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Background <p>Intranasal powder formulations offer advantages in terms of stability and portability; however, their absorption is critically dependent on dissolution within the limited fluid volume of the nasal cavity. Conventional dissolution tests, originally developed for oral medicines, fail to adequately capture dissolution dynamics under nasal conditions, making the prediction of bioavailability after intranasal powder administration (BAp) particularly challenging.</p> Methods <p>A Raman spectroscopy-based approach was established to directly monitor the time-dependent dissolution of drug particles in Calu-3 cell layers. Dissolution rate constants derived from particle size reduction were integrated with the nasal mean residence time (MRT) and bioavailability after intranasal solution administration (BAs) to define a predictive metric, the dissolution-MRT-BAs (DTB) parameter.</p> Results <p>Model drugs exhibited distinct dissolution profiles: rapid (antipyrine and atenolol), intermediate (acyclovir and levofloxacin), and limited (norfloxacin and griseofulvin). The DTB parameter was strongly correlated with BAp (R = 0.983, p &lt; 0.001), and the enhancement of norfloxacin dissolution by lactose was also captured by this metric.</p> Conclusion <p>The DTB parameter, which integrates dissolution kinetics, nasal residence time, and bioavailability, serves as a rational tool for predicting the absorption behavior of nasal powder formulations. This study highlights the potential of Raman spectroscopy as a quantitative method to support formulation design and establish <i>in vitro</i>-<i>in vivo</i> correlations in nasal drug delivery.</p>

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Raman Imaging-based Analysis of Drug Powder Dissolution on Calu-3 Cell Monolayers as a Mechanistic Predictor of Nasal Absorption

  • 期刊论文

  • 发表日期：

    2026年5月5日

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  • Tomoyuki Furubayashi,
  • Akiko Tanaka,
  • Ryosuke Tatsuta,
  • Maako Fujiwara,
  • Nana Izumi,
  • Mamiko Kiyohara,
  • Kei Moriyama

摘要

Background

Intranasal powder formulations offer advantages in terms of stability and portability; however, their absorption is critically dependent on dissolution within the limited fluid volume of the nasal cavity. Conventional dissolution tests, originally developed for oral medicines, fail to adequately capture dissolution dynamics under nasal conditions, making the prediction of bioavailability after intranasal powder administration (BAp) particularly challenging.

Methods

A Raman spectroscopy-based approach was established to directly monitor the time-dependent dissolution of drug particles in Calu-3 cell layers. Dissolution rate constants derived from particle size reduction were integrated with the nasal mean residence time (MRT) and bioavailability after intranasal solution administration (BAs) to define a predictive metric, the dissolution-MRT-BAs (DTB) parameter.

Results

Model drugs exhibited distinct dissolution profiles: rapid (antipyrine and atenolol), intermediate (acyclovir and levofloxacin), and limited (norfloxacin and griseofulvin). The DTB parameter was strongly correlated with BAp (R = 0.983, p < 0.001), and the enhancement of norfloxacin dissolution by lactose was also captured by this metric.

Conclusion

The DTB parameter, which integrates dissolution kinetics, nasal residence time, and bioavailability, serves as a rational tool for predicting the absorption behavior of nasal powder formulations. This study highlights the potential of Raman spectroscopy as a quantitative method to support formulation design and establish in vitro-in vivo correlations in nasal drug delivery.