A novel micelle of coumarin derivative monoend-functionalized PEG for anti-tumor drug delivery: in vitro and in vivo study.

In this paper, a novel micelle for anti-tumor drug delivery was reported. Two 7-carboxymethoxy coumarin molecules were immobilized on the terminal group of a methoxy poly(ethylene glycol) chain via l-lysine as linker. The amphiphilic 7-carboxymethoxy coumarin monoend-functionalized methoxy poly(ethylene glycol) (mPEG-Lys-DCOU) chains were self-assembled micelles. Anti-tumor drug doxorubicin was loaded in the mPEG-Lys-DCOU micelles and the release profile was studied. The cytotoxicity of mPEG-Lys-DCOU was evaluated by NIH 3T3 fibroblasts. The drug-loaded micelles were incubated with HepG2 tumor cells to investigate the in vitro anti-tumor effect. The in vivo inhibition efficacy of drug-loaded micelles was carried out on 4T1 breast cancer animal model. The results showed that both hydrophobic and π-π stacking interactions within mPEG-Lys-DCOU amphiphiles were contributed to the self-assembly. Both blank and drug loaded micelles were monodisperse nanoparticles with the average diameters around 300 nm. The release profile exhibited certain pH dependence. The drug release rate at pH = 5.5 was much faster than that at pH = 7.4. mPEG-Lys-DCOU amphiphiles were non-toxic to NIH 3T3 fibroblasts. Both in vitro and in vivo studies demonstrated that the inhibition efficacy of drug-loaded micelles were comparable to that of doxorubicin hydrochloride. mPEG-Lys-DCOU micelles are promising carriers for anti-tumor drug delivery.
AuthorsYusi Lai, Youyu Long, Ying Lei, Xin Deng, Bin He, Mingming Sheng, Ming Li, Zhongwei Gu
JournalJournal of drug targeting (J Drug Target) Vol. 20 Issue 3 Pg. 246-54 (Apr 2012) ISSN: 1029-2330 [Electronic] England
PMID22118403 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Coumarins
  • Drug Carriers
  • Micelles
  • Polyethylene Glycols
  • Doxorubicin
  • Animals
  • Antineoplastic Agents (administration & dosage, chemistry, pharmacology, therapeutic use)
  • Breast Neoplasms (drug therapy, pathology)
  • Coumarins (adverse effects, chemistry)
  • Doxorubicin (administration & dosage, adverse effects, pharmacology, therapeutic use)
  • Drug Carriers (administration & dosage, chemistry, pharmacology, therapeutic use)
  • Drug Compounding
  • Female
  • Hep G2 Cells
  • Humans
  • Liver Neoplasms (drug therapy, pathology)
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Micelles
  • NIH 3T3 Cells
  • Nanoparticles (adverse effects, chemistry, ultrastructure)
  • Polyethylene Glycols (adverse effects, chemistry)
  • Random Allocation
  • Specific Pathogen-Free Organisms

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