4.7 Article

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

Journal

DRUG DELIVERY
Volume 23, Issue 9, Pages 3452-3460

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/10717544.2016.1194498

Keywords

5-Fluorouracil; Erlich's tumor; gold nanoparticles; reversed micelles; SLN

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Context: The effective treatment of skin carcinoma is warranted for targeting the chemotherapeutic agents into tumor cells and avoiding unwanted systemic absorption.Objective: 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).Methods: 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.Results: 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 1375.5nm to 800 +/- 53.6, zeta potential of -19.70 +/- 0.40mV and entrapment efficiency of 47.92 +/- 2.34%. The diffusion of the drug-loaded SLN (269.37 +/- 10.92g/cm(2)) was doubled when compared with the free drug (122 +/- 3.09g/cm(2)) 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.Conclusion: SLN possesses the capacity to be manipulated to entrap and release hydrophilic antitumor drugs with ease.

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