摘要
合成了一种甘露醇引发的星型共聚物甘露醇-聚乳酸-聚乙三醇1000维生素E琥珀酸酯(M-PLATPGS).利用纳米沉淀法制备载紫杉醇M-PLA-TPGS纳米颗粒.纳米颗粒近似球形,粒径分布较窄.对载药纳米颗粒进行粒径、表面电荷、载药量、包封率和体外药物释放的表征,结果表明,体外药物释放呈双相释放模型,M-PLA-TPGS纳米颗粒在前列腺癌PC-3细胞中的摄取水平要高于PLGA和PLA-TPGS纳米颗粒.载紫杉醇M-PLA-TPGS纳米颗粒对于前列腺癌细胞的的毒性显著高于载紫杉醇PLA-TPGS纳米颗粒和商业制剂Taxol,证明星型M-PLA-TPGS聚合物作为纳米药物载体优于线性PLGA和PLA-TPGS聚合物.
The objective of this research is to fabricate novel nanoparticles （NPs） of star-shaped mannitolfunctionalized polylactic acid-D-a-tocopheryl polyethylene glycol 1000 suelinat（PLA-TPGS） copolymer for paelitaxel delivery for prostate cancer treatment, and evaluate their therapeutic effects in prostate cancer cell line in comparison with the linear PLGA NPs and PLA-TPGS NPs. The paclitaxel-loaded M-PLA-TPGS NPs, prepared by a modified nano-precipitation method, were observed by field emission scanning electron microscopy （FESEM） to be near-spherical shape with narrow size distribution. The drug-loaded NPs were further characterized in terms of size, surface charge, drug content, encapsulation efficiency and in vitro drug release. In vitro drug release exhibited biphasic pattern with initial burst release followed by slow and continuous release. The cellular uptake level of M-PLA-TPGS NPs was demonstrated higher than linear PLGA NPs and PLA-TPGS NPs in PC-3 cells. The data also showed that the paclitaxel-loaded M-PLA-TPGS nanoparticles have higher antitumor efficacy than that of linear PLA-TPGS nanoparticles and commercial Taxol in vitro. The star-shaped co- polymer M-PLA-TPGS could be used as a potential and promising molecular biomaterial applied in developing novel nanoformulation for prostate cancer treatment.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2014年第10期2239-2245,共7页
Chemical Journal of Chinese Universities
基金
国家自然科学基金(批准号:81100100,51103180,31200674)资助~~
