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

Overview

Journal Pharmaceutics

Publisher MDPI

Date 2024 Feb 24

PMID 38399248

Authors

Jana Ismail

Lea C Klepsch

Philipp Dahlke

Ekaterina Tsarenko

Antje Vollrath

David Pretzel

Paul M Jordan

Kourosh Rezaei

Justyna A Czaplewska

Steffi Stumpf

Baerbel Beringer-Siemers

Ivo Nischang

Stephanie Hoeppener

Oliver Werz

Ulrich S Schubert

Affiliations

Soon will be listed here.

Abstract

Hybrid nanoparticles (HNPs) were designed by combining a PLGA core with a lipid shell that incorporated PEG-Lipid conjugates with various functionalities (-RGD, -cRGD, -NH, 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 ~140 nm and d ~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.

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