Synthesis, Characterization and Targeted Drug Delivery of Curcumin-Loaded PLGA Nanoparticles

Mohammad Chand Jamali¹*, Amged Gaffer Mostafa Gaffer ¹, Sameh Elsonbaty ¹, Javed Yasin ²

This study revealed curcumin-loaded PLGA nanoparticles' potential to enhance bioavailability, stability, and therapeutic efficacy, supporting their application in targeted therapy and controlled release.

Abstract

Background: Nanoparticle-based drug delivery systems have revolutionized therapeutic delivery, offering advantages such as enhanced bioavailability, controlled release, and targeted delivery to diseased tissues. Among these, polymeric nanoparticles, especially those utilizing poly(lactic-co-glycolic acid) (PLGA), have shown significant potential due to their biocompatibility, biodegradability, and stability. Curcumin, a polyphenolic compound with potent anti-inflammatory and anticancer properties, faces clinical limitations due to poor solubility and low bioavailability. Encapsulation in PLGA nanoparticles could enhance curcumin’s therapeutic efficacy by improving stability, controlled release, and targeted delivery. Methods: Curcumin-loaded PLGA nanoparticles were synthesized using a solvent evaporation method. Nanoparticles were characterized using dynamic light scattering (DLS) for size and zeta potential, and scanning electron microscopy (SEM) for morphology. In vitro drug release was assessed using a dialysis method, while cytotoxicity and anti-inflammatory activity were evaluated using MTT and nitric oxide inhibition assays, respectively. Results: DLS analysis revealed an average particle size of 150 ± 10 nm and a zeta potential of -25 ± 2 mV, indicating stability and suitability for therapeutic applications. SEM imaging showed smooth, spherical nanoparticles. Drug release studies displayed a biphasic pattern, with an initial burst followed by sustained release over 72 hours. Cytotoxicity assays demonstrated enhanced anticancer activity of curcumin-loaded nanoparticles compared to free curcumin, with a significantly lower IC50 value (5 ± 0.5 µM versus 15 ± 1.0 µM). Anti-inflammatory studies showed a 60% inhibition of nitric oxide production in LPS-induced macrophages, indicating improved anti-inflammatory efficacy over free curcumin. Conclusion: Curcumin-loaded PLGA nanoparticles show promise as a targeted drug delivery system, with enhanced stability, controlled release, and increased therapeutic efficacy. These findings support further in vivo studies to validate the clinical potential of curcumin nanoparticles in cancer and inflammatory diseases, providing a foundation for advanced therapeutic applications.

Keywords: Curcumin, PLGA nanoparticles, targeted drug delivery, controlled release, anti-inflammatory

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