Development of a Novel Nano-Formulation of Artemisinin Using Nigerian Mango Kernel Lipid Nanoparticles for Enhanced Malaria Pharmacotherapy

📖 ABSTRACT/OVERVIEW

Background: Artemisinin suffers from poor oral bioavailability due to its lipophilicity, rapid first-pass metabolism, and short plasma half-life. Lipid nanoparticle formulations offer a viable delivery strategy to enhance bioavailability, prolong drug release, and improve clinical efficacy. Nigerian mango kernel fat represents an abundant, low-cost local lipid excipient with suitable physicochemical properties for nanoparticle preparation. This study develops and evaluates artemisinin-loaded mango kernel lipid nanoparticles for enhanced malaria pharmacotherapy. Methods: Solid lipid nanoparticles (SLNs) were prepared using Nigerian mango kernel fat as the lipid matrix via hot homogenisation. Nanoparticle characterisation included particle size, zeta potential, encapsulation efficiency, and in vitro drug release profiling. Pharmacokinetic studies compared oral bioavailability of the SLN formulation versus unformulated artemisinin in Wistar rats. Antimalarial efficacy was assessed in Plasmodium berghei-infected mice using the 4-day suppression test. Results: Optimised SLNs demonstrated a mean particle size of 186 nm, zeta potential of -28 mV, and encapsulation efficiency of 79 percent. SLN formulation increased oral bioavailability 3.2-fold and prolonged Tmax compared to free artemisinin. Antimalarial parasitaemia suppression was significantly superior for the SLN formulation (p less than 0.01). Conclusion: Artemisinin-loaded mango kernel lipid nanoparticles represent a promising, locally sourced delivery system with superior pharmacokinetic and antimalarial properties. This formulation strategy offers a pathway toward affordable enhanced malaria therapeutics. Keywords: artemisinin, lipid nanoparticles, bioavailability, mango kernel, malaria

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