title: Stability and antimicrobial effect of amikacin-loaded solid lipid nanoparticles.
abstract: Solid lipid nanoparticles (SLNs) of amikacin were designed in this study for pulmonary delivery to reduce the dose or its administration intervals leading to reduction of its toxicities especially in long term treatment. Nanoparticles of amikacin were prepared from cholesterol by solvent diffusion technique and homogenization. The size, zeta potential, loading efficiency, and release profile of the nanoparticles were studied. The conventional broth macrodilution tube method was used to determine the minimum inhibitory concentration (MIC) and minimum bacteriostatic concentration (MBC) of amikacin SLNs with respect to Pseudomonas aeruginosa in vitro. To guarantee the stability of desired SLNs, they were lyophilized using cryoprotectants. Results showed that considering the release profile of amikacin from the studied nanocarrier, MIC and MBC of amikacin could be about two times less in SLNs of amikacin compared to the free drug. Therefore, fewer doses of amikacin in SLNs can clear the infection with less adverse effects and more safety. Particle size enlargement after lyophilization of desired SLNs after two months storage was limited in comparison with non-lyophilized particles, 996 and 194 nm, respectively. Zeta potential of lyophilized particles was increased to +17 mV from +4 mV before lyophilization. Storage of particles in higher temperature caused accelerated drug release.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy and Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
authors.forename: Solmaz
authors.initials: S
authors.lastname: Ghaffari
authors.forename: Jaleh
authors.initials: J
authors.lastname: Varshosaz
authors.forename: Afrooz
authors.initials: A
authors.lastname: Saadat
authors.forename: Fatemeh
authors.initials: F
authors.lastname: Atyabi
mesh_terms: D000583:Amikacin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D002784:Cholesterol / Q000008:administration & dosage / Q000737:chemistry; D004355:Drug Stability; D005612:Freeze Drying; D008826:Microbial Sensitivity Tests; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013696:Temperature
chemical_list: D000900:Anti-Bacterial Agents; D000583:Amikacin; D002784:Cholesterol