Formulation of Novel Artesunate-Loaded Solid Lipid Microparticles (SLMs) Based on Dika Wax Matrices: In Vitro and in Vivo Evaluation

• Published in: Journal of drug delivery science and technology Vol. 24; no. 1; pp. 69 - 77
• Main Authors: Chinaeke, E.E., Chime, S.A., Kenechukwu, F.C., Müller-Goymann, C.C., Attama, A.A., Okore, V.C.
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.01.2014
• Subjects: Anti-malaria; Artesunate; Characterisation; P90G-modified dika wax; SLMs; P90G-modified dika wax; SLMs; Characterisation; Anti-malaria; Artesunate
• ISSN: 1773-2247
• DOI: 10.1016/S1773-2247(14)50010-X

The aims of the work were to formulate artesunate-loaded solid lipid microparticles (SLMs) based on dika wax matrices and to study the in vitro and in vivo properties. Lipid matrices consisting of mixtures of Phospholipon 90G (P90G) and dika wax were formulated and characterized by differential scanning calorimetry (DSC), small angle X-ray diffraction (SAXD) and wide angle X-ray diffraction (WAXD). The SLMs were prepared by melt-homogenization. Time-dependent particle size analysis, pH studies, encapsulation efficiency (EE%), in vitro drug release and anti-malarial properties were studied. Results show that SAXD diffractograms showed strong reflection at 2θ =2.48°, d =3.56Å. Particle size of SLMs increased with time (from 1 to 90 days). The SLMs exhibited maximum EE% of 80.6 % and had good sustained release properties. In vivo studies showed that the SLMs had significant (p <0.05) reduction in parasitaemia level compared with reference tablet. Artesunate-loaded SLMs could be used orally for the treatment of malaria.