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Research Article Volume 5 Issue 1
Novel nanostructured lipid carrier for oral delivery of a poorly soluble antimalarial agent lumefantrine: characterization and pharmacokinetics evaluation
Jingjing Liu, Liu Tian, Shilei Chen, Guihua Huang
School of Pharmaceutical Sciences, Shandong University, China
Received: January 03, 2018 | Published: February 7, 2018
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. MOJ Bioequiv Availab. 2018;5(1):33-38. DOI: 10.15406/mojbb.2018.05.00079
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 (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 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.
Keywords: lumefantrine, malaria, nanostructured lipid carriers, oral delivery, pharmacokinetics, bio-availability, polydispersity, efficiency, soybean, monostearin, stearic acid, oleic acid, calorimetry, hepatocytes, therapeutic efficacy, anti-parasitic, chlorobenzylidene, nonoliposomes, solubility, morphology
©2018 Liu, et al. This is an open access article distributed under the terms of the, which permits unrestricted use, distribution, and build upon your work non-commercially.