Article: Folic acid conjugated mPEG-PEI600 as an efficient non-viral vector for targeted nucleic acid delivery
| Title | Folic acid conjugated mPEG-PEI600 as an efficient non-viral vector for targeted nucleic acid delivery |
|---|---|
| Authors | Xu, Z1 2 Jin, J1 Siu, LKS1 Yao, H2 Sze, J2 Sun, H1 Kung, HF2 Poon, WS2 Ng, SSM1 Lin, MC1 2 |
| Keywords | PEG Polyethylenimine Polymer Tumor gene delivery |
| Issue Date | 2012 |
| Publisher | Elsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ijpharm |
| Citation | International Journal Of Pharmaceutics, 2012, v. 426 n. 1-2, p. 182-192 [How to Cite?] DOI: http://dx.doi.org/10.1016/j.ijpharm.2012.01.009 |
| Abstract | In this study we describe a novel polymer, mPPS-FA, synthesized as a potential gene transfer vector. To complete mPPS-FA, folic acid was conjugated to a backbone (named mPPS) consisting of a copolymer of methyl PEG-2000, PEI-600, and sebacoyl chloride. 1H NMR, FT-IR, and UV spectroscopy were used to characterize the structure of mPPS-FA. It was revealed that mPPS-FA holds the ability to bind plasmid DNA yielding positively charged particles (polyplexes). Dynamic light scattering (DLS) and TEM techniques were used to study the size and morphology of the formed mPPS-FA/DNA nanocomplexes. The mPPS-FA/DNA nanoparticles exhibited low cytotoxicity as transfection of B16-F0, U87MG, CHO-1, and Ho-8910 cells produced >80% viability indicating low cytotoxicity of the polymer. The ability of mPPS-FA to deliver EGFP plasmid to melanoma B16-F0, U87, CHO-1, Ho-8910, and A549 cells was investigated in vitro as compared to the lipid-based transfection agent Lipofectamine™2000 and Linear PEI 22kDa (L-PEI 22kDa). We found that mPPS-FA/DNA complexes yielded the highest GFP transfection efficiency in B16-F0, U87, CHO-1, and Ho-8910 cells, which all highly express folate receptors (FR), at an mPPS-FA/DNA ratio (w/w) of 15. Furthermore, the transfection of mPPS-FA/DNA complexes in CHO-1 cells could be competitively blocked by free folic acid molecules. In contrast, in low FR expressing A549 cells, mPPS-FA showed similar low transfection efficiency as mPPS. Taken together, mPPS-FA showed the highest efficiency in vitro and the potential to be developed as a nonviral gene carrier. © 2012 Elsevier B.V. All rights reserved. |
| ISSN | 0378-5173 2011 Impact Factor: 3.35 2011 SCImago Journal Rankings: 0.217 |
| DOI | http://dx.doi.org/10.1016/j.ijpharm.2012.01.009 |
| ISI Accession Number ID | WOS:000302364300021 |
| References | References in Scopus |
| dc.contributor.author | Xu, Z |
|---|---|
| dc.contributor.author | Jin, J |
| dc.contributor.author | Siu, LKS |
| dc.contributor.author | Yao, H |
| dc.contributor.author | Sze, J |
| dc.contributor.author | Sun, H |
| dc.contributor.author | Kung, HF |
| dc.contributor.author | Poon, WS |
| dc.contributor.author | Ng, SSM |
| dc.contributor.author | Lin, MC |
| dc.date.accessioned | 2012-08-16T05:48:59Z |
| dc.date.available | 2012-08-16T05:48:59Z |
| dc.date.issued | 2012 |
| dc.description.abstract | In this study we describe a novel polymer, mPPS-FA, synthesized as a potential gene transfer vector. To complete mPPS-FA, folic acid was conjugated to a backbone (named mPPS) consisting of a copolymer of methyl PEG-2000, PEI-600, and sebacoyl chloride. 1H NMR, FT-IR, and UV spectroscopy were used to characterize the structure of mPPS-FA. It was revealed that mPPS-FA holds the ability to bind plasmid DNA yielding positively charged particles (polyplexes). Dynamic light scattering (DLS) and TEM techniques were used to study the size and morphology of the formed mPPS-FA/DNA nanocomplexes. The mPPS-FA/DNA nanoparticles exhibited low cytotoxicity as transfection of B16-F0, U87MG, CHO-1, and Ho-8910 cells produced >80% viability indicating low cytotoxicity of the polymer. The ability of mPPS-FA to deliver EGFP plasmid to melanoma B16-F0, U87, CHO-1, Ho-8910, and A549 cells was investigated in vitro as compared to the lipid-based transfection agent Lipofectamine™2000 and Linear PEI 22kDa (L-PEI 22kDa). We found that mPPS-FA/DNA complexes yielded the highest GFP transfection efficiency in B16-F0, U87, CHO-1, and Ho-8910 cells, which all highly express folate receptors (FR), at an mPPS-FA/DNA ratio (w/w) of 15. Furthermore, the transfection of mPPS-FA/DNA complexes in CHO-1 cells could be competitively blocked by free folic acid molecules. In contrast, in low FR expressing A549 cells, mPPS-FA showed similar low transfection efficiency as mPPS. Taken together, mPPS-FA showed the highest efficiency in vitro and the potential to be developed as a nonviral gene carrier. © 2012 Elsevier B.V. All rights reserved. |
| dc.description.nature | Link_to_subscribed_fulltext |
| dc.identifier.citation | International Journal Of Pharmaceutics, 2012, v. 426 n. 1-2, p. 182-192 [How to Cite?] DOI: http://dx.doi.org/10.1016/j.ijpharm.2012.01.009 |
| dc.identifier.citeulike | 10280072 |
| dc.identifier.doi | http://dx.doi.org/10.1016/j.ijpharm.2012.01.009 |
| dc.identifier.epage | 192 |
| dc.identifier.hkuros | 205092 |
| dc.identifier.isi | WOS:000302364300021 |
| dc.identifier.issn | 0378-5173 2011 Impact Factor: 3.35 2011 SCImago Journal Rankings: 0.217 |
| dc.identifier.issue | 1-2 |
| dc.identifier.openurl | ![]() |
| dc.identifier.pmid | 22265912 |
| dc.identifier.scopus | eid_2-s2.0-84862832308 |
| dc.identifier.spage | 182 |
| dc.identifier.uri | http://hdl.handle.net/10722/159383 |
| dc.identifier.volume | 426 |
| dc.language | eng |
| dc.publisher | Elsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ijpharm |
| dc.publisher.place | Netherlands |
| dc.relation.ispartof | International Journal of Pharmaceutics |
| dc.relation.references | References in Scopus |
| dc.rights | NOTICE: this is the author’s version of a work that was accepted for publication in |
| dc.subject.mesh | Alkanes - chemistry - toxicity |
| dc.subject.mesh | Animals |
| dc.subject.mesh | Binding, Competitive |
| dc.subject.mesh | CHO Cells |
| dc.subject.mesh | Cell Survival - drug effects |
| dc.subject.mesh | Cricetinae |
| dc.subject.mesh | Cricetulus |
| dc.subject.mesh | DNA - chemistry - metabolism |
| dc.subject.mesh | Folic Acid - chemistry - metabolism - toxicity |
| dc.subject.mesh | Green Fluorescent Proteins - biosynthesis - genetics |
| dc.subject.mesh | Humans |
| dc.subject.mesh | Imines - chemistry - toxicity |
| dc.subject.mesh | Light |
| dc.subject.mesh | Magnetic Resonance Spectroscopy |
| dc.subject.mesh | Methylation |
| dc.subject.mesh | Mice |
| dc.subject.mesh | Microscopy, Electron, Transmission |
| dc.subject.mesh | Nanoparticles |
| dc.subject.mesh | Nanotechnology |
| dc.subject.mesh | Particle Size |
| dc.subject.mesh | Polyethylene Glycols - chemistry - toxicity |
| dc.subject.mesh | Polyethylenes - chemistry - toxicity |
| dc.subject.mesh | Scattering, Radiation |
| dc.subject.mesh | Spectrophotometry, Ultraviolet |
| dc.subject.mesh | Spectroscopy, Fourier Transform Infrared |
| dc.subject.mesh | Transfection - methods |
| dc.subject | PEG |
| dc.subject | Polyethylenimine |
| dc.subject | Polymer |
| dc.subject | Tumor gene delivery |
| dc.title | Folic acid conjugated mPEG-PEI600 as an efficient non-viral vector for targeted nucleic acid delivery |
| dc.type | Article |
Author Affiliations
- The University of Hong Kong
- Chinese University of Hong Kong


