期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 535, 期 1-2, 页码 180-193出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2017.11.015
关键词
Poly(beta-amino ester)s; Fluorination; Biocompatibility; Transfection
资金
- National Natural Science Foundation of China [81773667, 81573369]
- Natural Science Foundation of Jiangsu Province [BK20140659]
- National Science and Technology Major Project [2017YFA0205400]
- Project Program of State Key Laboratory of Natural Medicines of China Pharmaceutical University [SKLNMZZJQ201601]
- National High Technology Research and Development Program of China (863 Program) [2015AA020314]
- Outstanding Youth Fund of Jiangsu Province of China [BK20160031]
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
- 111 Project from the Ministry of Education of China
- State Administration of Foreign Experts Affairs of China [B16046]
Cationic polymers have been widely used as one of the most promising non-viral vehicles for gene delivery due to their potential safety and ease of large-scale production. Here, we report the design and synthesis of a series of novel biodegradable fluorinated poly(beta-amino ester) s (FPBAEs) by simple Michael-addition reaction as safe and efficient gene carrier. The results of transfection efficacy assay demonstrated the optimal FPBAE could mediated much higher GFP expression than the commercial transfection agents, polyethyleneimine (PEI, M-w = 25K) and Lipo 2000, as well as the non-fluorinated poly(beta-amino ester) s (PBAE) on both HeLa and HEK-293T cell lines (higher than 70 and 90%, respectively), which was largely attributed to fluorination. Moreover, MTT and hemolysis assay indicated a preferable biocompatibility of FPBAE compared with PEI 25K owing to the low molecular weight and the presence of cleavable ester bonds. Taken together, the novel polymer FPBAE with both excellent gene transfection efficacy and much lower toxicity could serve as a desirable gene vector.
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