Study of amphotericin B magnetic liposomes for brain targeting

Int J Pharm. 2014 Nov 20;475(1-2):9-16. doi: 10.1016/j.ijpharm.2014.08.035. Epub 2014 Aug 21.

Abstract

This study aims to prepare amphotericin B magnetic liposomes (AmB-MLPs), which may improve drug concentration in brain, enhance magnetic targeting for brain and reduce drug toxicity in the presence of magnetic field. AmB-MLPs were prepared by means of film dispersion-ultrasonication, and their physical properties were characterized. In vivo, the magnetic targeting for brain by carotid artery administration was investigated. The particle size of AmB-MLPs was 240±11 nm, the encapsulation efficiency was 79.32±2.03%, and the saturation magnetization was 32.54 memu g⁻¹ at room temperature, which had good magnetic responsiveness. The group of AmB injection was delivered by carotid artery, nevertheless they all died after 20 min. AmB-MLPs were injected by carotid artery, and the drug concentration in brain tissue was obviously increased in presence of magnetic field than that of in absence of magnetic field (P<0.05). The Prussian blue staining in brain of SD rats showed that the density of blue staining-positive particles in brain tissue of applying magnetic field group was higher than that of non magnetic field group. These results suggested that AmB-MLPs could reinforce brain targeting and reduce drug toxicity when they were injected by carotid artery under the effect of magnetic field.

Keywords: Amphotericin B; Brain targeting; Carotid artery administration; Magnetic liposomes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphotericin B / administration & dosage*
  • Amphotericin B / adverse effects
  • Amphotericin B / metabolism
  • Amphotericin B / pharmacokinetics
  • Animals
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / adverse effects
  • Antifungal Agents / metabolism
  • Antifungal Agents / pharmacokinetics
  • Blood-Brain Barrier / drug effects
  • Blood-Brain Barrier / metabolism*
  • Brain / drug effects
  • Brain / metabolism
  • Carotid Arteries
  • Cholesterol / adverse effects
  • Cholesterol / chemistry
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / adverse effects
  • Delayed-Action Preparations / metabolism
  • Delayed-Action Preparations / pharmacokinetics
  • Drug Carriers / administration & dosage*
  • Drug Carriers / adverse effects
  • Drug Carriers / metabolism
  • Drug Carriers / pharmacokinetics
  • Drug Compounding
  • Injections, Intravenous
  • Liposomes
  • Magnetic Phenomena*
  • Magnetite Nanoparticles / adverse effects
  • Magnetite Nanoparticles / chemistry*
  • Magnetite Nanoparticles / ultrastructure
  • Neurons / drug effects
  • Neurons / metabolism
  • Particle Size
  • Phosphatidylcholines / adverse effects
  • Phosphatidylcholines / chemistry
  • Rats, Sprague-Dawley
  • Tissue Distribution
  • Up-Regulation*

Substances

  • Antifungal Agents
  • Delayed-Action Preparations
  • Drug Carriers
  • Liposomes
  • Magnetite Nanoparticles
  • Phosphatidylcholines
  • Amphotericin B
  • Cholesterol