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Polylysine and cysteine functionalized chitosan nanoparticle as an efficient platform for oral delivery of paclitaxel
Du,Xiao1; Yin,Shaoping1; Xu,Linqiang1; Ma,Jiqun1; Yu,Hua3; Wang,Guangji2; Li,Juan1
2020-02-01
Source PublicationCarbohydrate Polymers
ISSN0144-8617
Volume229
Abstract

A novel chitosan-based multifunctional nanoparticle (PY-CS-PLA) using cationic polylysine (PL) polymer and L-cysteine has been developed and investigated for the oral delivery of paclitaxel (PTX). As amphiphilic polymer, PY-CS-PLA presented good capability in self-assembling into spherical nanoparticle with mean size of 165 nm, and encapsulating PTX into the hydrophobic core. The encapsulated PTX was observed to be sustainedly released from the functionalized chitosan nanoparticle, and with a positive correlation to the pH value of the medium in the range of 1.2 to 7.4. The in vitro studies indicated that PY-CS-PLA/PTX could effectively enhance the cellular uptake of the PTX in Caco-2 cells. Pharmacokinetic result indicated that the oral bioavailability of PY-CS-PLA/PTX in rats was determined to be 5.63-fold to that of Taxol. Moreover, PY-CS-PLA/PTX improved the distribution of PTX in tumor site and presented better antitumor efficacy in Heps tumor-bearing mice and with less toxicity than other formulations. In conclusion, the PY-CS-PLA/PTX nanoparticle might be developed as a promising delivery vehicle for improving the oral bioavailability and therapeutic effect of hydrophobic antitumor drugs.

KeywordBioavailability Chitosan Mucoadhesion Nanoparticle Oral Delivery
DOI10.1016/j.carbpol.2019.115484
URLView the original
Indexed BySCIE
WOS Research AreaChemistry ; Polymer Science
WOS SubjectChemistry, Applied ; Chemistry, Organic ; Polymer Science
WOS IDWOS:000501796600093
Scopus ID2-s2.0-85074407375
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Cited Times [WOS]:36   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorLi,Juan
Affiliation1.Department of Pharmaceutics,School of Pharmacy,China Pharmaceutical University,Nanjing,210009,China
2.Center for New Drug Safety Evaluation and Research,China Pharmaceutical University,Nanjing,210009,China
3.Institute of Chinese Medical Sciences,State Key Laboratory of Quality Research in Chinese Medicine,University of Macau,Macao SAR,China
Recommended Citation
GB/T 7714
Du,Xiao,Yin,Shaoping,Xu,Linqiang,et al. Polylysine and cysteine functionalized chitosan nanoparticle as an efficient platform for oral delivery of paclitaxel[J]. Carbohydrate Polymers,2020,229.
APA Du,Xiao,Yin,Shaoping,Xu,Linqiang,Ma,Jiqun,Yu,Hua,Wang,Guangji,&Li,Juan.(2020).Polylysine and cysteine functionalized chitosan nanoparticle as an efficient platform for oral delivery of paclitaxel.Carbohydrate Polymers,229.
MLA Du,Xiao,et al."Polylysine and cysteine functionalized chitosan nanoparticle as an efficient platform for oral delivery of paclitaxel".Carbohydrate Polymers 229(2020).
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