Preparation, Characterization, Pharmacokinetics and Tissue Distribution of Solid Lipid Nanoparticles Loaded with Tetrandrine

Abstract

Abstract. Tetrandrine (TET) is a poorly water-soluble bisbenzylisoquinoline alkaloid. In this study, TET solid lipid nanoparticles (SLNs) were prepared by a melt-emulsification and ultrasonication technique. Precirol ® ATO 5, glyceryl monostearate, and stearic acid were used as the lipid matrix for the SLNs, while Lipoid E80, Pluronic F68, and sodium deoxycholate were used as emulsifying and stabilizing agents. The physicochemical characteristics of the TET-SLNs were investigated when it was found that the mean particle size and zeta potential of the TET-SLNs were 134±1.3 nm and −53.8±1.7 mV, respectively, and the entrapment efficiency (EE) was 89.57%±0.39%. Differential scanning calorimetry indicated that TET was in an amorphous state in SLNs. TET-SLNs exhibited a higher release rate at a lower pH and a lower release rate at a higher pH. The release pattern of the TET-SLNs followed the Weibull model. The pharmacokinetics of TET-SLNs after intravenous administration to male rats was studied. TET-SLN resulted in a higher plasma concentration and lower clearance. The biodistribution study indicated that TET-SLN showed a high uptake in reticuloendothelial system organs. In conclusion, TET-SLNs with a small particle size, and high EE, can be produced by the method described in this study. The SLN system is a promising approach for the intravenous delivery of tetrandrine.

Mixed Polyethylene Glycol-Modified Breviscapine-Loaded Solid Lipid Nanoparticles for Improved Brain Bioavailability: Preparation, Characterization, and In Vivo Cerebral Microdialysis Evaluation in Adult Sprague Dawley Rats

“…Although there were no breviscapine characteristic exothermic peaks in the thermogram for breviscapine/palmitic acid solid dispersion, palmitic acid could not be used for the SLN formulation. This was because it failed to yield a stable nanoparticle formulation in the onefactor experiments for all conditions tested and flocculated within 1 h. Similar observation was reported by Li et al (27) where the drug solubility of tetrandrine was high in palmitic acid, but the formulation was unstable.…”

Effect of nanoparticles binding ß-amyloid peptide on nitric oxide production by cultured endothelial cells and macrophages

“…Exposure to solid lipid nanoparticles or PA-SLN at the range of concentrations previously used in vivo 37,38 resulted in decreased viability of HUVECs, which was not mediated by apoptosis, and increased production of nitric oxide only at the highest doses. Further, excessive production of nitric oxide and distress was seen in the macrophages after exposure to the solid lipid nanoparticles.…”

SLNs can Serve as the New Brachytherapy Seed: Determining Influence of Surfactants on Particle Size of Solid Lipid Microparticles and Development of Hydrophobised Copper Nanoparticles for Potential Insertion

“…Many scientists use the term nano to refer to sizes of less than 100 nm. They consist of a biocompatible solid lipophillic matrix, covered by a phospholipid monolayer coating [1,2]. Drug particles can either be dissolved or dispersed in the lipid matrix or concentrated in the inner and/or outer shell, providing different drug-release kinetic profiles ( Figure 1).…”