Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity

Shkodra-Pula, Blerina; Kretzer, Christian; Jordan, Paul; Klemm, Paul; Koeberle, Andreas; Pretzel, David; Banoglu, Erden; Lorkowski, Stefan; Höppener, Stephanie; Stumpf, Steffi; Vollrath, Antje; Schubert, Stephanie; Werz, Oliver; Schubert, Ulrich S.

Abstract:

Dual inhibitors of the 5-lipoxygenase-activating protein (FLAP) and the microsomal prostaglandin E2 synthase-1 (mPGES-1) may exert better anti-inflammatory efficacy and lower risks of adverse effects versus non-steroidal anti-inflammatory drugs. Despite these advantages, many dual FLAP/mPGES-1 inhibitors are acidic lipophilic molecules with low solubility and strong tendency for plasma protein binding that limit their bioavailability and bioactivity. Here, we present the encapsulation of the dual FLAP/mPGES-1 inhibitor BRP-187 into the biocompatible polymers acetalated dextran (Acdex) and poly(lactic-co-glycolic acid) (PLGA) via nanoprecipitation.

Year:

2020

Type of Publication:

Article

Journal:

Journal of Nanobiotechnology

Volume:

18

Pages:

73