Inoue Daisuke, Seto Yoshihiro, To Hideto
Department of Medical Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, University of Toyama, 2630 Sugitani, Toyama 930-0194, Japan.
Molecular Pharmaceutics Laboratory, College of Pharmaceutical Sciences, Ritsumeikan University, 1-1-1 Noji-higashi, Kusatsu Shiga 525-8577, Japan.
Pharmaceutics. 2025 Jun 30;17(7):863. doi: 10.3390/pharmaceutics17070863.
: The precise control of drug absorption through the nasal mucosa following intranasal administration can be achieved through optimal formulation development that considers the nasal retention properties of the administered dosage form. This study aimed to quantitatively elucidate the effect of formulation type on nasal residence time in vivo. : The nasal residence behavior of various formulation types, including solutions, particulates, and powders, was estimated in rats. Furthermore, the effect of mucoadhesive polymers on the nasal residence time was investigated using gel and powder dosage forms of sodium alginate. : The nasal retention behavior of the formulation in the nasal cavity differed depending on the dosage form. The polystyrene microparticles and lactose powder, a non-adhesive powder, were quickly eliminated into the nasopharynx, whereas the solution remained in the nasal cavity longer than the other formulations. The clearance behavior of the solution was investigated, and it was found that the solution was quickly transported to the stomach without being retained in the esophagus. The disappearance of the gel and powder with the mucoadhesive polymer was different, with the powder clearing faster. This difference in clearance is thought to be due to the powder being cleared before dissolving and diffusing into the nasal mucus. : It has been clearly shown that the nasal residence behavior differed depending on the dosage forms. The addition of mucoadhesive polymers was effective in improving the nasal residence of the drug, and more-effective formulations for nasal application can be developed by combining optimal dosage forms, such as powders and gels.
通过鼻内给药后，可通过考虑给药剂型鼻腔滞留特性的优化制剂开发来实现对药物经鼻黏膜吸收的精确控制。本研究旨在定量阐明制剂类型对体内鼻腔滞留时间的影响。在大鼠中评估了包括溶液、颗粒剂和粉剂在内的各种制剂类型的鼻腔滞留行为。此外，使用海藻酸钠的凝胶和粉剂剂型研究了黏膜黏附聚合物对鼻腔滞留时间的影响。制剂在鼻腔中的滞留行为因剂型而异。聚苯乙烯微粒和乳糖粉（一种非黏附性粉末）迅速排入鼻咽部，而溶液在鼻腔中停留的时间比其他制剂更长。对溶液的清除行为进行了研究，发现溶液迅速输送到胃中，而未滞留在食管中。含有黏膜黏附聚合物的凝胶和粉剂的清除情况不同，粉剂清除得更快。这种清除差异被认为是由于粉剂在溶解并扩散到鼻黏液之前就被清除了。已经清楚地表明，鼻腔滞留行为因剂型而异。添加黏膜黏附聚合物有效地改善了药物的鼻腔滞留，并且通过组合粉末和凝胶等最佳剂型可以开发出更有效的鼻腔应用制剂。
