Anticoagulants are important drugs capable of preventing diseases like thrombosis, which can lead to life-threatening conditions such as heart attacks and strokes. Aptamers can function as nucleic acid-based anticoagulants if they are directed against enzymes of the coagulation cascade. Aptamers have promising features including specific and reversible target binding and inhibition, but typically suffer from fast clearance from the blood stream. We present thrombin-binding aptamers that are displayed at high density on the surface of nanoscale polymeric micelles. We demonstrate that these micellar aptamers are stable in human serum and retain their native secondary structure. Moreover, they are effective inhibitors of plasma clotting in vitro. The inhibitory effect can be rapidly reversed by complementary nucleic acids that brake the aptamers’ secondary structure upon hybridization. The increased molecular weight and size of the described micellar aptamers may help to prevent fast renal clearance and thereby extend circulation times in vivo.

Micellar thrombin-binding aptamers as reversible nanoscale anticoagulants

253rd National Meeting (2017)

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