公开(公告)号：WO2011006011A2

公开(公告)日：2011-01-13

申请号：PCT/US2010/041432

申请日：2010-07-08

Applicant: VIRGINIA TECH INTELLECTUAL PROPERTIES INC. ,  REINEKE, Theresa ,  BRYSON, Joshua

Inventor： REINEKE, Theresa ,  BRYSON, Joshua

IPC: C08G69/44 ,  C08G73/16 ,  C12Q1/68 ,  G01N33/68 ,  G01N24/08

CPC classification number: C12N15/87 ,  A61K49/0019 ,  A61K49/0054 ,  A61K49/12 ,  C07C237/10 ,  C08G69/26 ,  C12Q1/6816 ,  Y02A50/52 ,  Y02A50/55 ,  Y02A50/58 ,  C12Q2525/301 ,  C12Q2565/601

Abstract: The present invention relates to vehicles for delivering macromolecules into cells. More particularly, embodiments of the invention relate to compounds and methods for binding and compacting nucleic acids into nanoparticles for transferring the polynucleotides into cells and which can be configured to provide a mechanism for visualization of the delivery vehicles on the nm/μm scale by microscopy and on the sub-mm scale by magnetic resonance imaging. Polycations according to embodiments of the invention have been designed to contain repeated oligoethyleneamines, for binding and compacting nucleic acids into nanoparticles, and lanthanide (Ln) chelates (for example, using luminescent europium Eu 3+ and paramagnetic gadolinium Gd 3+ ). Especially preferred, are structures chelated with either Eu3+ or Gd3+ for microscopy or MRI imaging, respectively. Such chelated lanthanides allow the visualization of the delivery vehicle both on the nm/μm scale by way of microscopy and on the sub-mm scale using MRI.

Abstract translation: 本发明涉及用于将大分子递送到细胞中的载体。 更具体地，本发明的实施方案涉及用于将核酸结合并压实成纳米颗粒的化合物和方法，用于将多核苷酸转移到细胞中，并且其可以被配置为提供通过显微镜在nm /μm标度上可视化递送载体的机制， 通过磁共振成像在sub-mm尺度上。 根据本发明实施方案的聚阳离子被设计成含有重复的低聚亚乙基胺，用于将核酸结合并压实成纳米颗粒，和镧系元素（Ln）螯合物（例如使用发光铕Eu3 +和顺磁钆Gd3 +）。 特别优选的是分别与Eu3 +或Gd3 +螯合的结构用于显微镜或MRI成像。 这种螯合的镧系元素允许通过显微镜和使用MRI在sub-mm尺度上以nm /μm标度显示递送载体。

公开(公告)号：WO2011006011A3

公开(公告)日：2011-04-28

申请号：PCT/US2010041432

申请日：2010-07-08

Applicant: VIRGINIA TECH INTELL PROP ,  REINEKE THERESA ,  BRYSON JOSHUA

Inventor： REINEKE THERESA ,  BRYSON JOSHUA

IPC: C08G69/44 ,  C08G73/16 ,  C12Q1/68 ,  G01N24/08 ,  G01N33/68

CPC classification number: C12N15/87 ,  A61K49/0019 ,  A61K49/0054 ,  A61K49/12 ,  C07C237/10 ,  C08G69/26 ,  C12Q1/6816 ,  C12Q2525/301 ,  C12Q2565/601

Abstract: The present invention relates to vehicles for delivering macromolecules into cells. More particularly, embodiments of the invention relate to compounds and methods for binding and compacting nucleic acids into nanoparticles for transferring the polynucleotides into cells and which can be configured to provide a mechanism for visualization of the delivery vehicles on the nm/µm scale by microscopy and on the sub-mm scale by magnetic resonance imaging. Polycations according to embodiments of the invention have been designed to contain repeated oligoethyleneamines, for binding and compacting nucleic acids into nanoparticles, and lanthanide (Ln) chelates (for example, using luminescent europium Eu3+ and paramagnetic gadolinium Gd3+). Especially preferred, are structures chelated with either Eu3+ or Gd3+ for microscopy or MRI imaging, respectively. Such chelated lanthanides allow the visualization of the delivery vehicle both on the nm/µm scale by way of microscopy and on the sub-mm scale using MRI.

Abstract translation: 本发明涉及用于将大分子递送到细胞中的载体。 更具体地说，本发明的实施方案涉及用于将核酸结合和压缩成纳米颗粒以将多核苷酸转移入细胞中的化合物和方法，并且其可以被配置成通过显微镜提供用于以nm /μm尺度显示递送载体的机制，和 通过磁共振成像在亚毫米级。 根据本发明的实施方案的聚阳离子已被设计成含有重复的寡聚乙烯胺，用于将核酸结合和压缩成纳米颗粒，以及镧系元素（Ln）螯合物（例如，使用发光铕Eu3 +和顺磁性钆Gd3 +）。 特别优选的是分别与Eu3 +或Gd3 +螯合的用于显微镜或MRI成像的结构。 这种螯合的镧系元素允许通过显微镜以nm /μm尺度显示递送载体并且使用MRI以亚毫米尺度显示递送载体。