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Eur J Pharm Sci. 2016 Oct 10;93:392-8. doi: 10.1016/j.ejps.2016.08.049. Epub 2016 Aug 26.

Amikacin loaded PLGA nanoparticles against Pseudomonas aeruginosa.

Author information

1
Department of Microbiology, Faculty of Biological Sciences, Alzahra University, Tehran, Iran; Department of Microbiology and Parasitology, University of Navarra, Pamplona, Spain; Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Pamplona, Spain.
2
Department of Microbiology, Faculty of Biological Sciences, Alzahra University, Tehran, Iran.
3
Department of Microbiology and Parasitology, University of Navarra, Pamplona, Spain. Electronic address: cgamazo@unav.es.
4
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Pamplona, Spain.

Abstract

Amikacin is a very effective aminoglycoside antibiotic but according to its high toxicity, the use of this antibiotic has been limited. The aim of this study was to formulate and characterize amikacin loaded PLGA nanoparticles. Nanoparticles were synthetized using a solid-in-oil-in-water emulsion technique with different ratio of PLGA 50:50 (Resomer 502H) to drug (100:3.5, 80:3.5 and 60:3.5), two different concentrations of stabilizer (pluronic F68) (0.5% or 1%) and varied g forces to recover the final products. The most efficient formulation based on drug loading (26.0±1.3μg/mg nanoparticle) and encapsulation efficiency (76.8±3.8%) was the one obtained with 100:3.5 PLGA:drug and 0.5% luronic F68, recovered by 20,000×g for 20min. Drug release kinetic study indicated that about 50% of the encapsulated drug was released during the first hour of incubation in phospahte buffer, pH7.4, 37°C, 120rpm. Using different cell viability/cytotoxicity assays, the optimized formulation showed no toxicity against RAW macrophages after 2 and 24h of exposure. Furthermore, released drug was active and maintained its bactericidal activity against Pseudomonas aeruginosa in vitro. These results support the effective utilization of the PLGA nanoparticle formulation for amikacin in further in vivo studies.

KEYWORDS:

Amikacin; Formulation; Optimization; PLGA; Pseudomonas aeruginosa

PMID:
27575877
DOI:
10.1016/j.ejps.2016.08.049
[Indexed for MEDLINE]

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