell coated with PEG chains.
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Document Type: Research Article

Publication date: August 1, 2016

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  • Science of Advanced Materials (SAM) is an interdisciplinary peer-reviewed journal consolidating research activities in all aspects of advanced materials in the fields of science, engineering and medicine into a single and unique reference source. SAM provides the means for materials scientists, chemists, physicists, biologists, engineers, ceramicists, metallurgists, theoreticians and technocrats to publish original research articles as reviews with author's photo and short biography, full research articles and communications of important new scientific and technological findings, encompassing the fundamental and applied research in all latest aspects of advanced materials.
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