Abstract
Despite the promising biological and antioxidant properties of curcumin, its medical applications are limited due to poor solubility in water and low bioavailability. Polymeric nanoparticles (NPs) adapted to oral delivery may overcome these drawbacks. Properties such as particle size, zeta potential, morphology and encapsulation efficiency were assessed. Then, the possibility of storing these NPs in a solid-state form obtained by freeze-drying, in vitro curcumin dissolution and cytocompatibility towards intestinal cells were evaluated. Curcumin-loaded Eudragit® RLPO (ERL) NPs showed smaller particle diameters (245 ± 2 nm) and better redispersibility after freeze-drying than either poly(lactic-co-glycolic acid) (PLGA) or polycaprolactone (PCL) NPs. The former NPs showed lower curcumin encapsulation efficiency (62%) than either PLGA or PCL NPs (90% and 99%, respectively). Nevertheless, ERL NPs showed rapid curcumin release with 91 ± 5% released over 1 h. The three curcumin-loaded NPs proposed in this work were also compatible with intestinal cells. Overall, ERL NPs are the most promising vehicles for increasing the oral bioavailability of curcumin.
Highlights
Curcumin, or diferuloylmethane [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione; molecular weight 368.37 g/mol] is a natural polyphenol isolated from the rhizome of turmeric (Curcuma longa), a member of the ginger family (Zingiberaceae)
Polymer specifications according to manufacturers’ data are presented in Table 1 and FTIR spectra of PCL, poly-(lactic-co-glycolic acid) (PLGA) and Eudragit® RLPO (ERL) are shown in the Supplementary Materials (Figure S1)
Due to the chemical reactivity/instability of curcumin, a method of NP preparation that involves dispersion of preformed polymers is more appropriate than polymerization
Summary
Diferuloylmethane [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione; molecular weight 368.37 g/mol] is a natural polyphenol isolated from the rhizome of turmeric (Curcuma longa), a member of the ginger family (Zingiberaceae). This popular spice is used for the treatment of inflammation, as a tonic and a blood purifier in traditional Indian (Ayurveda) and Chinese medicine [1,2,3]. Curcumin displayed antioxidant properties in vitro through free radical scavenging by the phenolic and methoxy groups on benzene rings and β-diketone [1,2,4]. It has been shown that curcumin inhibits the expression of TNF-α-induced pro-inflammatory cytokines, such as IL-1β, IL-6 in TNF-α-treated HaCaT cells (immortalized human keratinocytes) and inhibits the expression of TNF-α-induced cyclin E [5]
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