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Issue 30, 2016
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Ultra-small lipid–polymer hybrid nanoparticles for tumor-penetrating drug delivery

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Abstract

Lipid–polymer hybrid nanoparticles, consisting of a polymeric core coated by a layer of lipids, are a class of highly scalable, biodegradable nanocarriers that have shown great promise in drug delivery applications. Here, we demonstrate the facile synthesis of ultra-small, sub-25 nm lipid–polymer hybrid nanoparticles using an adapted nanoprecipitation approach and explore their utility for targeted delivery of a model chemotherapeutic. The fabrication process is first optimized to produce a monodisperse population of particles that are stable under physiological conditions. It is shown that these ultra-small hybrid nanoparticles can be functionalized with a targeting ligand on the surface and loaded with drug inside the polymeric matrix. Further, the in vivo fate of the nanoparticles after intravenous injection is characterized by examining the blood circulation and biodistribution. In a final proof-of-concept study, targeted ultra-small hybrid nanoparticles loaded with the cancer drug docetaxel are used to treat a mouse tumor model and demonstrate improved efficacy compared to a clinically available formulation of the drug. The ability to synthesize a significantly smaller version of the established lipid–polymer hybrid platform can ultimately enhance its applicability across a wider range of applications.

Graphical abstract: Ultra-small lipid–polymer hybrid nanoparticles for tumor-penetrating drug delivery

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Publication details

The article was received on 20 May 2016, accepted on 05 Jul 2016 and first published on 06 Jul 2016


Article type: Paper
DOI: 10.1039/C6NR04091H
Citation: Nanoscale, 2016,8, 14411-14419
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    Ultra-small lipid–polymer hybrid nanoparticles for tumor-penetrating drug delivery

    D. Dehaini, R. H. Fang, B. T. Luk, Z. Pang, C. J. Hu, A. V. Kroll, C. L. Yu, W. Gao and L. Zhang, Nanoscale, 2016, 8, 14411
    DOI: 10.1039/C6NR04091H

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