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Curcumin Acetate Nanocrystals for Sustained Pulmonary Delivery: Preparation, Characterization and In Vivo Evaluation
Hu, Xiao1,2; Yang, Fei-Fei1,2; Wei, Xiao-Lan1,2; Yao, Guang-Yin3; Liu, Chun-Yu1,2; Zheng, Ying4; Liao, Yong-Hong1,2
2017-01
Source PublicationJOURNAL OF BIOMEDICAL NANOTECHNOLOGY
ISSN1550-7033
Volume13Issue:1Pages:84-94
Abstract

The main objective of this study was to test the hypothesis that inhaled nanocrystals of a highly lipophilic drug could be used as a novel approach for producing sustained pulmonary delivery. Curcumin acetate, an ester prodrug of curcumin, was utilized as a highly lipophilic model drug. Curcumin acetate was subjected to wet ball milling to produce different particle sizes of nanocrystals and microparticles, and the milled curcumin acetate was spray-dried to yield similar inhal-able microparticles. Following intrapulmonary administration in rats, pharmacokinetic experiments indicated that curcumin acetate significantly extended the pulmonary absorption time by 7.2-fold compared to curcumin, possibly due to the high lipophilicity of the former. The biodistribution data showed that aerosolized curcumin acetate nanocrystals 123.7 nm in size not only prolonged pulmonary retention, with the AUC value of curcumin acetate being 7.62-fold higher than that of the microparticles 1120 nm in size, but also increased the local in vivo release rate by 3.3-fold and the local availability of converted curcumin by 25.1-fold. In addition, the improved local availability resulted in better pharmacological efficacy in a monocrotaline-induced rat model of pulmonary arterial hypertension. This study was the first to demonstrate that inhalable nanocrystals are a feasible means for the sustained pulmonary delivery of highly lipophilic drugs.

KeywordSustained Pulmonary Delivery Curcumin Nanocrystals Lung Retention In Vivo Release
DOIhttps://doi.org/10.1166/jbn.2017.2326
URLView the original
Indexed BySCI
Language英语
WOS Research AreaScience & Technology - Other Topics ; Materials Science
WOS SubjectNanoscience & Nanotechnology ; Materials Science, bioMaterials
WOS IDWOS:000396466900008
PublisherAMER SCIENTIFIC PUBLISHERS
The Source to ArticleWOS
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Cited Times [WOS]:14   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorLiao, Yong-Hong
Affiliation1.Chinese Acad Med Sci, Inst Med Plant Dev, Beijing 100193, Peoples R China
2.Peking Union Med Coll, Beijing 100193, Peoples R China
3.Beijing Dingguochangsheng Biotechnol Co Ltd, Beijing 102209, Peoples R China
4.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau 999078, Peoples R China
Recommended Citation
GB/T 7714
Hu, Xiao,Yang, Fei-Fei,Wei, Xiao-Lan,et al. Curcumin Acetate Nanocrystals for Sustained Pulmonary Delivery: Preparation, Characterization and In Vivo Evaluation[J]. JOURNAL OF BIOMEDICAL NANOTECHNOLOGY,2017,13(1):84-94.
APA Hu, Xiao.,Yang, Fei-Fei.,Wei, Xiao-Lan.,Yao, Guang-Yin.,Liu, Chun-Yu.,...&Liao, Yong-Hong.(2017).Curcumin Acetate Nanocrystals for Sustained Pulmonary Delivery: Preparation, Characterization and In Vivo Evaluation.JOURNAL OF BIOMEDICAL NANOTECHNOLOGY,13(1),84-94.
MLA Hu, Xiao,et al."Curcumin Acetate Nanocrystals for Sustained Pulmonary Delivery: Preparation, Characterization and In Vivo Evaluation".JOURNAL OF BIOMEDICAL NANOTECHNOLOGY 13.1(2017):84-94.
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