Issue 9, 2017

Precision spherical nucleic acids for delivery of anticancer drugs


We report a spherical nucleic acid (SNA) system for the delivery of BKM120, an anticancer drug for treatment of chronic lymphocytic leukemia (CLL). While promising for cancer treatment, this drug crosses the blood–brain barrier causing significant side-effects in patients. The DNA nanoparticle encapsulates BKM120 in high efficiency, and is unparalleled in its monodispersity, ease of synthesis and stability in different biological media and in serum. These DNA nanostructures demonstrate efficient uptake in human cervical cancer (HeLa) cells, and increased internalization of cargo. In vitro studies show that BKM120-loaded nanoparticles promote apoptosis in primary patient CLL lymphocytes, and act as sensitizers of other antitumor drugs, without causing non-specific inflammation. Evaluation of this drug delivery system in vivo shows long circulation times up to 24 hours, full body distribution, accumulation at tumor sites and minimal leakage through the blood–brain barrier. Our results demonstrate the great potential of these delivery vehicles as a general platform for chemotherapeutic drug delivery.

Graphical abstract: Precision spherical nucleic acids for delivery of anticancer drugs

Supplementary files

Article information

Article type
Edge Article
11 Apr 2017
29 Jun 2017
First published
05 Jul 2017
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2017,8, 6218-6229

Precision spherical nucleic acids for delivery of anticancer drugs

D. Bousmail, L. Amrein, J. J. Fakhoury, H. H. Fakih, J. C. C. Hsu, L. Panasci and H. F. Sleiman, Chem. Sci., 2017, 8, 6218 DOI: 10.1039/C7SC01619K

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