Preparation and evaluation of lipid emulsified docetaxel-loaded nanoparticles

Abstract

Abstract Objectives Lipid emulsified nanoparticles (LPNPs) have been developed to load anticancer drug docetaxel (DTX) in this work. Methods We evaluated DTX-loaded lipid emulsified nanoparticles (DTX-LPNPs) in vitro compared with the conventional nanoparticles (DTX-NPs). The newly developed formulation was compared with DTX-NPs in terms of physicochemical properties and in-vitro efficacy. Key findings These two formulations had similar physicochemical properties in our results. And it has been proven that phosphatidylethanolamine had higher emulsification efficiency (20-fold of polyvinyl alcohol) in the same preparation procedure. The in-vitro release of DTX from DTX-LPNPs showed burst release initially and then followed by a sustained release, which prolonged the half time. The cytotoxicity test indicated that the DTX-LPNPs were more effective against tumour growth, and the IC50 of Duopafei, DTX-NPs and DTX-LPNPs for the inhibition of human lung cancer A549 cells at 48 h (n = 3) were found to be 3.53 ± 0.43, 1.15 ± 0.06 and 0.55 ± 0.08 μm, respectively. The evaluation of the cellular uptake showed that DTX-LPNPs improved the drug delivery into cytoplasm compared with the commercial product Duopafei and DTX-NPs. Conclusions DTX-LPNPs may be a promising formulation for cancer therapy.