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Structure-activity relationships of fluorinated dendrimers in DNA and siRNA delivery
- Source :
- Acta Biomaterialia. 46:204-210
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Fluorinated dendrimers have shown great promise in gene delivery due to their high transfection efficacy and low cytotoxicity, however, the structure-activity relationships of these polymers still remain unknown. Herein, we synthesized a library of fluorinated dendrimers with different dendrimer generations and fluorination degrees and investigated their behaviors in both DNA and siRNA delivery. The results show that fluorination significantly improves the transfection efficacy of G4-G7 polyamidoamine dendrimers in DNA and siRNA delivery. Fluorination on generation 5 dendrimer yields the most efficient polymers in gene delivery, and the transfection efficacy of fluorinated dendrimers depends on fluorination degree. All the fluorinated dendrimers cause minimal toxicity on the transfected cells at their optimal transfection conditions. This study provides a general and facile strategy to prepare high efficient and low cytotoxic gene carriers based on fluorinated polymers. Statement of Significance The structure-activity relationships of fluorinated dendrimers in gene delivery is still unknown and the behavior of fluorinated dendrimers in siRNA delivery has not yet been investigated. Herein, we synthesized a library of fluorinated PAMAM dendrimers with different dendrimer generations and fluorination degrees and investigated their behaviors in both DNA and siRNA delivery. The results clearly indicate that fluorination significantly improves the transfection efficacy of dendrimers in both DNA and siRNA delivery without causing additional toxicity. G5 PAMAM dendrimer is best scaffold to synthesize fluorinated dendrimers and the transfection efficacy of fluorinated dendrimers depends on fluorination degree. This systematic study provides a general and facile strategy to prepare high efficient and low cytotoxic gene carriers based on fluorinated polymers.
- Subjects :
- Dendrimers
Materials science
Halogenation
Green Fluorescent Proteins
Biomedical Engineering
02 engineering and technology
Gene delivery
Transfection
010402 general chemistry
01 natural sciences
Biochemistry
Biomaterials
Structure-Activity Relationship
chemistry.chemical_compound
Dendrimer
Humans
Structure–activity relationship
RNA, Small Interfering
Cytotoxicity
Molecular Biology
chemistry.chemical_classification
Benzoxazoles
Cell Death
Gene carrier
Quinolinium Compounds
Gene Transfer Techniques
DNA
General Medicine
Polymer
021001 nanoscience & nanotechnology
Combinatorial chemistry
0104 chemical sciences
chemistry
0210 nano-technology
HeLa Cells
Biotechnology
Subjects
Details
- ISSN :
- 17427061
- Volume :
- 46
- Database :
- OpenAIRE
- Journal :
- Acta Biomaterialia
- Accession number :
- edsair.doi.dedup.....333eca501eabcbc1ecaf019dc17c7b41