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    • 9. 发明授权
    • Aerodynamically light particles for pulmonary drug delivery
    • 用于肺部药物递送的空气动力学轻微颗粒
    • US06977087B2
    • 2005-12-20
    • US10090418
    • 2002-03-01
    • David A. EdwardsGiovannia CaponettiJeffrey S. HrkachNoah LotanJustin HanesAbdell Aziz Ben-JebriaRobert S. Langer
    • David A. EdwardsGiovannia CaponettiJeffrey S. HrkachNoah LotanJustin HanesAbdell Aziz Ben-JebriaRobert S. Langer
    • A61K9/00A61K9/14A61K9/16A61K31/56A61K31/568A61K38/28
    • A61K9/0075A61K9/1647A61K31/56A61K31/568A61K38/28
    • Improved aerodynamically light particles for delivery to the pulmonary system, and methods for their preparation and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of a biodegradable material and have a tap density less than 0.4 g/cm3 and a mass mean diameter between 5 μm and 30 μm. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear α-hydroxy-acid polyester backbone having at least one amino acid group incorporated herein and at least on poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 μm, can be used for enhanced delivery of a therapeutic or diagnostic agent to the alveolar region of the lung. The aerodynamically light particles optionally can incorporate a therapeutic or diagnostic agent, and may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of a wide variety of incorporated agents.
    • 提供用于递送至肺系统的改善的空气动力学轻微颗粒,以及其制备和给药方法。 在优选的实施方案中,空气动力学轻微颗粒由可生物降解的材料制成,并且振实密度小于0.4g / cm 3,质量平均直径在5μm和30μm之间。 颗粒可以由可生物降解的材料如可生物降解的聚合物形成。 例如,颗粒可以由官能化的聚酯接枝共聚物形成,所述官能化聚酯接枝共聚物由具有至少一个引入本文的氨基酸基团和至少在从氨基酸延伸的聚(氨基酸)侧链上的直链α-羟基酸聚酯主链组成 集团在聚酯骨干。 在一个实施方案中,具有大平均直径(例如大于5μm)的空气动力学轻的颗粒可用于增强治疗或诊断剂递送至肺的肺泡区域。 空气动力学轻微颗粒任选地可以掺入治疗剂或诊断剂,并且可以有效地雾化用于给予呼吸道以允许各种并入药剂的全身或局部递送。