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Open AccessFeature PaperArticle

Nanoemulsion-Enabled Oral Delivery of Novel Anticancer ω-3 Fatty Acid Derivatives

1
National Council for Scientific and Technological Development—CNPq, Brasília 71605-001, Brazil
2
Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo, NSW 2007, Australia
3
School of Mathematical and Physical Sciences, Faculty of Science, University of Technology Sydney, Ultimo, NSW 2007, Australia
4
School of Aerospace, Mechanical and Mechatronic Engineering, University of Sydney, Sydney, NSW 2006, Australia
5
Discipline of Pharmacology, School of Medical Sciences, Sydney Medical School, University of Sydney, Sydney, NSW 2006, Australia
*
Author to whom correspondence should be addressed.
Current address: Food and Drug Department, Università degli Studi di Parma (Italy).
Nanomaterials 2018, 8(10), 825; https://doi.org/10.3390/nano8100825
Received: 3 September 2018 / Revised: 24 September 2018 / Accepted: 8 October 2018 / Published: 13 October 2018
(This article belongs to the Special Issue Pharmaceutical Nanotechnology)
Lipid-based drugs are emerging as an interesting class of novel anticancer drugs with the potential to target specific cancer cell metabolic pathways linked to their proliferation and invasiveness. In particular, ω-3 polyunsaturated fatty acids (PUFA) derivatives such as epoxides and their bioisosteres have demonstrated the potential to suppress growth and promote apoptosis in triple-negative human breast cancer cells MDA-MB-231. In this study, 16-(4′-chloro-3′-trifluorophenyl)carbamoylamino]hexadecanoic acid (ClFPh-CHA), an anticancer lipid derived from ω-3,17,18-epoxyeicosanoic acid, was formulated as a stable nanoemulsion with size around 150 nm and narrow droplet size distribution (PDI < 0.200) through phase-inversion emulsification process followed by high pressure homogenization in view of an oral administration. The ClFPh-CHA-loaded nanoemulsions were able to significantly decrease the relative tumor volume in mice bearing an intramammary tumor xenograft at all doses tested (2.5, 10 and 40 mg/kg) after 32 days of daily oral administration. Furthermore, absolute tumor weight was decreased to 50% of untreated control at 10 and 40 mg/kg, while intraperitoneal administration could achieve a significant reduction only at the highest dose of 40 mg/kg. Results suggest that oral administration of ClFPh-CHA formulated as a nanoemulsion has a sufficient bioavailability to provide an anticancer effect in mice and that the activity is at least equal if not superior to that obtained by a conventional parenteral administration of equivalent doses of the same drug. View Full-Text
Keywords: nanoemulsion; oral delivery; ω-3 polyunsaturated fatty acid derivative; MDA-MB-231; triple-negative breast cancer nanoemulsion; oral delivery; ω-3 polyunsaturated fatty acid derivative; MDA-MB-231; triple-negative breast cancer
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Garrastazu Pereira, G.; Rawling, T.; Pozzoli, M.; Pazderka, C.; Chen, Y.; Dunstan, C.R.; Murray, M.; Sonvico, F. Nanoemulsion-Enabled Oral Delivery of Novel Anticancer ω-3 Fatty Acid Derivatives. Nanomaterials 2018, 8, 825.

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