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Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity
No full textBackground Dual inhibitors of the 5-lipoxygenase-activating protein
(FLAP) and the microsomal prostaglandin E-2 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. Results The
nanoparticles containing BRP-187 were prepared by the nanoprecipitation
method and analyzed by dynamic light scattering regarding their
hydrodynamic diameter, by scanning electron microscopy for morphology
properties, and by UV-VIS spectroscopy for determination of the
encapsulation efficiency of the drug. Moreover, we designed fluorescent
BRP-187 particles, which showed high cellular uptake by leukocytes, as
analyzed by flow cytometry. Finally, BRP-187 nanoparticles were tested
in human polymorphonuclear leukocytes and macrophages to determine drug
uptake, cytotoxicity, and efficiency to inhibit FLAP and mPGES-1.
Conclusion Our results demonstrate that encapsulation of BRP-187 into
Acdex and PLGA is feasible, and both PLGA- and Acdex-based particles
loaded with BRP-187 are more efficient in suppressing 5-lipoxygenase
product formation and prostaglandin E-2 biosynthesis in intact cells as
compared to the free compound, particularly after prolonged
preincubation periods
Perkütan Tedavi Edilmiş Karaciğer Kist Hidatik Olgularının Retrospektif Değerlendirilmesi
No full textEarly indicators of disease progression in Fabry disease that may indicate the need for disease-specific treatment initiation: Findings from the opinion-based PREDICT-FD modified Delphi consensus initiative
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Pneumocystis Jirovecii pneumonia in newly diagnosed HIV infection: A challenging case report
No full textInvestigation of socio-economic characteristics of wheat producers on certified seed use: The case of Ankara Province [Buğday üreticilerinin sertifikalı tohum kullanımına etki eden sosyo-ekonomik özelliklerin incelenmesi: Ankara ili örneği]
No full textİç İçe Borulu Yay Tip Türbülatörlü Bir Isı Değiştiricisinin RNG k-ε Türbülans Modeli ile Sayısal Analizi
No full textLaparoscopic pectopexy and paravaginal repair after failed recurrent pelvic organ prolapse surgery
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