ADVERTISEMENT
2 /3 FREE ARTICLES LEFT THIS MONTH Remaining
Chemistry matters. Join us to get the news you need.

If you have an ACS member number, please enter it here so we can link this account to your membership. (optional)

ACS values your privacy. By submitting your information, you are gaining access to C&EN and subscribing to our weekly newsletter. We use the information you provide to make your reading experience better, and we will never sell your data to third party members.

ENJOY UNLIMITED ACCES TO C&EN

Pharmaceuticals

Shear-Activated Clot-Busting Drug

Biophysical strategy tears apart drug-carrying nanoparticle clusters to more efficiently clear blocked blood vessels

by Sarah Everts
July 9, 2012 | APPEARED IN VOLUME 90, ISSUE 28

[+]Enlarge
Credit: Courtesy of Wyss Institute
This fluorescence micrograph reveals the cross section of a blocked artery (about 1 mm wide); the nanoparticle-bound clot-busting drug tPA is shown in pink.
09028-scicon-korin1HRcxd.jpg
Credit: Courtesy of Wyss Institute
This fluorescence micrograph reveals the cross section of a blocked artery (about 1 mm wide); the nanoparticle-bound clot-busting drug tPA is shown in pink.

When blood clots form during atherosclerosis or a stroke, the obstruction increases the shear forces of blood in the blocked vessel. Researchers are now taking advantage of these forces to break apart nanoparticle clusters to deliver a clot-busting drug called tissue plasminogen activator (tPA) so that much less of the drug is required (Science, DOI: 10.1126/science.1217815). Because tPA causes serious side effects, such as excessive internal bleeding, the new delivery strategy has the potential to enhance drug safety, says Harvard University’s Donald E. Ingber, who led the research. Ingber’s team assembled aggregates of poly(lactic-co-glycolic acid) nanoparticles to which they attached tPA via a biotin linker. In normal blood flow, the aggregates remain intact. But near a blockage the increased shear forces break the aggregates apart, releasing the drug for efficient arrival at the clot site. Hurdles remain before the drug delivery system can enter the clinic, including ensuring nanoparticle safety and replacing biotin with a linker that doesn’t activate the human immune system.

X

Article:

This article has been sent to the following recipient:

Leave A Comment

*Required to comment