PREPARATION AND CHARACTERIZATION OF ARTEMETHER-LOADED PLGA NANOPARTICLES
Nnamani P.O 1 2*, Hansen S2, Lehr C-M 23
1 Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, University of Nigeria.
2 Department of Drug Delivery, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Center for Infection Research, Saarland University, Saarbrücken, Germany.
3 Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbrücken, Germany.
Afr. J Pharm Res Dev; Volume 10(1): 1-10; June/July 2018
PLGA particles of antimalarial drug, artemether (ART) were produced by emulsification-diffusion method and characterized. Fresh samples, reconstituted as well as stored samples were studied for particle size, polydispersity index (PDI) and zeta potential; thermal property by differential scanning calorimetry (DSC) while morphology was done by transmission electron microscopy (TEM) in addition to interaction study done by Fourier transform infrared spectroscopy (FTIR). Encapsulation efficiency and drug loading were determined by HPLC. Result shows stable monodispersed (0.01-0.21) spherical particles (201-246 nm) with molecular dispersion of 10 mg of ART while achieving encapsulation efficiency of ~13 % and drug loading of ~17 % superior to values obtained for the batch loaded with 5 mg of ART. FTIR showed interaction of OH-group of ART with C=O of PLGA resulting in shifts and/or reduction in peak intensity. The study reveals the feasibility of ART loaded PLGA nanoparticle (~246 nm) as having high potential for skin delivery since particle size is critical for tissue penetration, in vitro drug release, in vivo performances as well as degradation behavior. In an outlook, we are currently investigating the skin permeation and follicular uptake of these particles to hope for an alternative topical and/or transdermal antimalarial regimen of ART.
KEYWORDS: Malaria; Artemether; PLGA; Emulsion diffusion; HPLC; Characterization
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