Nanostructured Lipid Carriers (NLCs) of Lumefantrine with Enhanced Permeation

Purpose Lumefantrine (LF) is an antimalarial agent with low water solubility and inconsistent oral bioavailability (4–11%), which limits its therapeutic potential. Hence, this research aimed to design nanostructured lipid carriers (NLCs) for LF to improve its oral administration. Methods LF-NLCs were formulated using the hot emulsification-probe sonication method. Solubility and molecular interactions studies were performed for the selection of appropriate formulation excipients. Various critical formulation and process variables were optimized during this process. The optimized LF-NLC was then evaluated for various physicochemical properties. Ex vivo gut permeation was done to analyze LF-NLC permeation across the gut, and in vitro drug release was performed to understand its release behavior. Results Particle size, polydispersity index (PDI), zeta potential, and % encapsulation efficiency of the optimized formulation were found to be 78.85 ± 2.55 nm, 0.255 ± 0.03, -8.25 ± 2.29 mV, and 74.32 ± 1.63%, respectively. Transmission electron microscopy revealed the particulate nature and spherical shape of LF-NLCs. The loss of sharp endothermic peak in DSC and reduced crystallinity in XRD indicated the amorphization of encapsulated drug. The in vitro drug release study showed sustained release of LF from NLC. Ex vivo gut permeation exhibited an almost 3.5-fold increase in permeation of NLCs over plain drug suspension. Conclusion According to the above findings, NLC could be a promising approach for the oral delivery of LF and drugs with similar properties.