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.
Ren
Tianbin
T
Institute of Nano and Bio-Polymeric Materials, Tongji University, Shanghai 200092, People's Republic of China.
Xu
Nan
N
Cao
Chunhong
C
Yuan
Weizhong
W
Yu
Xiao
X
Chen
Jianghan
J
Ren
Jie
J
D000666:Amphotericin B / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001812:Blood-Brain Barrier / Q000378:metabolism; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003455:Cryptococcus neoformans / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D006403:Hematologic Tests; D007668:Kidney / Q000187:drug effects / Q000378:metabolism; D007773:Lactates / Q000737:chemistry*; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D016919:Meningitis, Cryptococcal / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D011092:Polyethylene Glycols / Q000737:chemistry*; D011136:Polysorbates / Q000737:chemistry*
D000890:Anti-Infective Agents; D004337:Drug Carriers; D007773:Lactates; D011136:Polysorbates; C088513:poly(lactic acid-ethylene glycol); D011092:Polyethylene Glycols; D000666:Amphotericin B