Insight into Fucoidan-Based PEGylated PLGA Nanoparticles Encapsulating Methyl Anthranilic Acid: In Vitro Evaluation and In Vivo Anti-Inflammatory Study

• Published in: Marine drugs Vol. 20; no. 11; p. 694
• Main Authors: Abdelkader, Dalia H, Elekhnawy, Engy, Negm, Walaa A, El-Masry, Thanaa A, Almukainzi, May, Zayed, Ahmed, Ulber, Roland
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 01.11.2022; MDPI
• Subjects: Anthranilic acid; Anti-inflammatory agents; aqueous coating; Bioavailability; Carrageenan; Carrageenans; Chemical properties; Cyclooxygenase-2; Cytokines; Drug delivery systems; Drugs; Edema; Entrapment; Enzymes; Evaluation; Fucoidan; Hydrophobicity; IL-1β; In vivo methods and tests; Inflammation; Interleukin 6; interleukins; Materials; Molecular weight; Nanoemulsions; Nanoparticles; Necrosis; Nitric oxide; Particle size; Pharmaceuticals; Pharmacokinetics; Pharmacology; Polylactide-co-glycolide; Polysaccharides; Prostaglandin E2; reactive oxygen species; single emulsion solvent evaporation; Structure; tumor necrosis factor-alpha; Tumor necrosis factor-TNF; Tumor necrosis factor-α; Vehicles; Zeta potential; Egypt
• ISSN: 1660-3397; 1660-3397
• DOI: 10.3390/md20110694

A potential fucoidan-based PEGylated PLGA nanoparticles (NPs) offering a proper delivery of N-methyl anthranilic acid (MA, a model of hydrophobic anti-inflammatory drug) have been developed via the formation of fucoidan aqueous coating surrounding PEGylated PLGA NPs. The optimum formulation (FuP2) composed of fucoidan:m-PEG-PLGA (1:0.5 w/w) with particle size (365 ± 20.76 nm), zeta potential (−22.30 ± 2.56 mV), % entrapment efficiency (85.45 ± 7.41), drug loading (51.36 ± 4.75 µg/mg of NPs), % initial burst (47.91 ± 5.89), and % cumulative release (102.79 ± 6.89) has been further investigated for the anti-inflammatory in vivo study. This effect of FuP2 was assessed in rats’ carrageenan-induced acute inflammation model. The average weight of the paw edema was significantly lowered (p ≤ 0.05) by treatment with FuP2. Moreover, cyclooxygenase-2 and tumor necrosis factor-alpha immunostaining were decreased in FuP2 treated group compared to the other groups. The levels of prostaglandin E2, nitric oxide, and malondialdehyde were significantly reduced (p ≤ 0.05) in the FuP2-treated group. A significant reduction (p ≤ 0.05) in the expression of interleukins (IL-1β and IL-6) with an improvement of the histological findings of the paw tissues was observed in the FuP2-treated group. Thus, fucoidan-based PEGylated PLGA–MA NPs are a promising anti-inflammatory delivery system that can be applied for other similar drugs potentiating their pharmacological and pharmacokinetic properties.