Large porous particles for pulmonary drug delivery
Large porous particles for pulmonary drug delivery
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DOI：
10.1126/science.276.5320.1868
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发表时间：
1997-06-20
期刊：
影响因子：
56.9
通讯作者：
Langer, R
中科院分区：
文献类型：
--
作者：
Edwards, DA;Hanes, J;Langer, R
一种新型吸入气雾剂，其特点是颗粒质量密度小、尺寸大，可以将吸入治疗药物高效地输送到体循环中。质量密度小于 0.4 克每立方厘米且平均直径超过 5 微米的颗粒被吸入肺部深处并逃脱肺部的自然清除机制，直到吸入的颗粒释放出治疗有效载荷。吸入大的多孔胰岛素颗粒会导致全身胰岛素水平升高，并在 96 小时内抑制全身血糖水平，而小的无孔胰岛素颗粒的这种作用仅持续 4 小时。通过吸入平均直径（20微米）约为传统吸入治疗颗粒10倍的多孔颗粒，也实现了睾酮的高全身生物利用度。
A new type of inhalation aerosol, characterized by particles of small mass density and large size, permitted the highly efficient delivery of inhaled therapeutics into the systemic circulation. Particles with mass densities less than 0.4 gram per cubic centimeter and mean diameters exceeding 5 micrometers were inspired deep into the lungs and escaped the lungs' natural clearance mechanisms until the inhaled particles delivered their therapeutic payload. Inhalation of large porous insulin particles resulted in elevated systemic levels of insulin and suppressed systemic glucose levels for 96 hours, whereas small nonporous insulin particles had this effect for only 4 hours. High systemic bioavailability of testosterone was also achieved by inhalation delivery of porous particles with a mean diameter (20 micrometers) approximately 10 times that of conventional inhaled therapeutic particles.