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