Curcumin Containing PEGylated Solid Lipid Nanoparticles for Systemic Administration: A Preliminary Study

Abstract

<jats:p>Curcumin (CUR) has a wide range of pharmacological properties, including anti-inflammatory and antioxidant activities, and it can be considered a good candidate for the potential treatment of central nervous system (CNS) pathologies, although its use in clinical practice is compromised due to its high lipophilicity. Solid lipid nanoparticles (SLNs) are well-known nanocarriers representing a consolidated approach for the delivery of lipophilic compounds, but their systemic use is limited due their short half-life. The formulation of stealth SLNs (pSLNs) could be a valid strategy to overcome this limit. Curcumin-loaded-pSLNs were prepared by the solvent evaporation method. Formulation was characterized for their mean size, zeta potential, size distribution, and morphology. Drug antioxidant activity was evaluated by Oxygen Radical Absorbance Capacity (ORAC) assay. Finally, the obtained formulations were analyzed in terms of long-term stability. Curcumin-loaded-pSLNs showed good technological parameters with a mean particle size below 200 nm, as confirmed by TEM images, and a zeta potential value around −30 mV, predicting good long-term stability. Differential Scanning Calorimetry (DSC) analysis confirmed that PEG micelles interacted with the SLN surface; this suggests the location of the PEG on the pSLN surface. Therefore, these preliminary studies suggest that the produced formulation could be regarded as a promising carrier for the systemic administration.</jats:p>

Curcumin Loaded Polymeric vs. Lipid Nanoparticles: Antioxidant Effect on Normal and Hypoxic Olfactory Ensheathing Cells

“…Cur-PNP and Cur-SLN were cryoprotected with glucose being a suitable excipient for both lipid and polymeric nanosuspensions [ 77 , 78 ].…”

Solid Lipid Nanoparticles as Carriers of Natural Phenolic Compounds

“…Santonocito et al prepared functionalized curcumin-loaded SLNs by solvent emulsification/evaporation technique for the systemic administration of curcumin [ 81 ]. Curcumin, Compritol 888 ATO and injectable soy lecithin were solubilized and melted in ethanol at 70 °C.…”

“…Curcumin, Compritol 888 ATO and injectable soy lecithin were solubilized and melted in ethanol at 70 °C. The melted lipid phase was dispersed in the hot surfactant solution (Lutrol F68) under stirring and then this solution was cooled in an ice bath and the organic solvent was removed by vacuum [ 81 ]. Small particles sizes can be obtained using this methodology due to the good solubilization of the lipid in the organic solvent, with the absence of any thermal stress or heat being a great advantage towards HPH.…”

“…Moreover, PEG chains are cleaved by matrix metalloproteinases, which allows for their efficient application in tumor cells where the concentration of these proteinases is increased in surrounding areas [ 114 ]. Several studies have even taken advantage on the functionalization with PEG chains and have combined it with other targeting molecules such as carboxylic acids or amines present in different targeting ligands [ 81 , 101 , 108 , 115 , 116 ].…”

Oxidative Stress Boosts the Uptake of Cerium Oxide Nanoparticles by Changing Brain Endothelium Microvilli Pattern

“…The use of antioxidant compounds for the management of neurodegenerative diseases is mainly limited by poor bioavailability, enzymatic degradation and scarce BBB crossing [ 14 , 15 ]. To overcome these issues, nanovectors for the delivery of antioxidants and inorganic nanoparticles (NPs) as free radical scavenger themselves have been proposed [ 14 , 16 , 17 , 18 ].…”