PEG-PCL nanomicelles for cancer theranosis: targeted imaging and drug delivery

doi:10.5246/jcps.2012.06.075

Abstract

Abstract:

Nanomicelles, self-assembling nanosized particles with a hydrophobic core and hydrophilic shell, are currently successfully used as carriers for targeted drug delivery systems via the enhanced permeability and retention (EPR) effect at the tumor sites. In this study, a near-infrared fluorescent cyanine dye (Cy7-NHS) was conjugated to poly (ethylene glycol)-block-poly (ε-caprolactone) (NH₂-PEG-b-PCL), and the resulting Cy7-PEG-PCL was further mixed with mPEG-b-PCL to form nanomicelles as carriers for paclitaxel (PTX) delivery. Our results showed that the selected mPEG₄₀₀₀-b-PCL₂₅₀₀copolymers self-assembled to form stable micelles with an average size of 30 nm in diameter and a zeta potential of approximately –3 mV. The micelles also exhibited more than 95% encapsulation efficiency of PTX when the molar ratio between paclitaxel and copolymers was 1/4. In vitro cytotoxicity study showed that the PTX-loaded nanomicelles had a similar cell growth inhibition efficacy to that of Taxol^® against human breast cancer MCF-7 cells. In vivo imaging showed that the Cy7-labeled nanomicelles could be passively targeted to tumor sites effectively after intravenous injection via the tail vein. Also, a strong anti-tumor activity was observed in the nude mice xenografted MCF-7 breast tumor after treatment with PTX-loaded micelles, similar to that of Taxol^®. As a result, the micelle drug delivery system designed in this paper has great potential in targeted imaging of tumors and chemotherapy.

Key words: Micelles, PEG-b-PCL block copolymers, Paclitaxel, Cyanine dye, In vivo imaging, Tumor therapy

CLC Number:

R943

Supporting:

Hua Zheng, Wenjie Hou, Jiancheng Wang^*, Qiang Zhang. PEG-PCL nanomicelles for cancer theranosis: targeted imaging and drug delivery [J]. , DOI: 10.5246/jcps.2012.06.075.

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