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Roles of maltodextrin and inulin as matrix formers on particle performance of inhalable drug nanocrystal-embedded microparticles

•FLA-NEP was respectively designed using MD and IN as matrix former.•FLA-NS could be embedded into the amorphous structure of MD or IN.•MD significantly prevented the aggregation of FLA-NEM induced by the high aw.•FLA-NEM/MD showed the excellent redispersibility and aerodynamic performance.•MD could...

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Published in:Carbohydrate polymers 2020-05, Vol.235, p.115937-115937, Article 115937
Main Authors: Luo, Yijing, Zhang, Zengzhu, Huang, Guiting, Yu, Huaping, Ma, Yueqin, Zheng, Qin, Yue, Pengfei
Format: Article
Language:English
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Summary:•FLA-NEP was respectively designed using MD and IN as matrix former.•FLA-NS could be embedded into the amorphous structure of MD or IN.•MD significantly prevented the aggregation of FLA-NEM induced by the high aw.•FLA-NEM/MD showed the excellent redispersibility and aerodynamic performance.•MD could be an excellent matrix former for inhalable FLA-NEM. The objective of this study was to investigate the influence of inulin (IL) and maltodextrin (MD) as matrix formers on the physical properties of drug nanocrystal-embedded microparticles (NEM) during spray-drying and storage. The redispersibility, aerodynamic performance and phase behaviour of NEM/MD and NEM/IL stored at different water activity (aw) values were evaluated. NEM with 2 g/g (relative to the weight of drug) of IL and MD exhibited the excellent performance after spray-drying. The water activity significantly influenced the redispersibility and aerodynamic performance of NEM/MD and NEM/IL. The NEM/MD presented a higher Tg at all aw values than did NEM/IL. The moisture-induced collapse of the amorphous glassy matrix of IL and MD could be responsible for the poor redispersibility and aerodynamic performance of NEM/IL and NEM/MD, respectively. The NEM/MD exhibited better aerodynamic performance at high aw (0.528) than did NEM/IL. Therefore, MD could be an excellent matrix former for inhalable NEM.
ISSN:0144-8617
1879-1344
DOI:10.1016/j.carbpol.2020.115937