<p>The effect of surface treatment on the brain delivery of curcumin nanosuspension: in vitro and in vivo studies</p>

Abstract

Background: Curcumin, a bioactive component with multiple characteristics, has been shown to have many therapeutic effects. However, there are several limitations regarding the use of curcumin such as instability, low solubility, poor bioavailability, and rapid elimination. Different approaches have been used to solve these problems. Materials and methods: In this study, surface-modified nanosuspension (NS) is investigated as a novel brain delivery system. Two different methods were used for the preparation of nanosuspensions with two different stabilizers. The surface of the nanosuspensions was coated with D-α-tocopheryl polyethylene glycol 1,000 succinate (TPGS) and Tween 80 using physical adsorption. Curcumin NSs were prepared using two different top-down techniques by high-pressure homogenizer and probe sonicator. A validated sensitive and selective high-performance liquid chromatography method using fluorescence detection was used for the determination and quantification of curcumin. Pharmacokinetics and biodistribution of curcumin NSs and solutions after intravenous administration in rats were studied. Results: Higher levels of curcumin in the brain were detected when Tween 80-coated NS was used compared with the curcumin solution and TPGS coated NS (TPGS-NS) ( P -value<0.05). Absorption of ApoE and/or B by Tween 80-coated nanoparticles (NPs) from the blood were caused transferring of these NPs into the brain using receptor-mediated endocytosis. Distribution of TPGS-NS in the brain compared with the curcumin solution was higher ( P -value<0.05). Higher levels of curcumin concentration in the liver, spleen, and lung were also observed with TPGS-NS. Conclusion: The results of this study indicate that the surface-coating of NSs by Tween 80 may be used to improve the biodistribution of curcumin in the brain.

Precision and Advanced Nano-Phytopharmaceuticals for Therapeutic Applications

“…Curcumin nanosuspensions, consisting of stable nanoscale droplets of the compound with surfactants and biopolymers, improved solubilization and increased intravenous plasma distribution to vital organs compared with standard curcumin. Higher levels of curcumin in male Wistar rat brains were discovered when delivered via Tween 80-coated nanoparticles (NPs) in comparison to curcumin solution [37]. The mechanism of action exerted by curcumin in neuroblastoma cells involved the regulation of PTEN-Akt (phosphatase and tensin homolog-protein kinase B), NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells), and p53 (tumor protein P53), signaling, activation of the apoptosis cascade, and mitochondrial dysfunction [36].…”

Curcumin’s Beneficial Effects on Neuroblastoma: Mechanisms, Challenges, and Potential Solutions

“…TPGS-NS and Tween-NS exhibit rapid and complete dissolution in phosphate-buffered saline, compared to the slower and incomplete dissolution of pure curcumin. Moreover, the IV administration of these nanosuspensions increases curcumin concentrations in the plasma, brain, heart, and digestive system in comparison to standard curcumin at 10 mg/kg [ 112 ].…”

Advanced modification of drug nanocrystals by using novel fabrication and downstream approaches for tailor-made drug delivery

“…For example, Paclitaxel nanosuspension with TPGS significantly prevented the drug resistant of P-gp for H460 human cancer cells and was observed five times higher tumor inhibition than the paclitaxel solution (Gao et al., 2014). Tween 80 as the nanosuspension stabilizer could contribute to the transportation of curcumin to brain in the way of receptor-mediated endocytosis (Dibaei et al., 2019). In a recent study, the charges of stabilizers were proven the effect on the mucoadhesiveness and permeation of cell monolayers, which confirmed that positively charged nanosized clarithromycin was observed better mucoadhesiveness than the not charged and the negatively charged nanocrystals, and both charged nanocrystals reflected an improved drug delivery compared to the uncharged (Soisuwan et al., 2019).…”