Novel nanostructured lipid carrier for oral delivery of a poorly soluble antimalarial agent lumefantrine: characterization and pharmacokinetics evaluation

Guihua Huang, Jingjing Liu, Liu Tian, Shilei Chen
2018 MOJ Bioequivalence & Bioavailability  
The objective of this study was to design nanostructured lipid carriers (NLC) for the oral delivery of a poorly soluble antimalarial agent lumefantrine (LFN), which could increase the solubility and oral bioavailability of LFN, with the aim to further improve therapeutic efficacy. The lumefantrine-nanostructured lipid carriers (LFN-NLC) were prepared by the method of ultrasonication. Based on the optimized results of single-factor screening experiment, LFN-NLC was found to be relatively uniform
more » ... in size (213.30±8.54) nm with a narrow polydispersity index (PDI) (0.192±0.02). The average entrapment efficiency (EE) and drug loading (DL) were (94.90±0.51)% and (9.05±0.19)%, respectively. The differential scanning calorimetry (DSC) analysis showed that LNF was not in crystalline state in LNF-NlC. In vivo studies indicated that LFN-NLC showed higher AUC and C max values compared with LFN-suspension after oral administration to rats. The decrease of t max and two absorption peaks indicated that LFN can be absorbed into blood faster and have higher therapeutic efficacy after encapsulated into the NLC. These encouraging results revealed that LFN-NLC would be an promising carrier for LNF to increase therapeutic efficacy on malaria. Citation: Liu J, Tian L, Chen S, et al. Novel nanostructured lipid carrier for oral delivery of a poorly soluble antimalarial agent lumefantrine: characterization and pharmacokinetics evaluation.
doi:10.15406/mojbb.2018.05.00079 fatcat:sgurtwltaja4rkqnpiuz55eps4