Research Papers:

Oseltamivir phosphate released from injectable Pickering emulsions over an extended term disables human pancreatic cancer cell survival

Kurt Wood, Myron R. Szewczuk _, Dérick Rousseau and Ronald J. Neufeld

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Oncotarget. 2018; 9:12754-12768. https://doi.org/10.18632/oncotarget.24339

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Kurt Wood1, Myron R. Szewczuk2, Dérick Rousseau3 and Ronald J. Neufeld1

1Department of Chemical Engineering, Queen’s University, Kingston, Ontario K7L3N6, Canada

2Department of Biomedical and Molecular Sciences, Queen’s University, Kingston, Ontario K7L3N6, Canada

3Department of Chemistry and Biology, Ryers on University, Toronto, Ontario M5B 2K3, Canada

Correspondence to:

Myron R. Szewczuk, email: [email protected]

Dérick Rousseau, email: [email protected]

Ronald J. Neufeld, email: [email protected]

Keywords: Pickering emulsion; sustained release; oseltamivir phosphate; competitive adsorption

Received: October 06, 2017     Accepted: January 20, 2018     Published: January 29, 2018


Pickering emulsions are colloidal dispersions stabilized by particles that either migrate to, or are formed at, the oil-water interface during emulsification. Here, we fabricated and characterized Pickering water-in-oil emulsions where molten glycerol monostearate crystallized at the surface of micron-sized water droplets and formed protective solid shells. We tested this emulsion as a reservoir delivery platform for the sustained release of low molecular weight hydrophilic molecules including sodium chloride (NaCl) and sodium citrate as model compounds, and the therapeutic oseltamivir phosphate (OP), the delivery of which was the ultimate goal of this research. The objective was to achieve long-term (30-day) release of challenging to encapsulate actives and ultimately demonstrate the sustained release of OP for 20–30 days from an injectable formulation. OP was used because of its anticancer properties targeting mammalian neuraminidase 1 (Neu1) involved in multistage tumorigenesis. All actives including OP encapsulated in Pickering emulsions displayed a near linear release profile over 30 days. It was demonstrated that the release could be modulated by the addition of a second, competing surfactant sorbitan monooleate, Span 80, to the emulsion at levels above its critical micelle concentration. OP released from the emulsions significantly reduced cell viability in the human PANC-1 pancreatic cancer cell line for up to 30 days. The findings from this study indicate a simple, potentially injectable formulation and method that is easily upscaled resulting in a stable product with the potential to fully retain small hydrophilic molecules/drugs for sustained, near linear release over days, weeks, and potentially months.

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