Polylysine and cysteine functionalized chitosan nanoparticle as an efficient platform for oral delivery of paclitaxel.
Carbohydr Polym
; 229: 115484, 2020 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-31826482
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 165â¯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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Polilisina
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Portadores de Fármacos
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Paclitaxel
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Cisteína
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Quitosana
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Nanopartículas
Limite:
Animals
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Humans
Idioma:
En
Revista:
Carbohydr Polym
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
China