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

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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

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Amphotericin B
Nanoparticles
Lipids
Aspergillus fumigatus
In Vitro Techniques
Particle Size
Pharmaceutical Preparations
Efficiency
Drug Carriers
Water
Microbial Sensitivity Tests
Drug-Related Side Effects and Adverse Reactions
Crowns
Candida albicans
Half-Life

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Jung, Suk Hyun ; Lim, Deok Hwi ; Jung, Soon Hwa ; Lee, Jung Eun ; Jeong, Kyu-Sung ; Seong, Hasoo ; Shin, Byung Cheol. / Amphotericin B-entrapping lipid nanoparticles and their in vitro and in vivo characteristics. In: European Journal of Pharmaceutical Sciences. 2009 ; Vol. 37, No. 3-4. pp. 313-320.
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Amphotericin B-entrapping lipid nanoparticles and their in vitro and in vivo characteristics. / Jung, Suk Hyun; Lim, Deok Hwi; Jung, Soon Hwa; Lee, Jung Eun; Jeong, Kyu-Sung; Seong, Hasoo; Shin, Byung Cheol.

In: European Journal of Pharmaceutical Sciences, Vol. 37, No. 3-4, 28.06.2009, p. 313-320.

Research output: Contribution to journalArticle

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AU - Jung, Suk Hyun

AU - Lim, Deok Hwi

AU - Jung, Soon Hwa

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AU - Jeong, Kyu-Sung

AU - Seong, Hasoo

AU - Shin, Byung Cheol

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