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Nanoparticles mediating the sustained puerarin release facilitate improved brain delivery to treat parkinson's disease
Chen,Tongkai1,2,5; Liu,Wei1,2; Xiong,Sha1,2; Li,Dongli1,2; Fang,Shuhuan1,2; Wu,Zhenfeng3; Wang,Qi1,2; Chen,Xiaojia4,6
Source PublicationACS Applied Materials and Interfaces

Recent work has highlighted the potential of puerarin (PU) as a valuable compound to treat Parkinson's disease (PD), but its undesirable water solubility and bioavailability have constrained its utility. In this study, we sought to develop nanoparticles (NPs) that could be used to encapsulate PU, thereby extending its in vivo half-life and improving its bioavailability and accumulation in the brain to treat the symptoms of PD. We prepared spherical NPs (88.36 ± 1.67 nm) from six-Armed star-shaped poly(lactide-co-glycolide) (6-s-PLGA) NPs that were used to encapsulate PU (PU-NPs) with 89.52 ± 1.74% encapsulation efficiency, 42.97 ± 1.58% drug loading, and a 48 h sustained drug release. NP formation and drug loading were largely mediated by hydrophobic interactions, while changes in the external environment led these NPs to become increasingly hydrophilic, thereby leading to drug release. Relative to PU alone, PU-NPs exhibited significantly improved cellular internalization, permeation, and neuroprotective effects. Upon the basis of Förster resonance energy transfer (FRET) of NPs-Administered zebrafish, we were able to determine that these NPs were rapidly absorbed into circulation whereupon they were able to access the brain. We further conducted oral PU-NPs administration to rats, revealing significant improvements in PU accumulation within the plasma and brain relative to rats administered free PU. In MPTP-mediated neurotoxicity in mice, we found that PU-NPs treatment improved disease-Associated behavioral deficits and depletion of dopamine and its metabolites. These findings indicated that PU-NPs represent a potentially viable approach to enhancing PU oral absorption, thus improving its delivery to the brain wherein it can aid in the treatment of PD.

KeywordBrain Delivery Nanoparticles Neuroprotective Effects Puerarin Sustained Release
URLView the original
Indexed BySCIE
WOS Research AreaScience & Technology - Other Topics ; Materials Science
WOS SubjectNanoscience & Nanotechnology ; Materials Science, Multidisciplinary
WOS IDWOS:000501620700038
Scopus ID2-s2.0-85074796022
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Cited Times [WOS]:33   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorChen,Tongkai; Chen,Xiaojia
Affiliation1.Science and Technology Innovation Center,Guangzhou University of Chinese Medicine,Guangzhou,510405,China
2.Institute of Clinical Pharmacology,Guangzhou University of Chinese Medicine,Guangzhou,510405,China
3.Key Laboratory of Modern Preparation of Traditional Chinese Medicine,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang,330004,China
4.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macau,999078,Macao
5.Address: Institute of Clinical Pharmacology,Guangzhou University of Chinese Medicine,Guangzhou,12 Jichang Road,510405,China
6.Institute of Chinese Medical Sciences,University of Macau,Taipa,Room 6007, N22,Macao
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Chen,Tongkai,Liu,Wei,Xiong,Sha,et al. Nanoparticles mediating the sustained puerarin release facilitate improved brain delivery to treat parkinson's disease[J]. ACS Applied Materials and Interfaces,2019,11(48):45276-45289.
APA Chen,Tongkai,Liu,Wei,Xiong,Sha,Li,Dongli,Fang,Shuhuan,Wu,Zhenfeng,Wang,Qi,&Chen,Xiaojia.(2019).Nanoparticles mediating the sustained puerarin release facilitate improved brain delivery to treat parkinson's disease.ACS Applied Materials and Interfaces,11(48),45276-45289.
MLA Chen,Tongkai,et al."Nanoparticles mediating the sustained puerarin release facilitate improved brain delivery to treat parkinson's disease".ACS Applied Materials and Interfaces 11.48(2019):45276-45289.
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