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Development of folate-functionalized zein nanoparticles for ligand-directed delivery of paclitaxel

Title
Development of folate-functionalized zein nanoparticles for ligand-directed delivery of paclitaxel
Author
최한곤
Keywords
folic acid; paclitaxel; nanoparticle; zein
Issue Date
2019-10
Publisher
MDPI
Citation
PHARMACEUTICS, v. 11, No. 11, Article no. 562
Abstract
In this study, we investigated the active targeted delivery of a hydrophobic drug, paclitaxel (PTX), via receptor-mediated endocytosis by folate receptors expressed on cancer cells using a protein-based nanoparticle system. PTX was loaded on zein nanoparticles and conjugated with folate (PTX/Zein-FA) to estimate its chemotherapeutic efficacy in folate receptor-expressing KB cancer cells. PTX/Zein-FA nanoparticles were successfully developed, with a nanoparticle size of ~180 nm and narrow polydispersity index (~0.22). Accelerated release of PTX in an acidic environment was observed for PTX/Zein-FA. An in vitro cellular study of PTX/Zein-FAs in KB cells suggested that PTX/Zein-FA improved the cytotoxic activity of PTX on folate receptors overexpressed in cancer cells by inducing proapoptotic proteins and inhibiting anti-apoptotic proteins. In addition, PTX/Zein-FA exhibited anti-migratory properties and could alter the cell cycle profile of KB cells. A549 cells, which are folate receptor-negative cancer cells, showed no significant enhancement in the in vitro cellular activities of PTX/Zein-FA. We describe the antitumor efficacy of PTX/Zein-FA in KB tumor-bearing mice with minimum toxicity in healthy organs, and the results were confirmed in comparison with free drug and non-targeted nanoparticles.
URI
https://www.mdpi.com/1999-4923/11/11/562https://repository.hanyang.ac.kr/handle/20.500.11754/121248
ISSN
1999-4923
DOI
10.3390/pharmaceutics11110562
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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