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Anticancer drug delivery of PEG based micelles with small lipophilic moieties.

International journal of pharmaceutics (2013-06-13)
Ying Lei, Yusi Lai, Yuanlin Li, Sai Li, Gang Cheng, Dong Li, Haiping Li, Bin He, Zhongwei Gu
ABSTRACT

Herein, we reported a new type of self-assembly micelles based on amphiphilic polymers of cinnamate and coumarin derivatives modified PEG for drug delivery applications. Lipophilic cinnamic acid (CIN) and 7-carboxyl methoxycoumarin (COU) were immobilized on the terminal groups of poly(ethylene glycol) (PEG) to prepare amphiphiles. The amphiphiles self-assembled into micelles. The amphiphiles and micelles were characterized by (1)H NMR, FT-IR, DLS and TEM. Doxorubicin (DOX) was used as a model drug to investigate the lipophilic moieties effects on the drug release behaviors. The DOX loaded micelles were incubated with HepG2 liver cancer cells to study the in vitro anticancer activities. The results showed that DOX could be encapsulated in the micelles efficiently. The mean diameter of the drug loaded micelles was around 100 nm. Drug release profile revealed that the release rate of DOX loaded COU-PEG-COU micelles was significantly slower than that of CIN-PEG-CIN micelles. The DOX loaded micelles could be internalized in HepG2 cells. Both CLSM and flow cytometry results showed that the DOX loaded CIN-PEG-CIN micelles exhibited better anticancer efficacy.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
trans-Cinnamic acid, 97%
Sigma-Aldrich
trans-Cinnamic acid, natural, ≥99%, FCC, FG
Sigma-Aldrich
trans-Cinnamic acid, ≥99%, FG
Sigma-Aldrich
trans-Cinnamic acid, ≥99%
Supelco
trans-Cinnamic acid, analytical standard