Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbrücken, Germany.
Inhal Toxicol. 2009 Jul;21 Suppl 1:137-43. doi: 10.1080/08958370902962283.
Inhalation therapy is still limited by the low bioavailability of the administered drugs. Advantages of the pulmonary administration site like large resorption area, low enzymatic equipment, and circumvention of the first pass effect are set into perspective by the rigid barrier properties of the alveolar region. As a consequence, the systemic bioavailability of peptides and proteins is still relatively limited, even when administered by modern pharmaceutical aerosol technologies. In the context of advanced pulmonary drug therapy the use of nanoparticles as alternative to micronsized drug formulation could be of special interest, because nanoparticles seem to overcome some cellular barriers quite efficiently. Besides such outstanding permeation properties, nanoparticles may also hold promises to escape from pulmonary clearance mechanisms and to allow for cell-specific targeting within the lung. Such opportunities and challenges of inhalative nanomedicine are reviewed in this short review.
吸入疗法仍然受到所给予药物生物利用度低的限制。肺部给药部位具有较大的吸收面积、低酶设备和避免首过效应等优势,但肺泡区域的刚性屏障特性限制了其应用。因此,即使采用现代制药气溶胶技术,多肽和蛋白质的全身生物利用度仍然相对有限。在先进的肺部药物治疗中,使用纳米颗粒作为微米药物制剂的替代物可能具有特殊的意义,因为纳米颗粒似乎能够有效地克服一些细胞屏障。除了这些突出的渗透特性外,纳米颗粒还可能有希望逃避肺部清除机制,并允许在肺部进行细胞特异性靶向。本文综述了吸入纳米医学的这些机遇和挑战。