Author: Jordan, Paul M. ; Beringer-Siemers, Baerbel ; Hoeppener, Stephanie ; Nischang, Ivo ; Chi, Mingzhe ; Werz, Oliver ; Czaplewska, Justyna Anna ; Kellner, Carolin ; Dahlke, Philipp ; Kretzer, Christian ; Vollrath, Antje ; Schubert, Ulrich S. ; Sierka, Marek ; Tsarenko, Ekaterina ; Behnke, Mira ; Larios, Francisco Paez ; Eggeling, Christian ; Weber, Christine ; Stumpf, Steffi ; Dirauf, Michael

Poly(ester amide)s (PEAs) consisting of L-valine (Val), glycolic acid (G), and L-isoleucine (Ile), i.e., PValG and PIleG, and various poly(2-ethyl-2-oxazoline)-block-poly(ester amide) copolymers (PEtOx-b-PEA) were investigated for their suitability as particle-based delivery systems for the anti-inflammatory drugs BRP-187 and BRP-201.A small-scale, high-throughput formulation approach was utilized to evaluate the nanoparticle properties in dependence of the composition of mixtures of PEA homo- and copolymers.Atomistic mol. dynamics simulations of PValG and PIleG with the active ingredients indicated thermodn. compatibility of the PEAs with the drugs.Drug encapsulation studies confirmed the formation of stable formulations, and the enzymic degradation of the nanoparticles was also demonstrated.The nanoparticles exhibited no cytotoxicity and were able to efficiently deliver the active pharmaceutical ingredients, i.e., BRP-187 and BRP-201 into macrophages and HEK293 cells.All nanoparticle systems displayed anti-inflammatory effectiveness as they were able to suppress cellular 5-lipoxygenase activity.The most promising effects were obtained with the block copolymer-based PEtOx-b-PEA nanoparticles, which revealed an enhanced performance compared to the control PLGA nanoparticles.

01 Dec 2023·International Journal of Pharmaceutics: X

Ethoxy acetalated dextran nanoparticles for drug delivery: A comparative study of formulation methods

Article

Author: Dahlke, Philipp ; Schubert, Stephanie ; Czaplewska, Justyna Anna ; Shkodra, Blerina ; Stumpf, Steffi ; Hoeppener, Stephanie ; Jordan, Paul M ; Werz, Oliver ; Schubert, Ulrich S ; Vollrath, Antje ; Klemm, Paul ; Behnke, Mira ; Beringer-Siemers, Baerbel

Dextran-based polymers, such as ethoxy acetalated dextran (Ace-DEX), are increasingly becoming the focus of research as they offer great potential for the development of polymer-based nanoparticles as drug delivery vehicles. Their major advantages are the facile synthesis, straightforward particle preparation and the pH-dependent degradation of the particles that can be fine-tuned by the degree of acetalation of the polymer. In this study we have shown that Ace-DEX can not only compete against the commonly used and FDA-approved polymer poly(lactic-co-glycolic acid) (PLGA), but even has the potential to outperform it in its encapsulation properties, e.g., for the herein used anti-inflammatory leukotriene biosynthesis inhibitor BRP-187. We used three different methods (microfluidics, batch nanoprecipitation and emulsion solvent evaporation) for the preparation of BRP-187-loaded Ace-DEX nanoparticles to investigate the influence of the formulation technique on the physicochemical properties of the particles. Finally, we evaluated which production method offers the greatest potential for achieving the demands for a successful translation from research into pharmaceutical production by fulfilling the basic requirements, such as reaching a high loading capacity of the particles and excellent reproducibility while being simple and affordable.

01 Apr 2022·Journal of Colloid and Interface ScienceQ2 · CHEMISTRY

Miniemulsion polymerization at low temperature: A strategy for one-pot encapsulation of hydrophobic anti-inflammatory drugs into polyester-containing nanoparticles

Q2 · CHEMISTRY

Article

Author: Schubert, Stephanie ; Kleinsteuber, Maximilian ; De San Luis, Alicia ; Schuett, Timo ; Schubert, Ulrich S

HYPOTHESISConventional synthesis methods of polymeric nanoparticles as drug delivery systems are based on the use of large amounts of organic solvents, hence requiring several steps for the obtaining of waterborne dispersions. In view of the need for new environmentally friendly methods, emulsion polymerization and their related techniques are a good alternative for the production of monodispersed waterborne dispersions of biodegradable nanoparticles in a cleaner, reproducible and faster manner.EXPERIMENTSHerein, the miniemulsion polymerization technique at low temperature using poly(2-ethyl-2-oxazoline) as surfactant has been developed for poly(hydroxyethyl methacrylate-lactic acid) and poly(hydroxyethyl methacrylate-lactic-co-glycolic acid) nanoparticles. Additionally, the anti-inflammatory drug BRP-187 was used to proof the potential of this technique in the encapsulation of hydrophobic drugs. The effect of the oligomer composition on the miniemulsion and the final dispersion stability, the final oligomer conversion, the polymer particle size and the drug encapsulation efficiency has been studied.FINDINGSMonodisperse spherical particles ranging between 170 and 250 nm in diameter in long term non-toxic stable waterborne dispersions were obtained with drug encapsulation efficiencies up to 66%. In contrast with conventional synthesis techniques, residual organic solvents are completely removed and, thus, the potential of redox initiated miniemulsion polymerization to obtain stable drug loaded poly(hydroxyethyl methacrylate-lactic acid) and poly(hydroxyethyl methacrylate-lactic-co-glycolic acid) nanoparticles in an efficient and fast manner is shown.

100 Deals associated with BRP-187

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Preclinical	Germany	Friedrich Schiller University of Jena	-
Asthma	Preclinical	Italy	Università degli Studi di Perugia	-
Atherosclerosis	Preclinical	Germany	Friedrich Schiller University of Jena	-
Atherosclerosis	Preclinical	Italy	Università degli Studi di Perugia	-

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