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

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.

Fabrication of Polymeric Microparticles by Electrospray: The Impact of Experimental Parameters

“…Moreover, ES settings can be varied by changing the collector. There are several types of collectors used to obtain particles, such as aluminum plates [31][32][33], stainless steel plates [34,35], steel plates covered with foil [15,32] and the receiver solution [28,[36][37][38][39], which are all demonstrated in Figure 2a-d. Moreover, previous studies have demonstrated the use of alcohol solutions, buffers and surfactants as the MP receptor solution [28,[36][37][38][39].…”

Sustained release paclitaxel-loaded core-shell-structured solid lipid microparticles for intraperitoneal chemotherapy of ovarian cancer

“…Recently, we succeeded in preparing artemether-loaded and curcumin-loaded core-shell-structured PLGA MPs using CEHDA process for different applications in our lab [23,34]. However, in the present study, we have developed CEHDA technology for scalable production of PTX-laden SLMPs (PTX-SLMPs) with core-shell structure in a single-step process.…”

Electrosprayed microparticles: a novel drug delivery method

“…The effects of liquid properties on the electrospraying process. [10], [11] Reprinted with permission. Copyright (2019) American Chemical Society.…”