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Optimization and characterization of primaquine–loaded solid lipid nanoparticles (SLN) for liver schinonticide targeting by freeze drying


MOJ Drug Design Development & Therapy
James Jorum Owuor,1,2 Florence Oloo,1,2 Daniel Ouma,1 Wesley Nyaigoti Omwoyo,2,4 Jeremiah Waweru Gathirwa2,3
Department of Chemical Sciences and Technology, Technical University of Kenya, Kenya
Florence Oloo, Department of Chemical Sciences and Technology, Technical University of Kenya, Kenya
Daniel Ouma, Department of Chemical Sciences and Technology, Technical University of Kenya, Kenya
Wesley Nyaigoti Omwoyo, Center for Research in Therapeutic Sciences, Strathmore University Nairobi, Kenya
Jeremiah Waweru Gathirwa, Kenya Medical Research Institute, Kenya

Abstract

The aim of this study was preparation of a liver schinonticide Primaquine phosphate (PQ) directly to the hepatocytes using solid lipid nanoparticles (SLN). The PQ-loaded solid lipid nanoparticles (PQ-SLNs) were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion and dried freeze drying (PQ-SLNFD) to obtain the nanoparticles. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNFD were 236 nm, +23 mV, 14%, and 75%, respectively. A spherical morphology of PQ-SLNFD was seen by scanning electron microscope had traces of drug crystals. In vitro, release profile depicted a steady drug release over 400 hours for PQ-SLNFD. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei-infected Swiss albino mice. This study established an effective process of developing a nanomedicine delivery system for PQ.

Keywords

double emulsion, solid lipid nanoparticles, freeze dried

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