• Applied Chemistry for Engineering
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• v.34 no.1
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• pp.1-8
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• 2023

Polyethylenimine (PEI) is a cationic polymer that can bind to negatively charged biomaterials such as nucleic acids through strong electrostatic interactions. Based on these properties, PEI has been used as an efficient drug delivery system for a long time. However, the strong cationic nature of PEI has the problem of causing cytotoxicity by non-specific interaction with anionic biological materials in the cells. In order to overcome these problems, many researchers have developed various types of biocompatible PEI-based materials. In this review, we would like to introduce the recent developments of functional PEI and their applications in biomedical research.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.315.2-316
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• 2003

Polyethylenimine (PEI) has been used as a non-viral gene delivery carrier. To improve the efficacy of transfection, transferrin was incorporated by covalent linkage to PEI. As a model plasmid DNA, pHME185/b-gal, a mammalian expression vector was used. The transferrin-polyethylenimine (TfPEI) was synthesized by conjugate PEI with transferrin using sodium periodateand and characterized by FT-IR and 1H-NMR. (omitted)

• Journal of Industrial and Engineering Chemistry
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• v.67
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• pp.284-292
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• 2018

Receptor for advanced glycation end-products (RAGE) is overexpressed in various cancer cells. In this study, a RAGE-binding peptide (RBP) was conjugated to polyethylenimine (25 kDa, PEI). RBP-conjugated PEI (PEI-RBP) was characterized as a dual-functional reagent, a RAGE-mediated gene carrier and an anti-angiogenic reagent. As a gene carrier, PEI-RBP had higher transfection efficiency to the C6 glioblastoma cells than PEI. As an anti-angiogenic reagent, the pEmpty/PEI-RBP complex reduced RAGE expression on the surface of the C6 glioblastoma cells. Also, the complex reduced the VEGF expression and tube formation of endothelial cells. Therefore, PEI-RBP may be useful for development of glioblastoma therapy.

• Bulletin of the Korean Chemical Society
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• v.28 no.1
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• pp.95-98
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• 2007

Polyethylenimine (PEI) has been widely investigated for delivery of DNA into cells. It was previously reported that there were at least two types of cytotoxicity in PEI-mediated gene delivery, immediate and delayed toxicities. PEI-mediated gene delivery protocols use net cationic complexes with an excess of PEI to maintain equilibrium between the complexed and dissociated forms in solution. In this study, toxicity of free PEI or PEI/ DNA complex was investigated. Human embryonic kidney 293 cells were incubated with free PEI or PEI/DNA complex for 4 hrs. Then, the cells were analyzed at 6, 24, 48, and 96 hrs after the incubation. In MTT assay, the viability of the cells incubated with PEI/DNA complex was continuously decreased with time, while that of the cells incubated with free PEI was not. On the contrary, the expression level of the luciferase gene increased gradually along with time. Release of DNAs from the complexes for transcription produces free PEIs in the cells. This process may proceed slowly due to high charge density of PEI and may be related to delayed toxicity. In addition, apoptotic cells were observed only in the cells incubated with the PEI/DNA complex from 24 hrs after the incubation. The results suggest that PEI/DNA complex contributes to the delayed toxicity by inducing apoptosis and that the delayed toxicity may be related to decomplexation of the complexes in the cells.

• Biotechnology and Bioprocess Engineering:BBE
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• v.6 no.4
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• pp.269-273
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• 2001

This study presents a new formulation method for improving DNA transfection effi-ciency using a fusogenic peptide and polyethylene glycol-grafted polyethylenimine. Succinimidyls succinate polyethylene glycol (PEG-SSA) was conjugated with polyethylenimine(PEL). PEL is well known for a good endosomal escaping and DNA condensign agent. The positively charged syn-thetic fusogenic peptide, KALA was coated on the negatively charged PEG-g-PEI/DNA and PEI/DNA complexes. The KALA/PEI/ DNA complexes exhibited aggregation behavior at higher KALA coating amount with an effective diameter of around 1,000 nm. However, the LALA/PEG-g-PEI/DNA complexes were 100-300 nm in size with a surface zeta-potential (ζ)value of about +20mV. The conjugated PEG molecules suppressed any KALA-mediated inter-particle aggregation, and thereby improved the transfection efficiency, Consequently, the transfection efficiency of the KALA/PEG-g-PEI/DNA complexes was obtained by utilizing both the fusogenic activity of KALA and the steric repulsion effect of PEC.

• Bulletin of the Korean Chemical Society
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• v.27 no.9
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• pp.1335-1340
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• 2006

It has been found that a number of diseases are associated with mutations in the mitochondrial DNA. Therapeutic gene delivery to mitochondria has been suggested as a clinical option for these diseases. In this study, we developed a gene carrier to mitochondria by the conjugation of mitochondrial leader peptide (LP) to polyethylenimine (PEI). Mitochondrial LP conjugated PEI (PEI-LP) was synthesized with low molecular weight PEI (2,000 Da, PEI2K). Gel retardation assay showed that PEI2K-LP formed complexes at a 1.0/1 weight ratio. In addition, PEI2K-LP protected DNA from the enzymatic degradation for at least 60 min, while naked DNA was completely degraded within 20 min. PEI2K-LP was compared with LP conjugated high molecular weight PEI (25,000 Da, PEI25K) in terms of toxicity and delivery efficiency. MTT assay showed that PEI2K-LP had much lower cytotoxicity than PEI25K-LP to 293 cells. In addition, cell-free DNA delivery assay showed that PEI2K-LP delivered more DNA to mitochondria at a 1.8/1 weight ratio than naked DNA or PEI. This result suggests that PEI2K-LP may be useful for the development of mitochondrial gene therapy system with lower cytotoxicity.

• Bulletin of the Korean Chemical Society
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• v.22 no.1
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• pp.46-52
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• 2001

To evaluate the non-ionic polymer, poly(ethylene glycol) (PEG), as a component in cationic copolymers for non-viral gene delivery systems, PEG was coupled to polyethylenimine (PEI). We present the effects of different degrees and shapes of pegylation of PEI on cytotoxicity, water solubility and transfection efficiency. This work reports the synthesis and characterization of a series of cationic copolymers on the basis of the conjugates of PEI with PEG. The modified molecules were significantly less toxic than the original polymer. Moreover, the chemical modification led to enhancement of their solubility. The comparison of pegylated PEIs with different degrees of derivation showed that all the polymers tested reached comparable levels of transgene expression to that of native PEI. As assessed by agarose gel electrophoresis, even highly substituted PEI derivatives were still able to form polyionic complexes with DNA. However, aside from an increase in solubility and retention of the ability to condense DNA, methoxy-PEG-modified PEIs resulted in a significant decrease in the transfection activity of the DNA complexes. In fact, the efficiency of the copolymer was compromised even at a low degree of modification suggesting that the PEG action resulting from its shape is important for efficient gene transfer. The mode of PEG grafting and the degree of modification influenced the transfection efficiency of PEI.

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.17-23
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• 2005

Polyethylenimine (PEI) has been used as cationic polymers for efficient gene transfer without the need for endosomolytic agents. Various kinds of PEIs with different molecular weight were tested in order to investigate the effects of the molecular weight of PEI on the transfection efficiency and cell cytotoxicity. The ${\beta}-galactosidase$ expression $(pCMV-{\beta}-gal)$ plasmid was used as a model DNA. Complex formation between PEI and pDNA was assessed by 1% agarose gel electrophoresis method. Particle size and zeta-potential of complexes were determined by electrophoretic light scattering spectrometer. In vitro transfection efficiency was assayed by measuring ${\beta}-galactosidase$ activity. Cell cytotoxicity was determined by MTT assay. Particle sizes of the complexes became smaller on increasing molecular weights of PEI and N/P ratios. Surface potential of complexes was increased as the molecular weight of PEI increased. Transfection efficiency of $pCMV-{\beta}-ga1$ on the HEK 293 cells was greatest with PEI 25 K system but having the lowest cell viability. PEI with high molecular weight showed higher transfection efficiency and cell viability than PEI with low molecular weight.

• Korean Journal of Environmental Biology
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• v.37 no.4
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• pp.741-748
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• 2019

As the occurrence of harmful algal blooms (HABs) have become severe in precious water resources, the development of efficient harmful algae treatment methods is considering as an important environmental issue for sustainable conservation of water resources. To treat HABs in water resources, various conventional physical and chemical methods have been utilized and showed treatment efficiency, However, these methods can lead to discharging of cyanotoxins into the water bodies by chemical or physical algal cell lysis or destruction. Thus, to overcome this limitation, the development of safe HABs treatment methods is required. In the present study, adsorption technology was investigated for the removal of harmful algal species, Microcystis aeruginosa from aqueous phases. Industrial waste biomass, Corynebacterium glutamicum biomass was valorized as biosorbent (PEI-modified alginate/biomass composite fiber; PEI-AlgBF) for M. aeruginosa through immobilization with alginate matrix and cationic polymer (polyethylenimine; PEI) coating. The functional groups characteristic of PEI-Alg was determined using FT-IR analysis. By adsorption process used PEI-AlgBF, 52 and 67% of M. aeruginosa could be removed under the initial density of M. aeruginosa 200×10⁴ cells mL^-1 and 50×10⁴ cells mL^-1, respectively. As the increasing surface area of PEI-AlgBF, the removal efficiency was increased. In addition, we could find that adsorptive removal of M. aeruginosa has occurred without any M. aeruginosa cell lysis and destruction.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.425.1-425.1
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• 2002

Nanoparticles of polylactic acid (PLA) and polyethylenimine (PEI) as an effective gene delivery agent were prepared and characterized. As a model plamid DNA. PME185/$\beta$-gal. a mammalian expression vector. and fluorescence enhancing protein (pEGHP) were used. The effects of PEI type on the physical properties of nanoparticles and transfection efficiency were examined. (omitted)