中国组织工程研究与临床康复2011，Vol.15Issue(8)：1385-1388,4.DOI:10.3969/j.issn.1673-8225.2011.08.013
新型多肽聚酰胺-胺型靶向药物载体的载药性能及细胞吸收和毒性
Drug loading properties, cell uptake and cytotoxicity of new peptide polyamidoamine targeting drug carrier
摘要
Abstract
BACKGROUND: Previous study screened a peptide (lung cancer targeting peptide, LCTP) which could bind NCI-H460 non-small cell lung cancer (NSCLC) by phage display in vivo. LCTP was combined with modified polyamidoamine (PAMAM)dendritic polymers to prepare nano-targeting drug carrier, PAMAM-Ac-FITC-LCTP. It had good targeting capability to NSCLC in vitro and in vivo.OBJECTIVE: To further study the PAMAM-Ac-FITC-LCTP as a targeting carrier on encapsulation, release, cell uptake, and toxicity properties of doxorubicin (DOX) based on previous research.METHODS: Taking screened peptide LCTP as targeting agent, PAMAM-Ac-FITC-LCTP targeting carrier was constructed.PAMAM-Ac-FITC-LCTP was combined with DOX using physical encapsulation method. The carrier on release fu nction of drug was observed by dialysis experiment in vitro. Confocal microscopy was used to observe cells uptake of the PAMAM-Ac-FITC-LCTP/DOX. Free DOX as controls, the effect of carrier on NCI-H460 cells was observed with MTT assay after the drug carrier.RESULTS AND CONCLUSION: The maximum encapsulation rate of PAMAM-Ac-FITC-LCTP to DOX was 7.46％. The carrier had obvious sustained release effect on DOX, and ion concentration, pH and temperature could affect DOX release. It is indicated that PAMAM-Ac-FITC-LCTP could combined with DOX by electrostatic interaction. PAMAM-Ac-FITC-LCTP/DOX was more efficient than individual drugs into NCI-H460 cells in a short period of time; however, the 24-hour cytotoxicity of complex was similar with DOX. These results suggest that PAMAM-Ac-FITC-LCTP might be a useful drug carrier for cancer treatment and clinical diagnosis.关键词
聚酰胺-胺/多肽/阿霉素/肿瘤靶向/静电作用/药物缓释分类
医药卫生引用本文复制引用
冯丽娜,刘金剑,褚丽萍,杨翠红,王德芝,张春明,刘鉴峰..新型多肽聚酰胺-胺型靶向药物载体的载药性能及细胞吸收和毒性[J].中国组织工程研究与临床康复,2011,15(8):1385-1388,4.基金项目
国家自然科学基金青年项目(30700178),天津市自然科学基金项目(09JCYBJC13400),放射医学研究所学科发展基金项目(SF0627,SF0823,ST1011). （30700178）
