Solid lipid nanoparticle

About: Solid lipid nanoparticle is a research topic. Over the lifetime, 3175 publications have been published within this topic receiving 127912 citations. The topic is also known as: LNP & SLN.

Preparation and stability of astaxanthin solid lipid nanoparticles based on stearic acid

Abstract: Astaxanthin (ASTA), a natural pigment carotenoid, is endowed with remarkable antioxidant activity in food and cosmetic products. However, the utilization of ASTA is limited due to its poor water-solubility, low bioavailability, and the decomposition under light, heat, and oxygen. In order to overcome these drawbacks, ASTA was encapsulated within solid lipid nanoparticles (SLNs). ASTA-SLNs, composed of lipid nucleation (ASTA, soybean oil, solid lipid matrix) and external water phase (Tween 20, deionized water), were prepared by high pressure homogenization (HPH). The contents of three different solid matrixes (stearic acid, glycerin monostearate, and glycerol distearates) and the preparation conditions (pressure and number of cycles) were optimized. Stearic acid (1 wt%) was selected on the basis of physico-chemical properties of ASTA-SLNs, such as mean particle size, zeta potential, and polydispersivity index (PDI). Moreover, ASTA-SLNs exhibited good long-term stability at 4 and 25°C, with no significant modification in the particle size. Comparative with the free ASTA, the chemical stability of ASTA in SLNs was significantly enhanced. Finally, the release experiments of ASTA-SLNs showed that SLNs could provide prolonged release of ASTA in simulated gastric and intestinal juices. Practical application: SLNs, a promising submicron drug delivery system, could be widely applied in food, cosmetics, drugs, and health products. In the fields of targeted delivery and controlled release of drugs, SLNs have attracted increasing attention. ASTA-SLNs can be prepared into various pharmaceutical dosage forms, such as oral tablet, intravenous infusion, and percutaneous absorption, thus achieving a long-time and stable therapeutic effect in small dosage. More importantly, based on the high pressure homogenization technology, ASTA-SLNs can be produced in large-scale. Astaxanthin solid lipid nanoparticles (ASTA-SLNs) were produced using high pressure homogenization. Internal lipid phase was prepared by adding the solid lipid matrix and ASTA into soybean oil with heating and stirring under a nitrogen atmosphere. External aqueous phase was prepared by dispersing Tween 20 (10% w/w) in deionized water. ASTA-SLNs were obtained through dispersion, high pressure homogenization, and refrigeration. The physical characteristics, stability, release behavior of ASTA-SLNs were measured.

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

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.

Nose to brain delivery of astaxanthin-loaded solid lipid nanoparticles: fabrication, radio labeling, optimization and biological studies

Abstract: The present study was carried out to investigate the intranasal delivery of astaxanthin as solid lipid nanoparticles with the intention of improving brain targeting of astaxanthin for neurological disorders. The astaxanthin solid lipid nanoparticles were prepared by a double emulsion solvent displacement method. Statistical analysis using response surface methodology showed that the optimum values of stearic acid (50 mg), drug weight percentage (6.11%) and ratio of surfactant to co-surfactant (poloxamer 188 : lecithin-1 : 6) resulted in a 213.23 nm particle size and 0.367 polydispersity index for the astaxanthin solid lipid nanoparticles. Radio labeling studies were performed using technetium-99m to evaluate the biodistribution pattern after administration through different routes in experimental subjects. Radiolabeled nanoparticles were found to be 96–98% stable even after 48 h of labeling in phosphate-buffered saline (pH 7.4). Comparative biodistribution data indicated that the higher drug concentration in the brain was achieved by intranasal administration of 99mTc labeled astaxanthin solid lipid nanoparticles as compared to the intravenous route, which was also confirmed by gamma scintigraphy analysis. Furthermore, studies on the pheochromocytoma-12 cell line demonstrated the antioxidant potential of astaxanthin solid lipid nanoparticles against H2O2 induced toxicity. Our findings strongly emphasize that nanoparticle-based nasal drug delivery of astaxanthin could impart the utmost neuroprotection from oxidative stress in neurological disorders under in vitro conditions.

A review of the application of lipid-based systems in systemic, dermal/ transdermal, and ocular drug delivery.

Abstract: The introduction of combinatorial chemistry and the development of high-throughput techniques has significantly increased the amount of new active lipophilic molecular entities. As a result, the need for successful delivery of these lipophilic active compounds has also increased. One such method of delivery is through the use of advanced lipid-based drug delivery systems. Traditionally, the majority of reviews of lipid-based drug delivery systems were based on the oral administration field only. This review article focuses on the use of lipids in parenteral, dermal/ transdermal, and ocular drug delivery systems. Specific needs, considerations, approaches, and limitations in lipid-based drug delivery are discussed herein on the basis of the anatomical and physiological diversity of the target organs and systems.