Ren Tianbin, Xu Nan, Cao Chunhong, Yuan Weizhong, Yu Xiao, Chen Jianghan, Ren Jie
Institute of Nano and Bio-Polymeric Materials, Tongji University, Shanghai 200092, People's Republic of China.
J Biomater Sci Polym Ed. 2009;20(10):1369-80. doi: 10.1163/092050609X12457418779185.
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.
通过纳米沉淀法制备了聚山梨酯80（吐温80）包被的两性霉素B（AmB）/聚乳酸-b-聚乙二醇（PLA-b-PEG）纳米颗粒，用于穿越血脑屏障（BBB）。研究了吐温80对AmB/PLA-b-PEG纳米颗粒的尺寸和分布、包封率及释放行为的影响。此外，还研究了包被纳米颗粒的脑靶向性和治疗效果。用吐温80包被纳米颗粒时，包封率显著提高。所制备的纳米颗粒呈球形，分布均匀。小鼠脑内药物浓度大大提高，这表明包被的纳米颗粒能够穿越血脑屏障。同时，AmB/PLA-b-PEG纳米颗粒能够降低AmB对肝脏、肾脏和血液系统的毒性，并提高治疗效果。
