5-Fluorouracil shell-enriched solid lipid nanoparticles (SLN) for effective skin carcinoma treatment

The effective treatment of skin carcinoma is warranted for targeting the chemotherapeutic agents into tumor cells and avoiding unwanted systemic absorption.

This work was dedicated to the purpose of engineering highly penetrating shell-enriched nanoparticles that were loaded with a hydrophilic chemotherapeutic agent, 5-fluorouracil (5-FU).

Varying ratios of lecithin and poloxamer188 were used to produce shell-enriched nanoparticles by enabling the formation of reversed micelles within this region of the SLN. The localization of 5-FU within the shell region of the SLN, was confirmed using 5-FU nanogold particles as a tracer. SLN were introduced within sodium carboxy methylcellulose hydrogel, and then applied onto the skin of mice-bearing Ehrlich's ascites carcinoma. The mice were treated with the gel twice daily for 6 weeks.

The transmission electron microscope (TEM) revealed the formation of uniform nanoparticles, which captured reversed micelles within their shell region. The SLNs' had particle size that ranged from 137 ± 5.5 nm to 800 ± 53.6, zeta potential of -19.70 ± 0.40 mV and entrapment efficiency of 47.92 ± 2.34%. The diffusion of the drug-loaded SLN (269.37 ± 10.92 μg/cm²) was doubled when compared with the free drug (122 ± 3.09 μg/cm²) when both diffused through a hydrophobic membrane. SLN-treated mice exhibited reduced inflammatory reactions, with reduced degrees of keratosis, in addition to reduced symptoms of angiogenesis compared to 5-FU-treated mice.

SLN possesses the capacity to be manipulated to entrap and release hydrophilic antitumor drugs with ease.