pH sensitive lipids based on ortho ester linkers, composition and method
    2.
    发明授权
    pH sensitive lipids based on ortho ester linkers, composition and method 失效
    基于原酸酯接头的pH敏感性脂质,组成和方法

    公开(公告)号:US06897196B1

    公开(公告)日:2005-05-24

    申请号:US09778388

    申请日:2001-02-07

    IPC分类号: A61K9/127 A61K31/00 A01N43/04

    CPC分类号: A61K9/1272 A61K31/00

    摘要: The invention comprises lipid derivatives that rapidly degrade in the pH range from 4.0 to 7.0 and lipidic delivery systems that contain them. These lipid derivatives can be used to modify the delivery properties of the lipidic delivery systems to enable prolonged circulation times or more rapid drug unloading in the target tissue. The lipid derivatives are amphipathic compounds comprising a hydrophilic head group joined to a hydrophobic group by an acid-labile ortho ester linkage. The delivery systems of the invention exhibit degradation of less than 10% within 3 hours at a pH of 7.4 and degradation greater than 50% within 60 min at a pH of 5.0.

    摘要翻译: 本发明包括在4.0至7.0的pH范围内迅速降解的脂质衍生物和含有它们的脂质递送系统。 这些脂质衍生物可用于改变脂质递送系统的递送性质,以使靶组织中的延长循环时间或更快速的药物卸载。 脂质衍生物是包含通过酸不稳定原酸酯键连接到疏水基团的亲水性头基的两亲性化合物。 本发明的递送系统在pH为7.4时在3小时内显示小于10%的降解,并且在pH5.0的60分钟内降解大于50%。

    Targeted drug delivery with a hyaluronan ligand
    8.
    发明授权
    Targeted drug delivery with a hyaluronan ligand 有权
    用透明质酸配体靶向药物递送

    公开(公告)号:US06593308B2

    公开(公告)日:2003-07-15

    申请号:US09454811

    申请日:1999-12-03

    IPC分类号: A01N4304

    CPC分类号: A61K9/1271 A61K47/6911

    摘要: The invention is a drug delivery system of a delivery vehicle having a low molecular weight hyaluronan ligand with an affinity for CD44 receptors. Preferably, the delivery vehicle is a liposome but other suitable delivery vehicles include microspheres, micelles, emulsions, lipid discs, polymers, viral particles and viruses. The systems of the invention may further comprise a drug, which can be any anticancer agent or other therapeutic or diagnostic agent. The invention also comprises methods of delivering a drug to a cell that expresses CD44 by contacting the cell with the drug delivery system. Further methods include treating a patient with cancer and targeting drug delivery to cells that express CD44 by attaching a glycosaminoglycan ligand.

    摘要翻译: 本发明是具有对CD44受体具有亲和力的低分子量透明质酸配体的递送载体的药物递送系统。 优选地,递送载体是脂质体,但是其它合适的递送载体包括微球,胶束,乳剂,脂质盘,聚合物,病毒颗粒和病毒。 本发明的系统还可以包含药物,其可以是任何抗癌剂或其它治疗或诊断剂。 本发明还包括通过使细胞与药物递送系统接触来将药物递送至表达CD44的细胞的方法。 其他方法包括治疗患有癌症的患者,并通过连接糖胺聚糖配体将药物递送靶向表达CD44的细胞。

    Preparation of liposome and lipid complex compositions
    9.
    发明授权
    Preparation of liposome and lipid complex compositions 失效
    脂质体和脂质复合物组合物的制备

    公开(公告)号:US5567434A

    公开(公告)日:1996-10-22

    申请号:US480227

    申请日:1995-06-07

    摘要: Liposome and lipidic particle formulations of compounds are prepared by dissolving in a solution of liposome-forming lipids in an aprotic solvent such as DMSO, optionally containing a lipid-solubilizing amount of a lower alkanol, and either injecting the resulting solution into an aqueous solution, or the aqueous solution into the resulting solution. The resulting liposome or lipidic particle suspension may then be dialyzed or otherwise concentrated. This method is particularly useful for compounds which are poorly-soluble in aqueous solution, but is generally useful for any compound or combination of compounds which can be dissolved in the aprotic solvent or aprotic solvent/lower alkanol mixture.

    摘要翻译: 通过将脂质体形成脂质溶解在非质子溶剂如DMSO中,任选地含有脂溶性量的低级链烷醇,并将所得溶液注入水溶液中制备化合物的脂质体和脂质颗粒制剂, 或将水溶液加入到所得溶液中。 然后可以将所得的脂质体或脂质颗粒悬浮液透析或以其它方式浓缩。 该方法对于难溶于水溶液的化合物特别有用,但通常可用于可溶于非质子溶剂或非质子溶剂/低级链烷醇混合物中的任何化合物或化合物的组合。