Development and evaluation of lipid nanoparticles for paclitaxel delivery: a comparison between solid lipid nanoparticles and nanostructured lipid carriers

Abstract

Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared as delivery system for water-insoluble anticancer agent, paclitaxel (PTX). The dispersion of SLNs was consisted of 5 % w/w tristearin, 3.75 % w/w egg phosphatidylcholine (egg PC) and 1 % w/w polysorbate 80 in water. NLCs were prepared using the same composition as SLNs except that 10 % of the solid lipid was replaced by triolein. PTX was incorporated into SLNs and NLCs to attain 0.025 % w/w in the dispersion. The particle size of the prepared SLNs and NLCs were 167.9 ± 21.3 and 121.9 ± 28.3 nm, respectively, and slightly increased to 239.1 ± 32.6 and 183.6 ± 36.2 nm by PTX incorporation. PTX incorporation also increased polydispersity index suggesting broader size distribution compared to that for empty particles. SLNs and NLCs showed sustained release of PTX in cell culture media containing 10 % fetal bovine serum at 37 °C compared to the commercial micellar formulation consisted of Cremophor EL and ethanol. PTX in SLNs and NLCs showed comparable cytotoxicity to the commercial formulation and free PTX against human breast cancer cell line, MCF-7. On the contrary, PTX in SLNs and NLCs showed higher anticancer activity against multidrug resistant (MDR) cancer cell line, MCF-7/ADR, compared to the free PTX delivered in DMSO, which indicates that both SLNs and NLCs would be effective carriers to avoid efflux pump expressed in MDR cancer cells. In conclusion, the SLNs and NLCs prepared in the present study showed similar characteristics each other and both can be used as effective delivery system for PTX.