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    Compositions and methods for non-parenteral delivery of oligonucleotides
    1.
    发明申请
    Compositions and methods for non-parenteral delivery of oligonucleotides 有权
    用于非肠胃外递送寡核苷酸的组合物和方法

    公开(公告)号：US20070249551A1

    公开(公告)日：2007-10-25

    申请号：US11237063

    申请日：2005-09-28

    申请人： Ching-Leou Teng ,  Phillip Cook ,  Lloyd Tillman ,  Gregory Hardee ,  David Ecker ,  Muthiah Manoharan

    发明人： Ching-Leou Teng ,  Phillip Cook ,  Lloyd Tillman ,  Gregory Hardee ,  David Ecker ,  Muthiah Manoharan

    IPC分类号： A61K48/00

    CPC分类号： A61K48/0008 ,  A61K9/0014 ,  A61K9/0031 ,  A61K9/107 ,  A61K9/1075 ,  A61K38/00 ,  A61K47/12 ,  A61K47/28 ,  A61K48/00 ,  A61K48/0025 ,  A61K48/0041 ,  C12N15/113 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/322 ,  C12N2310/3521 ,  C12N2310/3527 ,  C12N2310/3525

    摘要： The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes

    摘要翻译： 本发明涉及通过非肠胃外给药途径增强寡核苷酸和核酸的局部和全身摄取和递送的组合物和方法。 包含本文公开的寡核苷酸的药物组合物包括用于全身递送的乳液和微乳液制剂用于各种应用和口服剂型。 还令人惊讶地发现，可以用简单的溶液，例如纯的或盐水，通过直肠灌肠剂和栓剂将寡核苷酸局部递送至结肠部位。 寡核苷酸的这种药物组合物可以进一步包括一种或多种用于将寡核苷酸和其它核酸转移穿过粘膜的渗透增强剂。 本发明的组合物和方法用于对动物进行口服，口腔，直肠或阴道给予反义寡核苷酸，以调节动物中基因的表达用于调查，治疗，姑息或预防目的

    Compositions and methods for non-parenteral delivery of oligonucleotides
    2.
    发明授权
    Compositions and methods for non-parenteral delivery of oligonucleotides 失效
    用于非肠胃外递送寡核苷酸的组合物和方法

    公开(公告)号：US06747014B2

    公开(公告)日：2004-06-08

    申请号：US10029598

    申请日：2001-12-21

    申请人： Ching-Leou Teng ,  Phillip Dan Cook ,  Lloyd Tillman ,  Gregory E. Hardee ,  David J. Ecker ,  Muthiah Manoharan

    发明人： Ching-Leou Teng ,  Phillip Dan Cook ,  Lloyd Tillman ,  Gregory E. Hardee ,  David J. Ecker ,  Muthiah Manoharan

    IPC分类号： A61K3170

    CPC分类号： A61K48/0075 ,  A61K9/0014 ,  A61K9/0019 ,  A61K47/12 ,  A61K47/28 ,  A61K48/00 ,  C07H21/00 ,  Y10S514/946

    摘要： The present invention relates to compositions and methods which enhance the local and systemic uptake and delivery of oligonucleotides and nucleic acids via non-parenteral routes of administration. Pharmaceutical compositions comprising oligonucleotides disclosed herein include, for systemic delivery, emulsion and microemulsion formulations for a variety of applications and oral dosage formulations. It has also surprisingly been discovered that oligonucleotides may be locally delivered to colonic sites by rectal enemas and suppositories in simple solutions, e.g., neat or in saline. Such pharmaceutical compositions of oligonucleotides may further include one or more penetration enhancers for the transport of oligonucleotides and other nucleic acids across mucosal membranes. The compositions and methods of the invention are utilized to effect the oral, buccal, rectal or vaginal administration of an antisense oligonucleotide to an animal in order to modulate the expression of a gene in the animal for investigative, therapeutic, palliative or prophylactic purposes.

    摘要翻译： 本发明涉及通过非肠胃外给药途径增强寡核苷酸和核酸的局部和全身摄取和递送的组合物和方法。 包含本文公开的寡核苷酸的药物组合物包括用于全身递送的乳液和微乳液制剂用于各种应用和口服剂型。 还令人惊讶地发现，可以用简单的溶液，例如纯的或盐水，通过直肠灌肠剂和栓剂将寡核苷酸局部递送至结肠部位。 寡核苷酸的这种药物组合物可以进一步包括一种或多种用于将寡核苷酸和其它核酸转移穿过粘膜的渗透增强剂。 本发明的组合物和方法用于对动物进行口服，口腔，直肠或阴道施用反义寡核苷酸，以调节动物中基因在调查，治疗，姑息或预防目的中的表达。