Method of drug loading in liposomes by gradient
    3.
    发明申请
    Method of drug loading in liposomes by gradient 审中-公开
    通过梯度在脂质体中加载药物的方法

    公开(公告)号:US20100119590A1

    公开(公告)日:2010-05-13

    申请号:US12501606

    申请日:2009-07-13

    IPC分类号: A61K9/127 A61K31/55 A61P35/00

    摘要: A method for encapsulation of pharmaceutical agents (e.g., antineoplastic agents) in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes can be made by a process that loads the drug by an active mechanism using a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%. Drug:lipid ratios employed are higher than for older traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. After loading, residual acid is quenched with a quenching agent that is base permeable at low temperatures. The residual aciditiy is thus reduced and chemical stability (e.g. against hydrolysis) is enhanced. The stability of both the liposome and the pharmaceutical agent is thus maintained, prior to administration. The pH gradient is, however, present when the liposome is administered in vivo because the quenching agent rapidly exits the liposome.

    摘要翻译: 提供了在脂质体中封装药物(例如抗肿瘤剂)的方法,其优选具有高的药物:脂质比。 可以通过使用跨膜pH梯度的活性机制加载药物的方法制备脂质体。 使用这种技术,捕获效率接近100%。 药物:使用的脂质比例高于较老的传统脂质体制剂,并且药物从脂质体的释放速率降低。 加载后,残留的酸用低温基本可渗透的淬火剂骤冷。 残留的酸性因此降低,并且化学稳定性(例如抗水解)得到增强。 因此在施用之前维持脂质体和药剂的稳定性。 然而,当脂质体在体内施用时,pH梯度存在,因为猝灭剂快速离开脂质体。

    LIPID-BASED DISPERSIONS USEFUL FOR DRUG DELIVERY
    4.
    发明申请
    LIPID-BASED DISPERSIONS USEFUL FOR DRUG DELIVERY 审中-公开
    用于药物递送的基于脂质的分散剂

    公开(公告)号:US20090060998A1

    公开(公告)日:2009-03-05

    申请号:US10585915

    申请日:2005-01-14

    IPC分类号: A61K9/10

    CPC分类号: A61K9/127 A61K9/0019

    摘要: The invention provides lipid-based dispersion comprising, a) phosphatidyl choline; b) an anionic phospholipid; optionally c) up to 1% cholesterol by weight of total lipids; and optionally d) a therapeutic agent; wherein the mean particle size measured by dynamic light scattering is less than 100 nm. The invention also provides pharmaceutical compositions comprising such a dispersion as well as methods of producing a therapeutic effect in a mammal comprising administering an effective amount of such a dispersion.

    摘要翻译: 本发明提供了脂质基分散体,其包含:a)磷脂酰胆碱; b)阴离子磷脂; 任选地c)总脂质重量高达1%的胆固醇; 和任选地d)治疗剂; 其中通过动态光散射测量的平均粒度小于100nm。 本发明还提供包含这种分散体的药物组合物以及在哺乳动物中产生治疗效果的方法,包括施用有效量的这种分散体。