Polymeric Nanoparticles for Increasing Oral Bioavailability of Curcumin

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.

Improvement of Curcumin Bioavailability for Medical Applications

“…Nonetheless, the encapsulation efficiency of curcumin-Eudragit ® RLPO NPs was the lowest, 62%, whereas that of curcumin-PLGA NPs and curcumin-polycaprolactone NPs were 90 and 99%, respectively. In vitro experiments demonstrated that curcumin-loaded Eudragit ® RLPO NPs release 91 ± 5% of their curcumin over 1 h, whereas PLGA NPs and polycaprolactone NPs released only 55 ± 2% and 47 ± 2%, respectively, after 24 h. The authors point out that the polycationic Eudragit ® RLPO NPs could improve the oral bioavailability of curcumin due to its mucoadhesive properties and rapid curcumin release [127]. Additionally, curcumin has also been encapsulated in natural polymers, such as chitosan and gelatin.…”

Freeze drying of polyelectrolyte complex nanoparticles: Effect of nanoparticle composition and cryoprotectant selection

“…Freeze drying of polyelectrolyte complex NPs presents a particular challenge, as they are mainly stabilised by charge, thus susceptible to changes in the medium parameters (pH and ionic strength) (Cegnar et al, 2011), their shape/structure is less defined (Umerska et al, 2014b) as opposed to e.g. poly(lactic-co-glycolic) acid-based NPs and are surfactant-free formulations and surfactants such as polyvinyl alcohol can act as cryo-/lyo-protectants and facilitate redispersibility of the NPs (Umerska et al, 2018). For PEC NPs, freeze drying of chitosan-based NPs has been studied (Rampino et al, 2013), including alginate/chitosan (Cegnar et al, 2011) and hyaluronate-coated chitosan NPs (Veilleux et al, 2018), but not other types of PEC NPs.…”

Preparation and characterization of novel anti-inflammatory biological agents based on piroxicam-loaded poly-ε-caprolactone nano-particles for sustained NSAID delivery

“…The DSC curves indicate good thermal properties, despite a change in its thermal stability after adding collagen. that during the different stages of NP formulation, such as the purification step, material transfer is required that can cause NP loss (Umerska et al, 2018). Hence, it is necessary to calculate NP recovery, which is also called the NP yield.…”