Characterization and Body Distribution ofβ-Elemene Solid Lipid Nanoparticles (SLN)

Abstract

Solid lipid nanoparticles (SLN) containing beta-elemene, a volatile oil used for the treatment of cancer, were prepared by the method combining probe sonication and membrane extrusion. Effects of the formulations and procedures on the characteristics of SLN were investigated. Body distribution of beta-elemene SLN in rats after intravenous administration was compared with that of the commercial emulsion. The results showed that dispersing the surfactant in the melted lipid matrix could obtain smaller particles than that dispersing in the water phase. Increasing the ratio of monostearin in the lipid matrix or the concentration of surfactant reduced the mean volume size of the SLN. Optimized formulation was composed of monostearin and precirol ATO 5 at a mass ratio of 3:7, which was quite stable for 8 months at room temperature. In vitro release of beta-elemene from the SLN was slow and stable without obvious burst release and was found to follow the Higuich equation. After intravenous administration, the beta-elemene levels after 5 min injection of SLN formulation were 1.5, 2.9, and 1.4 times higher than those of beta-elemene emulsion in liver, spleen, and kidney, respectively, while the concentrations of beta-elemene were decreased 30% in heart and lung. Therefore, the SLN containing beta-elemene might be an attractive candidate for the treatment of liver cancer.

β-elemene inhibits monocyte–endothelial cells interactions via reactive oxygen species/MAPK/NF-κB signaling pathway in vitro

“…1A), a sesquiterpenes compound extracted from the Curcuma Wenyujin (Guo, 1983), is a traditional Chinese herbal medicine that has been shown to inhibit tumor cell growth in vivo and in vitro. Because of its proven safety, this compound has been applied in clinics for the treatment of malignant effusions and some solid tumors (Li et al, 2005;Wang et al, 2005a;Wang et al, 2005b). Previous studies have shown that β-elemene derivatives have a significant antioxidant activity and cytoprotective effects against oxidative damage in HUVECs (Chen et al, 2014).…”

An investigation of the ability of elemene to pass through the blood-brain barrier and its effect on brain carcinomas

“…In 1993, β‐elemene was officially approved as an anti‐cancer drug in China. After that, injectable emulsions of β‐elemene were used for the first‐line treatment of pleural malignancies, chest and abdominal ascites, malignant brain tumours and cancers of the respiratory and digestive tracts, and for the second‐line treatment of cancers of female reproductive organs, breast cancer, metastatic bone cancer, skin cancer, lymphoma and leukaemia 4–6 . However, little is known regarding the tissue distribution of elemene.…”

Preparation, characterization and biocompatibility studies on risperidone-loaded solid lipid nanoparticles (SLN): High pressure homogenization versus ultrasound

“…Alternatively, several other processes have been used for the production of these systems, in order to attempt cheaper and easier ways of production, e.g., ultrasound technique (US) and solvent-based techniques [4][5][6][7][8][9]. However, all these techniques have some drawbacks [10,11]: the use of US to obtain nanoparticles requires long sonication times, which improves the risk of metal contamination from the probe; the presence of highly polydisperse formulations, with a large amount of microparticles can be a problem for some administration routes; the total removal of the solvents used in solvent-dependent techniques is very difficult.…”