Development of Folate-Functionalized PEGylated Zein Nanoparticles for Ligand-Directed Delivery of Paclitaxelopen access
- Authors
- Soe, Zar Chi; Ou, Wenquan; Gautam, Milan; Poudel, Kishwor; Kim, Bo Kyun; Pham, Le Minh; Phung, Cao Dai; Jeong, Jee-Heon; Jin, Sung Giu; Choi, Han-Gon; Ku, Sae Kwang; Yong, Chul Soon; Kim, Jong Oh
- Issue Date
- Nov-2019
- Publisher
- MDPI
- Keywords
- folic acid; paclitaxel; nanoparticle; zein
- Citation
- PHARMACEUTICS, v.11, no.11
- Indexed
- SCIE
SCOPUS
- Journal Title
- PHARMACEUTICS
- Volume
- 11
- Number
- 11
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/2069
- DOI
- 10.3390/pharmaceutics11110562
- ISSN
- 1999-4923
- 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 similar to 180 nm and narrow polydispersity index (similar to 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.
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