Carboxymethylated Laminarin-Decorated ZIF-8 Enables Macrophage-Targeted Quercetin Delivery with Superior Anti-Inflammatory Efficacy.

Authors

Fei Jiao, Wenqian Zhou

Published in

Analytical biochemistry. Pages 116263. Oct 03, 2026. Epub Oct 03, 2026.

Abstract

To address the limitations of quercetin (Qu), including low bioavailability, limited targeting, and insufficient synergistic enhancement, we developed a ZIF-8-based nanodelivery system (Qu-ZIF-8-CMLA) coated with a carboxymethyl laminarin (CMLA) layer. The platform was designed for macrophage-targeted delivery with potential for oral administration. Qu-ZIF-8-CMLA exhibited a hydrodynamic diameter of 151.5 nm, a drug loading capacity of 15.2%, and colloidal stability. Characterization confirmed CMLA coating of the Qu-ZIF-8 surface through electrostatic interactions and hydrogen bonding. The resulting nanoparticles maintained structural integrity and exhibited pH-responsive, controlled-release properties. In simulated gastric fluid, Qu-ZIF-8-CMLA released 23.54% of the Qu, whereas release reached 70.08% under simulated intestinal conditions, indicating a more sustained release profile than free Qu. Release kinetic analysis suggested a non-Fickian mechanism involving polysaccharide erosion and drug diffusion. In RAW264.7 macrophages, CMLA modification increased uptake by 6.35-fold, while competitive inhibition with free CMLA significantly attenuated this enhancement, supporting the involvement of CMLA-sensitive receptor-associated recognition in macrophage uptake. At high concentrations, Qu-ZIF-8-CMLA maintained higher RAW264.7 cell viability than Qu-ZIF-8 under the tested conditions. Anti-inflammatory activity was evaluated in LPS-stimulated RAW264.7 macrophages by measuring TNF-α, IL-1β, and IL-6 secretion using ELISA. Qu-ZIF-8-CMLA significantly reduced three pro-inflammatory cytokines compared with the LPS model group, and no statistically significant differences were detected between the Qu-ZIF-8-CMLA and untreated control groups (p > 0.05). Qu-ZIF-8-CMLA showed significantly greater anti-inflammatory activity than free Qu and Qu-ZIF-8. Collectively, these findings provide in vitro proof of concept for CMLA-modified, macrophage-targeted Qu delivery and support further investigation of this platform for oral anti-inflammatory applications.

PMID:
42829162
Bibliographic data and abstract were imported from PubMed on 04 Oct 2026.

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