University of Kentucky, College of Pharmacy, Division of Pharmaceutical Sciences-Drug Development Division, Lexington, KY 40536, USA.
Int J Nanomedicine. 2009;4:299-319. doi: 10.2147/ijn.s4937. Epub 2009 Dec 29.
The lung is an attractive target for drug delivery due to noninvasive administration via inhalation aerosols, avoidance of first-pass metabolism, direct delivery to the site of action for the treatment of respiratory diseases, and the availability of a huge surface area for local drug action and systemic absorption of drug. Colloidal carriers (ie, nanocarrier systems) in pulmonary drug delivery offer many advantages such as the potential to achieve relatively uniform distribution of drug dose among the alveoli, achievement of improved solubility of the drug from its own aqueous solubility, a sustained drug release which consequently reduces dosing frequency, improves patient compliance, decreases incidence of side effects, and the potential of drug internalization by cells. This review focuses on the current status and explores the potential of colloidal carriers (ie, nanocarrier systems) in pulmonary drug delivery with special attention to their pharmaceutical aspects. Manufacturing processes, in vitro/in vivo evaluation methods, and regulatory/toxicity issues of nanomedicines in pulmonary delivery are also discussed.
由于可通过吸入式气溶胶进行非侵入性给药、避免首过代谢、可直接将药物递送至作用部位以治疗呼吸疾病，以及拥有巨大的表面积可供局部药物作用和全身吸收药物，肺部成为药物输送的一个有吸引力的靶标。肺部药物输送中的胶体载体（即纳米载体系统）具有诸多优势，例如有潜力在肺泡中实现药物剂量的相对均匀分布、提高药物自身水溶解度的溶解度、实现药物的持续释放，从而减少给药频率、提高患者顺应性、降低副作用发生率，以及具有使药物被细胞内化的潜力。本综述重点介绍了当前的现状，并探讨了胶体载体（即纳米载体系统）在肺部药物输送中的潜力，特别关注了其在药剂学方面的应用。还讨论了肺部输送中纳米药物的制造工艺、体外/体内评估方法以及监管/毒性问题。
