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Purpose <p>Various ternary components, such as lactose fines and magnesium stearate (MgSt), are frequently incorporated into carrier-based dry powder inhalations (DPIs) to enhance the fine particle fraction (FPF). However, the specific effects of a combination of lactose fines and MgSt on the performance of DPI formulations have not yet been reported.</p> Methods <p>Using salbutamol sulfate (SS), which has a weak drug-carrier adhesion, as a model drug, this study investigated the impact of lactose fines content on the powder properties and aerosolization performance of 0.5% MgSt containing DPI formulations. The influence of the mixing order of MgSt and lactose fines on DPI formulation performance was also examined. Finally, an attempt was made to predict the FPF using powder rheological parameters.</p> Results <p>The addition of 1–10% lactose fines to 0.5% MgSt containing SS-DPI formulations significantly improved the FPF, but the addition of MgSt had a negative impact on FPF according to the mixing order of the carrier-MgSt-lactose fines-drug. The mixing order of the MgSt and lactose fines significantly affected the deposition of SS. The FPF of the formulation mixed with 5% lactose fines followed by 0.5% MgSt was significantly higher (46.55%) than that of the formulation mixed with 0.5% MgSt followed by 5% lactose fines (33.86%) and the formulation with only 5% lactose fines (39.53%). Good flowability (24.44%) and strong adhesion (75.56%) were the key factors affecting the in vitro drug deposition in this system.</p> Conclusion <p>During the development of DPIs, ternary components should be selectively added in a specific mixing order based on drug-carrier adhesion to achieve optimal lung deposition.</p>

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Selected addition of ternary component at specific mixing order to tune drug-carrier adhesion for enhanced lung deposition

  • 期刊论文

  • 发表日期：

    2025年1月31日

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  • Xianhong He,
  • Jiayi Li,
  • Haoyuan Xu,
  • Sibo Ma,
  • Xuanguang Zhan,
  • Xuhong Ren,
  • Xin Zhang,
  • Jian Guan,
  • Shirui Mao

摘要

Purpose

Various ternary components, such as lactose fines and magnesium stearate (MgSt), are frequently incorporated into carrier-based dry powder inhalations (DPIs) to enhance the fine particle fraction (FPF). However, the specific effects of a combination of lactose fines and MgSt on the performance of DPI formulations have not yet been reported.

Methods

Using salbutamol sulfate (SS), which has a weak drug-carrier adhesion, as a model drug, this study investigated the impact of lactose fines content on the powder properties and aerosolization performance of 0.5% MgSt containing DPI formulations. The influence of the mixing order of MgSt and lactose fines on DPI formulation performance was also examined. Finally, an attempt was made to predict the FPF using powder rheological parameters.

Results

The addition of 1–10% lactose fines to 0.5% MgSt containing SS-DPI formulations significantly improved the FPF, but the addition of MgSt had a negative impact on FPF according to the mixing order of the carrier-MgSt-lactose fines-drug. The mixing order of the MgSt and lactose fines significantly affected the deposition of SS. The FPF of the formulation mixed with 5% lactose fines followed by 0.5% MgSt was significantly higher (46.55%) than that of the formulation mixed with 0.5% MgSt followed by 5% lactose fines (33.86%) and the formulation with only 5% lactose fines (39.53%). Good flowability (24.44%) and strong adhesion (75.56%) were the key factors affecting the in vitro drug deposition in this system.

Conclusion

During the development of DPIs, ternary components should be selectively added in a specific mixing order based on drug-carrier adhesion to achieve optimal lung deposition.