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

Abstract

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 in size plusmn nm with a narrow polydispersity index PDI plusmn The average entrapment efficiency EE and drug loading DL were plusmn and plusmn 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 Cmax values compared with LFN suspension after oral administration to rats The decrease of tmax 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