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Lee, Minji,Lee, Dong Jin,Youn, Yu Seok,Lee, Eun Seong Technomic Pub. Co 2016 Journal of bioactive and compatible polymers Vol.31 No.2
<P>We report extremely small-sized drug-carrying globular poly(ethylene glycol) particles. These particles were prepared using fullerene (C-60) as a backbone structure and poly(ethylene glycol) as a hydrophilic shell. All - carbon bonds in C-60 were combined with poly(ethylene glycol), which form a globular nano-cage with a hollow core (originating from the soccer-ball-shaped truncated icosahedron of C-60) and the poly(ethylene glycol) shell. Subsequently, we constructed chlorin e6-conjugated globular poly(ethylene glycol). The obtained globular poly(ethylene glycol)-chlorin e6 (average 3.6nm in diameter) was soluble in aqueous solution and enabled improved singlet oxygen generation. The preferential cellular uptake of globular poly(ethylene glycol)-chlorin e6 resulted in significant enhancement of in vitro or in vivo photodynamic tumor cell ablation under light illumination. Our approach offers a versatile strategy to create extremely small-sized drug carriers using a biocompatible polymer for various biomedical applications.</P>
Kim, Seong Kyeong,Lee, Jae Min,Oh, Kyung Taek,Lee, Eun Seong Elsevier/North Holland 2017 International journal of pharmaceutics Vol.528 No.1
<P><B>Abstract</B></P> <P>In this study, we report an extremely small-sized globular poly(ethylene glycol) (gPEG) conjugated with cyclic arginine-glycine-aspartic acid (cRGD) peptide and chlorin e6 (Ce6). This nanoparticle design takes advantage of the biocompatible functional gPEG (3–4nm in diameter) as an extremely small-sized drug carrier, the tumor targeting ability of cRGD, and the photodynamic tumor ablation ability of Ce6. We found that gPEG conjugated with cRGD and Ce6 (cRGD-gPEG-Ce6) exhibited much higher phototoxicity in SKOV-3 tumor cells (which have a very high density of integrin α<SUB>v</SUB>β<SUB>3</SUB> receptors) than in KB cells (which have a very low density of integrin α<SUB>v</SUB>β<SUB>3</SUB> receptors). Accordingly, cRGD-gPEG-Ce6 treatment resulted in a significant regression of <I>in vivo</I> SKOV-3 tumors, highlighting the potential of an extremely small-sized drug carrier platform for site-specific receptor-mediated tumor therapy.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Mitochondria-Selective Photodynamic Tumor Therapy Using Globular PEG Nanoparticles
구은비,오경택,윤유석,이은성 한국고분자학회 2016 Macromolecular Research Vol.24 No.7
In this study, we report water-soluble globular poly(ethylene glycol) (gPEG) nanoparticles for targeting mitochondria and for improved photodynamic tumor therapy. Here, gPEG (prepared after all of the π-π carbon bonds in fullerene (as a hollow core structure) were chemically combined with poly(ethylene glycol) (PEG)) was chemically linked with chlorin e6 (Ce6, as a photosensitizing anticancer drug) and iodomethyltriphenylphosphonium (IMTP). In particular, IMTP acted as a mitochondria-targeting molecule, accelerating the localization of nanoparticles into the mitochondria of tumor cells. From an in vitro evaluation, these nanoparticles exhibited improved singlet oxygen generation and significantly increased photodynamic tumor ablation. We believe that this nanoparticle provides a promising pathway for photodynamic drug delivery.
pH-Responsive globular poly(ethylene glycol) for photodynamic tumor therapy
Ku, E.B.,Lee, D.J.,Na, K.,Choi, S.W.,Youn, Y.S.,Bae, S.K.,Oh, K.T.,Lee, E.S. Elsevier 2016 Colloids and Surfaces B Vol.148 No.-
<P>In this study, we report the development of extremely small-sized globular poly(ethylene glycol) (gPEG) that can specifically recognize tumor acidic pH. gPEG coupled with chlorin e6 (Ce6, a photosensitizing drug) and 2,3-dimethylmaleic acid (DMA, as a pH-responsive moiety) (gPEG-Ce6-DMA, particle size: 3-4 nm in diameter) was easily dispersed in phosphate buffered saline (PBS) without any of the nanoparticle fabrication steps. We observed that gPEG-Ce6-DMA displayed pH-dependent zeta-potential changes due to coupling (at pH 7.4) or decoupling (at pH 6.8-6.0) of DMA. As a result, the uptake of gPEG-Ce6-DMA was significantly increased in tumors at acidic pH, likely due to the decoupling of DMA (backing cationic primary amines). As a result, the preferential cellular uptake of gPEG-Ce6-DMA at acidic pH allowed for a significant enhancement of in vitro/in vivo photodynamic tumor cell ablation under light illumination. (C) 2016 Elsevier B.V. All rights reserved.</P>