Ternary Dry Powder Agglomerate Inhalation Formulation of Melatonin With Air Jet Mixing to Improve In Vitro And In Vivo Performance
Copyright © 2023 The Authors. Published by Elsevier Inc. All rights reserved..
An improved agglomerate formulation with melatonin and fine lactose for dry powder inhalation using Turbuhaler® was developed. Co-grinding lactose with 1 % magnesium stearate prior to air jet mixing served as a key factor to improve the in vitro aerosolization and in vivo efficacy. Elevated mixing pressure facilitated the dispersion and homogenization of the cohesive mixture for even distribution of agglomerate size after spheroidization and subsequent higher emitted dose with lower variation. Magnesium stearate was employed as a tertiary component to adjust the interparticle force for better aerosolization. At optimized mixing pressure, co-grinding lactose with magnesium stearate before jet mixing displayed further improvement of fine particle fraction to 71.6 ± 3.1 %. The superior fine particle deposition efficiency contributed to rapid onset of action and a high bioavailability of 67.0 % after intratracheal administration to rats. Overall, an inhalable melatonin dry powder formulation exhibiting good aerosol property and lung deposition with clinical translation potential was developed.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:113 |
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| Enthalten in: |
Journal of pharmaceutical sciences - 113(2024), 2 vom: 04. Feb., Seite 434-444 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Zhang, Qingzhen [VerfasserIn] |
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| Links: |
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| Themen: |
Aerosols |
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| Anmerkungen: |
Date Completed 22.01.2024 Date Revised 05.03.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.xphs.2023.11.016 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM364870974 |
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| 520 | |a Copyright © 2023 The Authors. Published by Elsevier Inc. All rights reserved. | ||
| 520 | |a An improved agglomerate formulation with melatonin and fine lactose for dry powder inhalation using Turbuhaler® was developed. Co-grinding lactose with 1 % magnesium stearate prior to air jet mixing served as a key factor to improve the in vitro aerosolization and in vivo efficacy. Elevated mixing pressure facilitated the dispersion and homogenization of the cohesive mixture for even distribution of agglomerate size after spheroidization and subsequent higher emitted dose with lower variation. Magnesium stearate was employed as a tertiary component to adjust the interparticle force for better aerosolization. At optimized mixing pressure, co-grinding lactose with magnesium stearate before jet mixing displayed further improvement of fine particle fraction to 71.6 ± 3.1 %. The superior fine particle deposition efficiency contributed to rapid onset of action and a high bioavailability of 67.0 % after intratracheal administration to rats. Overall, an inhalable melatonin dry powder formulation exhibiting good aerosol property and lung deposition with clinical translation potential was developed | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a Air jet mixing | |
| 650 | 4 | |a High bioavailability | |
| 650 | 4 | |a Inhalable melatonin agglomerates | |
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| 700 | 1 | |a Kou, Shanglong |e verfasserin |4 aut | |
| 700 | 1 | |a Cui, Yingtong |e verfasserin |4 aut | |
| 700 | 1 | |a Dong, Jie |e verfasserin |4 aut | |
| 700 | 1 | |a Ye, Yuqing |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Yuanyuan |e verfasserin |4 aut | |
| 700 | 1 | |a Lu, Rui |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Xinduo |e verfasserin |4 aut | |
| 700 | 1 | |a Nie, Yi |e verfasserin |4 aut | |
| 700 | 1 | |a Shi, Kaiqi |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Fang |e verfasserin |4 aut | |
| 700 | 1 | |a Hall, Philip |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Xiaoling |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Zheng |e verfasserin |4 aut | |
| 700 | 1 | |a Jiang, Xingtao |e verfasserin |4 aut | |
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