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Ismail, Jana; Klepsch, Lea C.; Dahlke, Philipp; Tsarenko, Ekaterina; Vollrath, Antje; Pretzel, David; Jordan, Paul M.; Rezaei, Kourosh; Czaplewska, Justyna A.; Stumpf, Steffi; Beringer-Siemers, Baerbel; Nischang, Ivo; Hoeppener, Stephanie; Werz, Oliver; Schubert, Ulrich S.

PEG–Lipid–PLGA Hybrid Particles for Targeted Delivery of Anti-Inflammatory Drugs

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  • Media type: E-Article
  • Title: PEG–Lipid–PLGA Hybrid Particles for Targeted Delivery of Anti-Inflammatory Drugs
  • Contributor: Ismail, Jana; Klepsch, Lea C.; Dahlke, Philipp; Tsarenko, Ekaterina; Vollrath, Antje; Pretzel, David; Jordan, Paul M.; Rezaei, Kourosh; Czaplewska, Justyna A.; Stumpf, Steffi; Beringer-Siemers, Baerbel; Nischang, Ivo; Hoeppener, Stephanie; Werz, Oliver; Schubert, Ulrich S.
  • Published: MDPI AG, 2024
  • Published in: Pharmaceutics, 16 (2024) 2, Seite 187
  • Language: English
  • DOI: 10.3390/pharmaceutics16020187
  • ISSN: 1999-4923
  • Origination:
  • Footnote:
  • Description: Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG–Lipid conjugates with various functionalities (-RGD, -cRGD, -NH2, and -COOH) to create targeted drug delivery systems. Loaded with a neutral lipid orange dye, the HNPs were extensively characterized using various techniques and investigated for their uptake in human monocyte-derived macrophages (MDMs) using FC and CLSM. Moreover, the best-performing HNPs (i.e., HNP-COOH and HNP-RGD as well as HNP-RGD/COOH mixed) were loaded with the anti-inflammatory drug BRP-201 and prepared in two size ranges (dH ~140 nm and dH ~250 nm). The HNPs were examined further for their stability, degradation, MDM uptake, and drug delivery efficiency by studying the inhibition of 5-lipoxygenase (5-LOX) product formation, whereby HNP-COOH and HNP-RGD both exhibited superior uptake, and the HNP-COOH/RGD (2:1) displayed the highest inhibition.
  • Access State: Open Access