奥曲肽
生长抑素受体
生长抑素
受体
共轭体系
癌症研究
肿瘤细胞
化学
生长抑素受体2
医学
药理学
内科学
聚合物
有机化学
作者
Jianqing Peng,Xiaole Qi,Yi Chen,Ning Ma,Ziwei Zhang,Jiaxu Xing,Xuehua Zhu,Zhengrong Li,Zhenghong Wu
标识
DOI:10.3109/1061186x.2013.879386
摘要
Purpose: An octreotide-conjugated polyamidoamine (PAMAM) dendrimer was synthesized and employed as nanocarriers of methotrexate (MTX), for targeting to the somatostatin receptors over-expressed tumor cells.Methods: PAMAM–PEG–octreotide (PPO) and PAMAM–PEG (PPG) were synthesized and characterized. The cellular uptake of fluorescein isothiocyanate (FITC)-labeled PPO (PPO-FITC) and PPG (PPG-FITC) were investigated. The cytotoxicity of MTX and MTX nanoparticles were conducted in the MCF-7 cells. Besides, the pharmacokinetics studies on MTX nanoparticles were carried out in rats.Results: The structure of PPO was verified by NMR detection and the diameter was 11.05 ± 1.80 nm, with the amount of MTX encapsulated by PPO was 30 (molecule/molecule). MTX nanoparticles possessed significantly higher cytotoxicity against MCF-7 cells compared with free MTX, especially the PPO/MTX nanoparticles. Correspondingly, the PPO-FITC carrier had higher cellular uptake efficiency compared to PPG-FITC. In addition, pharmacokinetics studies showed that PPO/MTX nanoparticles increased mean residence time and bioavailability of MTX distinctly.Discussion and conclusion: With further cellular uptake test of FITC-labeled carriers, the enhanced cytotoxicity of PPO/MTX nanoparticles was reasonable to ascribe to the specific receptor-mediated endocytosis induced by octreotide. The present study suggests that this PAMAM–PEG–octreotide nanocarrier opens a new path for treating cancer with higher efficacy.
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