GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, Singapore, Singapore.
Engineering Technology Research Center for Processing and Preparation of Traditional Chinese Medicine and Ethnic Medicine, National Engineering Technology Research Center for Miao Medicine, College of Pharmaceutical Sciences, Guizhou University of Traditional Chinese Medicine, Guiyang, China.
Pharm Dev Technol. 2023 Feb;28(2):164-175. doi: 10.1080/10837450.2023.2171434. Epub 2023 Jan 26.
Surface roughness of carrier particles can impact dry powder inhaler (DPI) performance. There are opposing views on the effect of roughness on DPI performance. Hence, a systematic approach is needed to modify carrier surfaces and evaluate the impact on drug delivery. Carrier particle surfaces were modified by fluid bed coating with saturated lactose containing micronized lactose of different sizes (2, 5 and 8 μm) and coated to different levels (20, 40, 60 and 80%). Their drug delivery performance was assessed by the fine particle fraction (FPF). Roughness parameters, mean arithmetic roughness (R) and arithmetic mean height (S), of the carrier particles, were also evaluated using optical profilometry and scanning laser microscopy. Generally, particles of higher R had higher FPF. Higher S resulted in higher FPF only for particles with 60 and 80% coat levels. Reduced contact surface area between the drug particle and rougher carrier particle resulted in easier drug detachment during aerosolization. The 5 µm micronized lactose produced optimal carrier particles with respect to FPF and surface roughness. The study highlighted that with the ideal particles for surface roughening and coating level, surface roughening could be efficiently achieved by fluid bed coating for superior DPI performance.
载体颗粒的表面粗糙度会影响干粉吸入器（DPI）的性能。对于粗糙度对 DPI 性能的影响存在相反的观点。因此，需要采用系统的方法来改变载体表面，并评估其对药物输送的影响。通过流化床包衣用含有不同大小（2、5 和 8 μm）的微粉化乳糖的饱和乳糖来改变载体颗粒的表面，包衣到不同的水平（20、40、60 和 80%）。通过测定微细颗粒分数（FPF）评估它们的药物输送性能。使用光学轮廓仪和扫描激光显微镜评估载体颗粒的粗糙度参数，即平均算术粗糙度（R）和算术平均高度（S）。一般来说，R 值较高的颗粒具有较高的 FPF。对于包衣水平为 60%和 80%的颗粒，S 值较高仅导致较高的 FPF。在雾化过程中，药物颗粒与较粗糙的载体颗粒之间的接触表面积减小，导致药物更容易脱落。就 FPF 和表面粗糙度而言，5μm 微粉化乳糖产生的载体颗粒为最佳。该研究强调，通过流化床包衣，可以用理想的颗粒进行表面粗糙化和包衣水平，从而有效地实现表面粗糙化，以获得卓越的 DPI 性能。
