期刊
PHARMACEUTICS
卷 10, 期 4, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics10040252
关键词
dry powder inhalation; L-leucine; netilmicin; moisture resistant; lower respiratory tract infection
资金
- National Natural Science Foundation of China [81673375, 81703431]
- Science and Technology Foundation Guangzhou [201509030006]
- Sun Yat-Sen University [16ykpy23]
- National Students Innovation Training Program of China [201801172]
Netilmicin (NTM) is one of the first-line drugs for lower respiratory tract infections (LRTI) therapy, but its nephrotoxicity and ototoxicity caused by intravenous injection restrict its clinical application. Dry powder inhalation (DPI) is a popular local drug delivery system that is introduced as a solution. Due to the nature of NTM hygroscopicity that hinders its direct use through DPI, in this study, L-leucine (LL) was added into NTM dry powder to reduce its moisture absorption rate and improve its aerosolization performance. NTM DPIs were prepared using spray-drying with different LL proportions. The particle size, density, morphology, crystallinity, water content, hygroscopicity, antibacterial activity, in vitro aerosolization performance, and stability of each formulation were characterized. NTM DPIs were suitable for inhalation and amorphous with a corrugated surface. The analysis indicated that the water content and hygroscopicity were decreased with the addition of LL, whilst the antibacterial activity of NTM was maintained. The optimal formulation ND2 (NTM:LL = 30:1) showed high fine particle fraction values (85.14 +/- 8.97%), which was 2.78-fold those of ND0 (100% NTM). It was stable after storage at 40 +/- 2 degrees C, 75 +/- 5% relative humidity (RH). The additional LL in NTM DPI successfully reduced the hygroscopicity and improved the aerosolization performance. NTM DPIs were proved to be a feasible and desirable approach for the treatment of LRTI.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据