• Macromolecular Research
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• v.12 no.3
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• pp.276-281
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• 2004

In this study we investigated the spectral properties, including electric absorption, circular and linear dichroism (CD and LD), and fluorescence emission, of DNA in a DNA-branched polyethyleneimine (BPEI) polyplex at various polymer molecular weights (M$\_$w/) and BPEI-amine-to-DNA-phosphate ratios (N/P ratios). All BPEIs exhibited a common N/P dependence in their absorption and CD spectra. At N/P ratios ＜ 1.0, we observed some hyperchromism in the absorption spectrum, red-shifts in CD bands, and decreases in LD intensity and fluorescence intensity of intercalated ethidium. At intermediate N/P ratios, complete collapse of all spectra occurred. As the N/P ratio increased further, the polyplex dissolved in water. From its characteristic CD spectrum obtained under these conditions, we conclude that the DNA exists in a B-like form. The fluorescence and LD intensities never recovered even at high N/P ratios- which indicates that the dissolved polyplex possesses positive charges and the DNA in the polyplex is condensed despite its B-form CD spectrum. The N/P range in which the absorption and CD signals collapsed was wider when the BPEIs M$\_$w/ decreased. In the case where the BPEIs M$\_$w/ was 0.8 k, recovery of the absorption and CD spectral properties at a high N/P ratio was never achieved, which suggests that the molecular weight of the polymer plays an important role in its dissolution at a high N/P ratio.

• Journal of the Korean Chemical Society
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• v.62 no.1
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• pp.24-29
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• 2018

Despite the great potential for the versatile applications in food industry and medical area, chitosan as a biocompatible cationic polysaccharide has suffered from the limited solubility under physiological condition. Herein, we demonstrated the electrostatic formation of chitosan-based polyplex particles, counterbalanced by polyacrylate as an anionic polyelectrolyte. The resulting polyplex exhibited pH- and composition-dependent changes in their surface charges as measured by zeta potential, which can be employed to provide the interparticle repulsive forces for enhanced colloidal stability in homogeneous solution. Subsequently, amide coupling between the acrylates and glucosamine residues of chitosan inside the polyplex further generated the hydrogel particles, which showed the temperature-sensitive swelling property. This aspect can be attributed to the partial formation of acryl amide residues, which have been generally known to possess the lower critical solution temperature (LCST).

• Applied Chemistry for Engineering
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• v.33 no.1
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• pp.83-89
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• 2022

Since the pandemic of COVID-19, active investigation to develop immunity to infectious disease by delivering nucleic acids has been proceeded. Particularly, many studies have been conducted on non-viral vector as several vital side-effects which were found on nucleic acid delivery system using viral vectors. In this study, we have developed plasmid DNA (pDNA) loaded-hyaluronic acid derivative (HA) coated-polyethyleneimine (PEI) based polyplex for enhanced nucleic acid delivery efficiency. We have optimized the ratio of pDNA : PEI : HA by measuring size and protein transcription efficiency. The final product, polyplex-HA, was characterized through measuring size, zeta-potential and TEM image. Intracellular uptake and protein transcription efficiency were compared to commercially available transfection reagent, lipofectamine, through fluorescence image and flow cytometry. In conclusion, polyplex-HA presents a novel gene delivery system for efficient and stable protein transcription since it is available for delivering various genetic materials and has less immunoreactivity.

• Bulletin of the Korean Chemical Society
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• v.28 no.8
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• pp.1317-1321
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• 2007

Arginine conjugated PAMAM dendrimer, PAMAM-R was modified with propylene oxide via hydroxylation of primary amines of arginine residues. About 49 amines were detected to be converted to amino alcohols by 1H NMR. The newly synthesized polymer, PAMAM-R-PO was able to completely retard pDNA from a charge ratio of 2. The average diameter of PAMAM-R-PO polyplex was found to be 242 nm at a charge ratio of 30. The Zeta-potential value of PAMAM-R-PO polyplex was able to reach 20-30 mV over a charge ratio of 10. PAMAM-R-PO indicated higher cell viability than unmodified PAMAM-R on HeLa and 293 cells because of its hydroxylated amines. Transfection experiments on 293 cells showed that the transfection efficiency of PAMAM-R-PO was found to be 1.5-1.9 times higher than that of PEI25kDa at a charge ratio of 30. The polymer eventually displayed about 2 times greater transfection efficiency than PAMAM-R at the same charge ratio in the absence of serum. Therefore, we concluded that the modification of primary amines of PAMAMR to amino alcohols gives positive effects such as reduced cytotoxicity and enhanced transfection efficiency on 293 cells for gene delivery potency of PAMAM-R.

• Macromolecular Research
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• v.12 no.5
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• pp.501-506
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• 2004

We have investigated the spectral properties of DNA, including its electric absorption, circular and linear dichroism (CD and LD), and fluorescence emission, in the DNA-linear polyethyleneimine (LPEI) and DNA-branched polyethyleneimine (BPEI) complexes at various polymer concentrations. The spectral properties of both complexes are similar. We observed a relatively moderate change in the absorption and CD spectra at low amine/DNA phosphate (NIP) ratios (< 0.5), followed by a drastic collapse within the N/P range from 0.8 and 1.0. The absorption and CD spectra recovered as the N/P ratio increased to ca. 1.2. In contrast, the LD and emission of ethidium intercalated between the DNA bases decreased almost linearly at N/P ratios between 0.0 and 1.0. These spectra never recovered at higher N/P ratios. We believe that the moderate changes in the spectrum at low N/P ratios occurred because of electrostatic interactions between DNA and BPEI, while the collapsed spectra at N/P ratios between 0.5 and 1.5 occurred because of condensation/aggregation of the DNA. Considering the structure of the polymers, we suggest that the secondary amino group of LPEI and all three amino groups of BPEI are equally involved in DNA condensation.

• Bulletin of the Korean Chemical Society
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• v.24 no.1
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• pp.123-125
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• 2003

• Bulletin of the Korean Chemical Society
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• v.33 no.11
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• pp.3849-3852
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• 2012

• Bulletin of the Korean Chemical Society
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• v.32 no.2
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• pp.651-655
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• 2011

We synthesized a novel cationic dendrimer consisting of a poly(amidoamine) dendrimer (PAMAM, generation 4) backbone with both L-arginine (Arg) at the termini and 6-aminohexanoic acid (Ahx) between the original core polymer and the peripheral Arg units. The sequential chemical modification of PAMAM G4 with Ahx and Arg resulted in higher transfection efficiency with much less cytotoxicity. PAMAM G4-Ahx-Arg formed stable polyplexes at weight ratios of 8:1 or higher (polymer: plasmid DNA), and the mean polyplex diameter was $180{\pm}20nm$. PAMAM G4-Ahx-Arg showed much higher transfection ability than PAMAM G4 or PAMAM G4-Ahx. Furthermore, PAMAM G4-Ahx-Arg was much less cytotoxic than PEI25KD and PAMAM G4-Arg. In addition to Arg grafting of the PAMAM dendrimer, which endows a higher transfection capability, the addition of Ahx spacer increased dendrimer hydrophobicity, introduced flexibility into the conjugated amino acids, and reduced cytotoxicity. Overall, it appears that the concomitant modification of PAMAM with Ahx and Arg could lead to new PAMAM conjugates with better performances.

• Bulletin of the Korean Chemical Society
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• v.25 no.7
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• pp.1025-1030
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• 2004

A hybrid linear polymer-dendrimer block copolymer, poly(ethylene glycol)-block-poly(L-lysine) dendrimer, was synthesized and introduced to form polyionic complexes with DNA. The copolymer formed core-shell type nanoparticles with plasmid DNA. From dynamic light scattering experiments, the mean diameter of the polyplexes was observed to be 154.4 nm. The complex showed much increased water solubility compared to poly(L-lysine). The plasmid DNA in polyplexes was efficiently protected from the enzymatic digestion of DNase I. The cytotoxicity and transfection efficiency for 293 cells was measured in comparison with poly(Llysine).

• Journal of Pharmaceutical Investigation
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• v.40 no.spc
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• pp.45-61
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• 2010

Polymeric based nanomedicines have been developed for diagnosing, treating, and preventing diseases in human body. The nanosized drug delivery systems having various structures such as micelles, nanogels, drug-conjugates, and polyplex were investigated for a great goal in pharmaceutics: increasing therapeutic efficacy for diseases and decreasing drug toxicity for normal tissues. The functional polymers used for constituting these drug delivery systems should have several favorable properties such as stimuli-responsibility and biodegrdability for controlled drug release, and solublization capacity for programmed drug encapsulation. This review discusses recent developments and trends of functional polymers (e.g., pH-sensitive polymers, biodegradable polymers, and cationic polymers) used for nanosized drug carriers.