Alipour Shohreh, Montaseri Hashem, Tafaghodi Mohsen
a Department of Pharmaceutics, School of Pharmacy , Shiraz University of Medical Sciences , Shiraz , Iran .
b Nanotechnology Research Center and.
J Microencapsul. 2015;32(7):661-8. doi: 10.3109/02652048.2014.944949. Epub 2015 Sep 29.
Large porous particles (LPPs) could be used as a useful carrier for non-invasive delivery to the deep lung. Pulmonary delivery of paclitaxel-loaded LPPs (PTX-LPPs) can help to eliminate the highly complicated and harmful solvent used in PTX parenteral formulations. PTX-LPPs with mass median aerodynamic diameter (MMAD) of 5.74 ± 0.09 μm, high encapsulation efficiency and good aerosolisation properties were produced using ammonium bicarbonate as porogen. Cytotoxicity of PTX-LPPs on A549 and Calu-6 cell lines was comparable with Free-PTX. Endotracheal administration of PTX-LPPs in rats exhibited PTX plasma concentration in the therapeutic range which lasted 4-fold longer than i.v. injection. The bioavailability was measured as 51 ± 7.1%. The lung targeting efficiency (Te) of PTX-LPPs was 11.9-fold higher than i.v. administration. PTX-LPPs could deliver a higher PTX to lung with a non-toxic plasma level in a longer duration which shows their pulmonary delivery suitability.
大孔颗粒（LPPs）可作为一种有用的载体，用于非侵入性地递送至肺深部。负载紫杉醇的LPPs（PTX-LPPs）的肺部给药有助于消除PTX肠胃外制剂中使用的高度复杂且有害的溶剂。使用碳酸氢铵作为致孔剂制备了质量中值空气动力学直径（MMAD）为5.74±0.09μm、高包封率和良好雾化性能的PTX-LPPs。PTX-LPPs对A549和Calu-6细胞系的细胞毒性与游离紫杉醇相当。大鼠气管内给予PTX-LPPs后，PTX血浆浓度处于治疗范围内，持续时间比静脉注射长4倍。测得生物利用度为51±7.1%。PTX-LPPs的肺靶向效率（Te）比静脉给药高11.9倍。PTX-LPPs可以在更长的时间内以无毒的血浆水平将更高剂量的PTX递送至肺部，这表明它们适用于肺部给药。
