Nasal drug absorption from powder formulations: The effect of three types of hydroxypropyl cellulose (HPC)

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• 作者：Akiko Tanaka^a ; Tomoyuki Furubayashi^b ; Manami Tomisaki^a ; Mayuko Kawakami^a ; Shunsuke Kimura^c ; Daisuke Inoue^b ; Kosuke Kusamori^a ; Hidemasa Katsumi^a ; Toshiyasu Sakane^a ; ^d ; ^{sakane@mb.kyoto-phu.ac.jp} ; Akira Yamamoto^a
• 关键词：Nasal drug absorption ; Powder formulation ; Hydroxypropyl cellulose ; Nasal residence ; Mucociliary clearance
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：96
• 期：Complete
• 页码：284-289
• 全文大小：675 K
• 卷排序：96

文摘

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.