TY - JOUR
T1 - Nasal drug absorption from powder formulations
T2 - The effect of three types of hydroxypropyl cellulose (HPC)
AU - Tanaka, Akiko
AU - Furubayashi, Tomoyuki
AU - Tomisaki, Manami
AU - Kawakami, Mayuko
AU - Kimura, Shunsuke
AU - Inoue, Daisuke
AU - Kusamori, Kosuke
AU - Katsumi, Hidemasa
AU - Sakane, Toshiyasu
AU - Yamamoto, Akira
N1 - Publisher Copyright:
© 2016
PY - 2017/1/1
Y1 - 2017/1/1
N2 - Despite the numerous advantages of powder formulations, few studies have described their nasal drug absorption. The first aim of this study was to compare the drug absorption from powder formulation with that from a liquid formulation in rats. Since pharmaceutical excipients are usually added to most powder formulations, the second aim of the study was to investigate the effect of hydroxypropyl cellulose (HPC) on nasal drug absorption from the powder. Three types of HPC with different polymerization degrees were used: HPC(SL), HPC(M), and HPC(H). The model drugs were warfarin (BCS Class I), piroxicam (BCS Class II), and sumatriptan (BCS Class III). The absorption of these model drugs in the powder form was higher than that from the solution. All HPCs failed to enhance warfarin absorption, while the piroxicam absorption was enhanced only by HPC(M). Sumatriptan absorption was not enhanced by HPC(SL), but by HPC(M) and HPC(H). The differences in nasal absorption of the three model drugs promoted by HPCs depend on the permeability and solubility of the drug. Moreover, the nasal retention of different formulations was increased by HPCs. Because HPCs showed no toxic effect on the nasal epithelium. These findings indicate that powder formulations supplemented with HPC are a valuable and promising approach to increase the nasal absorption of highly soluble and poorly permeable drugs.
AB - Despite the numerous advantages of powder formulations, few studies have described their nasal drug absorption. The first aim of this study was to compare the drug absorption from powder formulation with that from a liquid formulation in rats. Since pharmaceutical excipients are usually added to most powder formulations, the second aim of the study was to investigate the effect of hydroxypropyl cellulose (HPC) on nasal drug absorption from the powder. Three types of HPC with different polymerization degrees were used: HPC(SL), HPC(M), and HPC(H). The model drugs were warfarin (BCS Class I), piroxicam (BCS Class II), and sumatriptan (BCS Class III). The absorption of these model drugs in the powder form was higher than that from the solution. All HPCs failed to enhance warfarin absorption, while the piroxicam absorption was enhanced only by HPC(M). Sumatriptan absorption was not enhanced by HPC(SL), but by HPC(M) and HPC(H). The differences in nasal absorption of the three model drugs promoted by HPCs depend on the permeability and solubility of the drug. Moreover, the nasal retention of different formulations was increased by HPCs. Because HPCs showed no toxic effect on the nasal epithelium. These findings indicate that powder formulations supplemented with HPC are a valuable and promising approach to increase the nasal absorption of highly soluble and poorly permeable drugs.
KW - Hydroxypropyl cellulose
KW - Mucociliary clearance
KW - Nasal drug absorption
KW - Nasal residence
KW - Powder formulation
UR - http://www.scopus.com/inward/record.url?scp=84992036663&partnerID=8YFLogxK
U2 - 10.1016/j.ejps.2016.09.028
DO - 10.1016/j.ejps.2016.09.028
M3 - 学術論文
C2 - 27664332
AN - SCOPUS:84992036663
SN - 0928-0987
VL - 96
SP - 284
EP - 289
JO - European Journal of Pharmaceutical Sciences
JF - European Journal of Pharmaceutical Sciences
ER -