Amphotericin B-entrapping lipid nanoparticles and their in vitro and in vivo characteristics

Suk Hyun Jung, Deok Hwi Lim, Soon Hwa Jung, Jung Eun Lee, Kyu Sung Jeong, Hasoo Seong, Byung Cheol Shin

Research output: Contribution to journalArticle

73 Citations (Scopus)

Abstract

Lipid nanoparticles (LNPs) as nano-scale drug carriers that can entrap poorly water-soluble drugs such as amphotericin B (AmB) in aqueous solution with high drug entrapment efficiency were developed and their in vitro and in vivo characteristics were investigated. The AmB-entrapping plain, anionic and PEG (polyethylene glycol)-LNPs were prepared by using spontaneous emulsification and solvent evaporation (SESE) method. Mean particle size of the AmB-entrapping LNPs ranged from 72.9 to 159.1 nm according to a variation of their lipid composition. The surface of AmB-entrapping PEG (0.2)-LNPs having 84.4 ± 6 nm of particle size was negatively charged showing -50.4 ± 5 mV of zeta-potential value. Entrapment efficiency of AmB in the PEG-LNPs reached up to 76.5 ± 5%. Cytotoxicity of the AmB-entrapping LNPs against human kidney cells, 293 cells, was lower than those of the commercialized AmB-formulations such as Fungizone® and AmBisome®. Hematotoxicity of the AmB-entrapping LNPs against red blood cells was much lower than that of Fungizone® but comparable to AmBisome®. Antifungal activity in vitro of AmB-entrapping LNPs against Candida albicans and Aspergillus fumigatus was better than the commercialized AmB formulations showing their low minimum inhibitory concentration (MIC) for 90% of growth inhibition of fungi. The AmB-entrapping LNPs increased circulation half life of AmB in blood stream and it was comparable to AmBisome®. Antifungal activity in vivo of the AmB-entrapping PEG-LNPs against Aspergillus fumigatus (ATCC 16424)-infected mice was superior to that of AmBisome®. The drug-entrapping LNPs, especially PEG-LNPs, can be applicable to entrapment of poorly water-soluble drugs and enhancement of therapeutic efficacy by modulating pharmacokinetic behaviors and/or drug-related toxicities. Crown

Original languageEnglish
Pages (from-to)313-320
Number of pages8
JournalEuropean Journal of Pharmaceutical Sciences
Volume37
Issue number3-4
DOIs
Publication statusPublished - 2009 Jun 28

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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