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The effect of hydrophilic and hydrophobic structure of amphiphilic polymeric micelles on their transportation in rats
Feiyang Deng1; Chao Yu1; Hua Zhang1; Wenbing Dai1; Bing He1; Ying Zheng2; Xueqing Wang1; Qiang Zhang1,3
2016-02-01
Source PublicationCurrent Drug Delivery
ISSN1567-2018
Volume13Issue:1Pages:105-110
Abstract

In the previous study, we have clarified how the hydrophilic and hydrophobic structures of amphiphilic polymers impact the transport of their micelles (PEEP-PCL, PEG-PCL and PEG-DSPE micelles) in epithelial MDCK cells (Biomaterials 2013, 34: 6284-6298). In this study, we attempt to clarify the behavior of the three micelles in rats. Coumarin-6 loaded micelles were injected into different sections of intestine of rats and observed by confocal laser scanning microscope (CLSM) or orally administrated and conducted pharmacokinetic study. All of the three kinds of micelles were able to cross the intestinal epithelial cells and enter blood circulation. The PEEP-PCL micelles demonstrated the fastest distribution mainly in duodenum, while the PEGDSPE micelles showed the longest distribution with the highest proportion in ileum of the three. No significant difference was observed among the pharmacokinetic parameters of the three micelles. The results were consistent in the two analysis methods mentioned above, yet there were some differences between in vivo and in vitro results reported previously. It might be the distinction between the environments in MDCK model and intestine that led to the discrepancy. The hydrophobicity of nanoparticles could both enhance uptake and hinder the transport across the mucus. However, there was no intact mucus in MDCK model, which preferred hydrophobic nanoparticles. PEEP was the most hydrophilic material constructing the micelles in the study and its uptake would be increased in rats compared to that in MDCK model, while DSPE was more hydrophobic than the others and MDCK model would be more ideal for its uptake. Considering the inconsistency of the results in the two models, whether the methods researchers were generally using at present were reasonable needs further investigation.

KeywordAmphiphilic Micelles Hydrophilicity Hydrophobicity In Vivo Pharmacokinetic Transport
DOIhttps://doi.org/10.2174/1567201812666150722122657
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000372335200012
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Cited Times [WOS]:3   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Co-First AuthorFeiyang Deng
Corresponding AuthorXueqing Wang
Affiliation1.Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau SAR, China
3.The State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China
Recommended Citation
GB/T 7714
Feiyang Deng,Chao Yu,Hua Zhang,et al. The effect of hydrophilic and hydrophobic structure of amphiphilic polymeric micelles on their transportation in rats[J]. Current Drug Delivery,2016,13(1):105-110.
APA Feiyang Deng.,Chao Yu.,Hua Zhang.,Wenbing Dai.,Bing He.,...&Qiang Zhang.(2016).The effect of hydrophilic and hydrophobic structure of amphiphilic polymeric micelles on their transportation in rats.Current Drug Delivery,13(1),105-110.
MLA Feiyang Deng,et al."The effect of hydrophilic and hydrophobic structure of amphiphilic polymeric micelles on their transportation in rats".Current Drug Delivery 13.1(2016):105-110.
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