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Solid lipid nanoparticles self-assembled from spray dried microparticles

Sanchez-Vazquez, B; Bong Lee, J; Strimaite, M; Buanz, A; Bailey, R; Gershkovich, P; Pasparakis, G; (2019) Solid lipid nanoparticles self-assembled from spray dried microparticles. International Journal of Pharmaceutics , 572 , Article 118784. 10.1016/j.ijpharm.2019.118784. Green open access

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Abstract

We report the self-assembly of anti-cancer drug-loaded solid lipid nanoparticles (SLNs) from spray dried microparticles comprising poly(vinylpyrrolidone) (PVP) loaded with glyceryl tristearate (GTS) and either indomethacin (IMC) or 5-fluorouracil (5-FU). When the spray dried microparticles are added to water, the PVP matrix dissolves and the GTS and drug self-assemble into SLNs. The SLNs provide a non-toxic delivery platform for both hydrophobic (indomethacin) and hydrophilic (5-fluorouracil) drugs. They show extended release profiles over more than 24 h, and in permeation studies the drug cargo is seen to accumulate inside cancer cells. This overcomes major issues with achieving local intestinal delivery of these active ingredients, in that IMC permeates well and thus will enter the systemic circulation and potentially lead to side effects, while 5-FU remains in the lumen of the small intestine and will be secreted without having any therapeutic benefit. The SLN formulations are as effective as the pure drugs in terms of their ability to induce cell death. Our approach represents a new and simple route to the fabrication of SLNs: by assembling these from spray-dried microparticles on demand, we can circumvent the low storage stability which plagues SLN formulations.

Type: Article
Title: Solid lipid nanoparticles self-assembled from spray dried microparticles
Open access status: An open access version is available from UCL Discovery
DOI: 10.1016/j.ijpharm.2019.118784
Publisher version: https://doi.org/10.1016/j.ijpharm.2019.118784
Language: English
Additional information: This version is the author accepted manuscript. For information on re-use, please refer to the publisher’s terms and conditions.
Keywords: Spray-drying; self-assembly; solid lipid nanoparticle; drug delivery system; stability
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
URI: https://discovery.ucl.ac.uk/id/eprint/10085160
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