Preparation and Therapeutic Efficacy of Polysorbate-80-Coated Amphotericin B/PLA-b-PEG Nanoparticles

Amphotericin B (AmB)/poly(lactic acid)-b-poly(ethylene glycol) (PLA-b-PEG) nanoparticles coated with polysorbate 80 (Tween-80) were prepared by nanoprecipitation for transport across the blood-brain barrier (BBB). The effects of Tween-80 on the size and distribution, entrapment efficiency and release behavior of AmB/PLA-b-PEG nanoparticles were investigated. Furthermore, the brain targeting and curative effect of coated nanoparticles were also investigated. The entrapment efficiency was significantly enhanced when nanoparticles were coated with Tween-80. The prepared nanoparticles were spherical with homogeneous distribution. Drug concentration in mice brain was greatly enhanced, which indicated that the coated nanoparticles could get across the BBB. Meanwhile, the AmB/PLA-b-PEG nanoparticles are able to reduce the toxicity of AmB to liver, kidney and blood system with improved therapeutic effect. (C) Koninklijke Brill NV, Leiden, 2009