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

ORCID
0000-0002-6277-3565
Affiliation
Pharmaceutical Technology Department, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt
Abdelkader, Dalia H.;
ORCID
0000-0001-8287-1026
Affiliation
Pharmaceutical Microbiology Department, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt
Elekhnawy, Engy;
ORCID
0000-0003-0463-8047
Affiliation
Department of Pharmacognosy, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt
Negm, Walaa A.;
Affiliation
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt
El-Masry, Thanaa A.;
ORCID
0000-0001-6732-7591
Affiliation
Department of Pharmaceutical Science, College Pharmacy, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia
Almukainzi, May;
ORCID
0000-0001-5747-6972
Affiliation
Department of Pharmacognosy, Faculty of Pharmacy, Tanta University, Tanta 31527, Egypt
Zayed, Ahmed;
Affiliation
Institute of Bioprocess Engineering, Technical University of Kaiserslautern, Gottlieb-Daimler-Straße 49, 67663 Kaiserslautern, Germany
Ulber, Roland

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-1 β 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.

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