Development of Artocarpin-Loaded Chitosan Particles for Controlled Release and Inflammatory Application

Area of Science:

• Pharmacology and Drug Delivery
• Natural Product Chemistry
• Materials Science

Background:

• Artocarpin, a flavonoid from *Artocarpus altilis*, exhibits anti-inflammatory and geroprotective properties.
• Enhancing artocarpin's stability and efficacy requires advanced delivery systems.
• Chitosan microparticles offer a biocompatible platform for drug delivery.

Purpose of the Study:

• To isolate and characterize artocarpin from *Artocarpus altilis* heartwood.
• To develop and optimize chitosan-based microparticles for artocarpin delivery.
• To evaluate the physicochemical properties, in vitro release, and anti-inflammatory activity of the artocarpin-loaded microparticles.

Main Methods:

• Artocarpin isolation via maceration and chromatographic purification.
• Chitosan microparticle formulation using sodium tripolyphosphate cross-linking.
• Characterization using HPLC, DLS, FTIR, XRD, and in vitro release studies.
• Assessment of anti-inflammatory activity via nitric oxide inhibition in LPS-stimulated RAW 264.7 macrophages.

Main Results:

• Isolated artocarpin with 81% purity; developed stable chitosan microparticles (1-4 µm) with good encapsulation efficiency.
• FTIR and XRD confirmed successful artocarpin incorporation into the chitosan matrix.
• In vitro studies showed biphasic release and significant, dose-dependent reduction in nitric oxide production (34.33-73.19%).

Conclusions:

• Artocarpin-loaded chitosan microparticles (CSPs/AE) represent a promising delivery system for artocarpin.
• The developed system exhibits effective anti-inflammatory properties.
• This formulation holds potential for managing inflammatory conditions like osteoarthritis.