Characteristics of Artemether-Loaded Poly(lactic-co-glycolic) Acid Microparticles Fabricated by Coaxial Electrospray: Validation of Enhanced Encapsulation Efficiency and Bioavailability

Molecular Pharmaceutics
Farhana Akbar MangrioRonald X Xu

Abstract

Artemether is one of the most effective drugs for the treatment of chloroquine-resistant and Plasmodium falciparum strains of malaria. However, its therapeutic potency is hindered by its poor bioavailability. To overcome this limitation, we have encapsulated artemether in poly(lactic-co-glycolic) acid (PLGA) core-shell microparticles (MPs) using the coaxial electrospray method. With optimized process parameters including liquid flow rates and applied electric voltages, experiments are systematically carried out to generate a stable cone-jet mode to produce artemether-loaded PLGA-MPs with an average size of 2 μm, an encapsulation efficiency of 78 ± 5.6%, and a loading efficiency of 11.7%. The in vitro release study demonstrates the sustained release of artemether from the core-shell structure in comparison with that of plain artemether and that of MPs produced by single-axial electrospray without any relevant cytotoxicity. The in vivo studies are performed to evaluate the pharmacokinetic characteristics of the artemether-loaded PLGA-MPs. Our study implies that artemether can be effectively encapsulated in a protective shell of PLGA for controlled release kinetics and enhanced oral bioavailability.

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Citations

Jul 26, 2019·Expert Opinion on Drug Delivery·Muhammet Emin CamMohan Edirisinghe
Jan 19, 2020·Journal of Functional Biomaterials·Alan Í S MoraisAnderson O Lobo
Nov 6, 2020·Journal of Applied Biomaterials & Functional Materials·Jing Song, Ziping Zhang
Dec 15, 2020·Journal of Applied Biomaterials & Functional Materials·Ying ZhangPeng Chen

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