Preparation and evaluation of PEG-PCL nanoparticles for local tetradrine delivery
Preparation and evaluation of PEG-PCL nanoparticles for local tetradrine delivery
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用于局部粉防己碱递送的 PEG-PCL 纳米颗粒的制备和评价。
DOI：
10.1016/j.ijpharm.2009.06.007
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发表时间：
2009-09-08
影响因子：
5.8
通讯作者：
Liu, Baorui
中科院分区：
文献类型：
--
作者：
Li, Rutian;Li, Xiaolin;Liu, Baorui
为了建立令人满意的粉防己碱局部递送系统，以甲氧基聚乙二醇-聚己内酯二嵌段共聚物（MePEG-PCL）和聚己内酯-聚乙二醇-聚己内酯三嵌段共聚物（PCL-PEG-PCL）制备了四种核壳纳米粒子。研究了四种纳米颗粒的理化特性，包括形态、粒径、zeta电位、载药量、稳定性和体外释放曲线。我们还通过体外细胞摄取实验、对LoVo细胞的细胞毒性测定和生物相容性研究评估了四种纳米颗粒。组织培养药物反应测定（HDRA）是一种通常用于评估化学敏感性的更具预测性的方法，在我们的研究中首先应用来评估聚合物纳米粒子的抗肿瘤效力。目前的研究表明，四种共聚物均表现出显着的体外抗肿瘤作用，尤其是在HDRA检测中。共聚物的构型和组成对于纳米颗粒的性能和功能很重要。由二嵌段共聚物制备的粒径约为300 nm、疏水成分约为80%的纳米颗粒被确定为最有效的药物载体，有待进一步研究。 (C) 2009 Elsevier B.V. 保留所有权利。
To establish a satisfactory delivery system for local delivery of Tetradrine Jet), four kinds of core-shell nanoparticles were prepared from di-block copolymer of methoxy poly(ethylene glycol)-polycaprolactone (MePEG-PCL) and tri-block copolymer of polycaprolactone-poly(ethylene glycol)-polycaprolactone (PCL-PEG-PCL). The physiochemical traits of the four kinds of nanoparticles including morphology, particle size, zeta-potential, drug-loading content, stability, and in vitro release profile were studied. We also evaluated the four kinds of nanoparticles by in vitro cellular uptake experiment, cytotoxicity assay against LoVo cells, and biocmpatibility study. Histoculture Drug Response Assay (HDRA), a more predictive method usually used to evaluate chemosensitivity was firstly applied in our study to evaluate the antitumor potency of polymeric nanoparticles. The current study showed that all the four kinds of copolymers exhibited remarkable in vitro antitumor effects, especially in HDRA assay. The configuration and composition of the copolymers were important for the properties and functions of the nanoparticles. Nanoparticles prepared from the di-block copolymer with a particle size around 300 nm and the hydrophobic composition about 80% was determined as the most effective drug carrier for further studies. (C) 2009 Elsevier B.V. All rights reserved.