Abstract:
Chitosan (Ch)-coated nanostructured lipid carriers (NLCs) have great potential for topical delivery with high localization of chemotherapeutics. In this study, tetrahydrocurcumin (THC), a primary metabolite of curcumin with enhanced antioxidant and anticancer properties, was used as a model drug to prepare NLCs. Response surface methodology was employed to optimize THC-loaded Ch-coated NLCs (THC-Ch-NLCs) fabricated by high-shear homogenization. The optimized THC-Ch-NLCs had particle size of 244 ± 18 nm, zeta potential of -17.5 ± 0.5 mV, entrapment efficiency of 76.6 ± 0.2% and drug loading of 0.28 ± 0.01 mg/mL. In vitro release study of THC-Ch-NLCs showed sustained release following the Korsmeyer-Peppas model with Fickian diffusion mechanism. THC-Ch-NLCs demonstrated a significantly higher permeation through the artificial membrane than the THC-NLCs. Furthermore, THC-Ch-NLCs also exhibited cytotoxicity against TNF-α-induced HaCaT cell lines. However, the findings need further investigation to prove that the cytotoxicity is due to the encapsulation of THC in the Ch-NLC since the same effect is also observed in the blank lipid-nanoparticles.
