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

• Main Authors: Jana Ismail (Author), Lea C. Klepsch (Author), Philipp Dahlke (Author), Ekaterina Tsarenko (Author), Antje Vollrath (Author), David Pretzel (Author), Paul M. Jordan (Author), Kourosh Rezaei (Author), Justyna A. Czaplewska (Author), Steffi Stumpf (Author), Baerbel Beringer-Siemers (Author), Ivo Nischang (Author), Stephanie Hoeppener (Author), Oliver Werz (Author), Ulrich S. Schubert (Author)
• Format: Book
• Published: MDPI AG, 2024-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

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 (d_H ~140 nm and d_H ~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.

Item Description

10.3390/pharmaceutics16020187
1999-4923