Citation: Li Huilan, Li Jieming, He Xinyi, Zhang Bo, Liu Chunxia, Li Qifei, Zhu Ying, Huang Wenlong, Zhang Wei, Qian Hai, Ge Liang. Histology and antitumor activity study of PTX-loaded micelle, a fluorescent drug delivery system prepared by PEG-TPP[J]. Chinese Chemical Letters, ;2019, 30(5): 1083-1088. doi: 10.1016/j.cclet.2019.01.003 shu

Histology and antitumor activity study of PTX-loaded micelle, a fluorescent drug delivery system prepared by PEG-TPP

Li Huilan ^a ,
Li Jieming ^a ,
He Xinyi ^b ,
Zhang Bo ^a ,
Liu Chunxia ^a ,
Li Qifei ^a ,
Zhu Ying ^b ,
Huang Wenlong ^a,c ,
Zhang Wei ^d ,
Qian Hai ^a,c,*, ,
Ge Liang ^b,**,

a.
Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China
b.
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
c.
Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing 210009, China
d.
Department of Biochemistry and Molecular Biology, Nanjing Medical University, Nanjing 10029, China

^**

qianhai24@163.com

geliang1981@hotmail.com

Received Date: 17 December 2018
Revised Date: 2 January 2019
Accepted Date: 3 January 2019
Available Online: 7 May 2019

Figures(5)

We synthesized PEG-TPP as carrier to encapsulate paclitaxel (PTX) in the form of micelles to overcome its water-solubility problem. PTX-loaded micelles possess a-week stability and appropriate particle size (152.1±1.2 nm) which is beneficial for enhanced permeability and retention (EPR) effect. Strong pH dependence of PTX releasing from micelles is verified by in vitro release study. At cellular level, PTX-loaded micelles can target mitochondria effectively which may results a better cytotoxicity of micelles (especially IC₅₀=0.123±0.035 μmol/L of micelles and 0.298±0.067 μmol/L of PTX alone on MCF-7 cells). The fluorescence distributions of both isolated and sliced organs show that the micelles can effectively target tumors. Moreover, we further prove the enhanced therapeutic effects of micelles in tumor-bearing mice comparing with PTX alone. The results show that the biodegradable drug delivery system prepared by PEG-TPP can overcome the poor solubility of paclitaxel and improve its tumor targeting and antitumor activity.
- PEG-TPP,
- Anticancer,
- Micelles,
- EPR,
- Mitochondria
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