Weers Jeffry G, Tarara Thomas E, Clark Andrew R
Nektar Therapeutics, 150 Industrial Road, San Carlos, CA 94070, USA.
Expert Opin Drug Deliv. 2007 May;4(3):297-313. doi: 10.1517/17425247.4.3.297.
Particle design for inhalation is characterized by advances in particle processing methods and the utilization of new excipients. Processing methods such as spray drying allow control over critical particle design features, such as particle size and distribution, surface energy, surface rugosity, particle density, surface area, porosity and microviscosity. Control of these features has enabled new classes of therapeutics to be delivered by inhalation. These include therapeutics that have a narrow therapeutic index, require a high delivered dose, and/or elicit their action systemically. Engineered particles are also being utilized for immune modulation, with exciting advances being made in the delivery of antibodies and inhaled vaccines. Continued advances are expected to result in 'smart' therapeutics capable of active targeting and intracellular trafficking.
吸入用颗粒设计的特点是颗粒加工方法的进步以及新型辅料的应用。喷雾干燥等加工方法能够控制关键的颗粒设计特性,如粒径和分布、表面能、表面粗糙度、颗粒密度、表面积、孔隙率和微粘度。对这些特性的控制使得新型治疗药物能够通过吸入给药。这些药物包括治疗指数窄、需要高给药剂量和/或全身起效的药物。工程颗粒也被用于免疫调节,在抗体和吸入疫苗的递送方面取得了令人兴奋的进展。预计持续的进步将产生能够实现主动靶向和细胞内运输的“智能”疗法。