采用固体脂质纳米粒实现10-羟基喜树碱的细胞内靶点递送以对抗多药耐药性。
Intracellular target delivery of 10-hydroxycamptothecin with solid lipid nanoparticles against multidrug resistance.
作者信息
Liu Min, Chen Didi, Wang Chenxu, Chen Xunhu, Wen Zhili, Cao Yu, He Hongxuan
机构信息
a Key Laboratory of Pesticide and Chemical Biology (Ministry of Education), College of Chemistry, Central China Normal University , Wuhan , People's Republic of China and.
b National Research Center for Wild life Born Diseases, Key Laboratory of Animal Ecology and Conservation Biology, Institute of Zoology, Chinese Academy of Sciences , Beijing , China.
出版信息
J Drug Target. 2015;23(9):800-5. doi: 10.3109/1061186X.2015.1020427. Epub 2015 Mar 13.
The main objective of this study was to design a suitable drug delivery system for 10-hydroxycamptothecin (HCPT). In this study, HCPT-loaded solid lipid nanoparticle (HCPT-loaded SLN) was successfully prepared. The HCPT-loaded SLN was characterized by size, entrapment efficiency and drug release manner. The cytotoxicity of HCPT-loaded SLN was assessed in vitro using HepG2/HCPT cells and in vivo utilizing human tumor xenograft nude mouse model. HCPT-loaded SLN indicated the ability to target HepG2/HCPT cells and accumulated higher drug content in HepG2/HCPT cells. HCPT-loaded SLN enhanced the cytotoxicity of HCPT in a concentration-dependent manner. Based on these results, HCPT-loaded SLN suggested being a promising vehicle for liver-targeted drug delivery. Moreover, it can be of clinical interest to overcome multidrug resistance (MDR) effectively.
本研究的主要目的是为10-羟基喜树碱（HCPT）设计一种合适的药物递送系统。在本研究中，成功制备了载有HCPT的固体脂质纳米粒（HCPT-SLN）。通过粒径、包封率和药物释放方式对HCPT-SLN进行了表征。使用HepG2/HCPT细胞在体外评估了HCPT-SLN的细胞毒性，并利用人肿瘤异种移植裸鼠模型在体内进行了评估。HCPT-SLN显示出靶向HepG2/HCPT细胞的能力，并在HepG2/HCPT细胞中积累了更高的药物含量。HCPT-SLN以浓度依赖的方式增强了HCPT的细胞毒性。基于这些结果，HCPT-SLN有望成为肝靶向药物递送的载体。此外，有效克服多药耐药性（MDR）可能具有临床意义。
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