Preparation, characterization and in vivo pharmacokinetic evaluation of curcuminoids-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs)

Curcuminoids are considered as one of the most promising phytochemicals with numerous pharmacological effects and therapeutic potentials. Nevertheless, their inappropriate pharmacokinetic properties (i.e., poor bioavailability) have made pharmaceutical industries face many challenges in developing an efficient formulation. To address this issue, we designed curcuminoids-loaded solid lipid nanoparticles (CUR-SLNs) and nanostructured lipid carriers (CUR-NLCs) using high shear homogenization and ultrasound technique.

The optimized SLNs and NLCs formulations exhibited average particle sizes of 160.7 $\pm$ 2.69 and 151.4 $\pm$ 3.54 nm, respectively. The encapsulation efficiency of CUR-SLNs and CUR-NLCs were 95.30% $\pm$ 1.71 and 97.37% $\pm$ 2.83. Transmission electron microscopy imaging revealed the spherical shape of the lipid nanoparticles. Differential scanning calorimetry (DSC) studies showed an amorphous state of the curcuminoids incorporated into the nanoparticles.

Furthermore, pharmacokinetic studies that were conducted to prove the absorption enhancing effect of the developed formulations, demonstrated significant improvement in pharmacokinetic parameters including area under the concentration-time curve (AUC) and maximum plasma concentration (Cmax) of the nanocarriers in comparison with free curcuminoids. The results suggested that SLNs and nanomicellar formulations, as compared to NLCs, were better functioned at boosting the pharmacokinetic properties of curcuminoids.

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Article information: Shabnam Dolatabadi, Maryam Karimi, Samira Nasirizadeh, Mahdi Hatamipour, Shiva Golmohammadzadeh, Mahmoud Reza Jaafari. Preparation, characterization and in vivo pharmacokinetic evaluation of curcuminoids-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), Journal of Drug Delivery Science and Technology, 2021. https://doi.org/10.1016/j.jddst.2021.102352.