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Solid lipid nanoparticles self-assembled from spray dried microparticles

Sanchez-Vazquez, Brenda; Lee, Jong Bong; Strimaite, Margarita; Buanz, Asma; Bailey, Russell; Gershkovich, Pavel; Pasparakis, George; Williams, Gareth R.

Authors

Brenda Sanchez-Vazquez

Jong Bong Lee

Margarita Strimaite

Asma Buanz

Russell Bailey

Pavel Gershkovich

George Pasparakis

Gareth R. Williams



Abstract

We report the self-assembly of 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 (IMC) and hydrophilic (5-FU) 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.

Journal Article Type Article
Publication Date Dec 15, 2019
Journal International Journal of Pharmaceutics
Print ISSN 0378-5173
Electronic ISSN 1873-3476
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 572
Article Number 118784
APA6 Citation Sanchez-Vazquez, B., Lee, J. B., Strimaite, M., Buanz, A., Bailey, R., Gershkovich, P., …Williams, G. R. (2019). Solid lipid nanoparticles self-assembled from spray dried microparticles. International Journal of Pharmaceutics, 572, https://doi.org/10.1016/j.ijpharm.2019.118784
DOI https://doi.org/10.1016/j.ijpharm.2019.118784
Keywords Spray-drying; Self-assembly; Solid lipid nanoparticle; Drug delivery system; Stability
Publisher URL https://www.sciencedirect.com/science/article/pii/S0378517319308294
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