Cargando…
Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying
Co-suspension drug-loading technology, namely Aerosphere™, can improve fine particle fraction (FPF) and delivered dose content uniformity (DDCU). However, because of its poor drug-loading efficacy, the phospholipid carrier dosage in Aerosphere™ is usually dozens of times greater than that of the dru...
Autores principales: | , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier
2023
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9988654/ https://www.ncbi.nlm.nih.gov/pubmed/36896094 http://dx.doi.org/10.1016/j.ijpx.2023.100158 |
_version_ | 1784901613643628544 |
---|---|
author | Xi, Quan Miao, Jiaying Cao, Zhen Wang, Hao |
author_facet | Xi, Quan Miao, Jiaying Cao, Zhen Wang, Hao |
author_sort | Xi, Quan |
collection | PubMed |
description | Co-suspension drug-loading technology, namely Aerosphere™, can improve fine particle fraction (FPF) and delivered dose content uniformity (DDCU). However, because of its poor drug-loading efficacy, the phospholipid carrier dosage in Aerosphere™ is usually dozens of times greater than that of the drug, resulting in a high material cost and blockage of the actuator. In this study, spray-freeze-drying (SFD) technology was used to prepare inhalable distearoylphosphatidylcholine (DSPC)-based microparticles for pressurized metered-dose inhalers (pMDI). Water-soluble, low-dose formoterol fumarate was used as an indicator to evaluate the aerodynamic performance of the inhalable microparticles. Water-insoluble, high-dose mometasone furoate was used to investigate the effects of drug morphology and drug-loading mode on the drug delivery efficiency of the microparticles. The results demonstrated that DSPC-based microparticles prepared using the co-SFD technology not only achieved higher FPF and more consistent delivered dose than those of drug crystal-only pMDI, but the amount of DSPC was also reduced to approximately 4% of that prepared using the co-suspension technology. This SFD technology may also be used to improve the drug delivery efficiency of other water-insoluble and high-dose drugs. |
format | Online Article Text |
id | pubmed-9988654 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | Elsevier |
record_format | MEDLINE/PubMed |
spelling | pubmed-99886542023-03-08 Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying Xi, Quan Miao, Jiaying Cao, Zhen Wang, Hao Int J Pharm X Research Paper Co-suspension drug-loading technology, namely Aerosphere™, can improve fine particle fraction (FPF) and delivered dose content uniformity (DDCU). However, because of its poor drug-loading efficacy, the phospholipid carrier dosage in Aerosphere™ is usually dozens of times greater than that of the drug, resulting in a high material cost and blockage of the actuator. In this study, spray-freeze-drying (SFD) technology was used to prepare inhalable distearoylphosphatidylcholine (DSPC)-based microparticles for pressurized metered-dose inhalers (pMDI). Water-soluble, low-dose formoterol fumarate was used as an indicator to evaluate the aerodynamic performance of the inhalable microparticles. Water-insoluble, high-dose mometasone furoate was used to investigate the effects of drug morphology and drug-loading mode on the drug delivery efficiency of the microparticles. The results demonstrated that DSPC-based microparticles prepared using the co-SFD technology not only achieved higher FPF and more consistent delivered dose than those of drug crystal-only pMDI, but the amount of DSPC was also reduced to approximately 4% of that prepared using the co-suspension technology. This SFD technology may also be used to improve the drug delivery efficiency of other water-insoluble and high-dose drugs. Elsevier 2023-01-03 /pmc/articles/PMC9988654/ /pubmed/36896094 http://dx.doi.org/10.1016/j.ijpx.2023.100158 Text en © 2023 The Authors https://creativecommons.org/licenses/by-nc-nd/4.0/This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Research Paper Xi, Quan Miao, Jiaying Cao, Zhen Wang, Hao Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title | Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title_full | Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title_fullStr | Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title_full_unstemmed | Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title_short | Inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
title_sort | inhalable aerosol microparticles with low carrier dosage and high fine particle fraction prepared by spray-freeze-drying |
topic | Research Paper |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9988654/ https://www.ncbi.nlm.nih.gov/pubmed/36896094 http://dx.doi.org/10.1016/j.ijpx.2023.100158 |
work_keys_str_mv | AT xiquan inhalableaerosolmicroparticleswithlowcarrierdosageandhighfineparticlefractionpreparedbysprayfreezedrying AT miaojiaying inhalableaerosolmicroparticleswithlowcarrierdosageandhighfineparticlefractionpreparedbysprayfreezedrying AT caozhen inhalableaerosolmicroparticleswithlowcarrierdosageandhighfineparticlefractionpreparedbysprayfreezedrying AT wanghao inhalableaerosolmicroparticleswithlowcarrierdosageandhighfineparticlefractionpreparedbysprayfreezedrying |