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doi:10.1016/j.biomaterials.2006.12.018 
Copyright © 2006 Elsevier Ltd All rights reserved.
Folate-decorated poly(lactide-co-glycolide)-vitamin E TPGS nanoparticles for targeted drug delivery
Received 8 November 2006;
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Abstract
Doxorubicin-loaded nanoparticles (NPs) of vitamin E TPGS-folate (TPGS-FOL) conjugate and doxorubicin-poly(lactide-co-glycolide)-vitamin E TPGS (DOX-PLGA-TPGS) conjugate were prepared by the solvent extraction/evaporation method for targeted chemotherapy of folate-receptor rich tumors. X-ray photoelectron spectroscopy demonstrated that folate was distributed on the NP surface while the drug molecules were entrapped in the NP matrix. The NPs were found of 
350 nm diameter and exhibited a biphasic pattern of in vitro drug release. The cell uptake of the fluorescent NPs and the cell viability of the drug formulated in the NPs were quantitatively investigated, which were found dependent on the content of targeting TPGS-FOL conjugate. The NPs of 50% TPGS-FOL showed cellular uptake by MCF-7 cells 1.5 times higher and by C6 cells 1.7 times higher than the NPs with no TPGS-FOL component after 30 min incubation. The MCF-7 cell viability was found decreased significantly from 50.8% for the drug-loaded NPs of no TPGS-FOL to 8.2% for those of 50% TPGS-FOL after incubation at 100 μm drug concentration at 37 °C. The latter NPs also exhibited much lower IC50 value than the DOX after 24 h incubation, i.e., 19.4 vs. 43.7 μm for MCF-7 cells and 3.3 vs. >100 μm for C6 cells.
Keywords: Cancer nanotechnology; Biodegradable polymers; Doxorubicin; Nanomedicine; Nanobiotechnology
Article Outline
- 1. Introduction
- 2. Materials and methods
- 2.1. Materials
- 2.2. Synthesis of DOX-PLGA-TPGS
- 2.3. Synthesis of TPGS-FOL
- 2.4. Characterization of the synthesized conjugates
- 2.5. Preparation of DOX-loaded NPs
- 2.6. Characterization of the DOX-loaded NPs
- 2.7. Surface chemistry
- 2.8. In vitro drug release kinetics
- 2.9. In vitro cytotoxicity
- 2.10. In vitro cellular uptake of NPs
- 2.11. Statistical analysis
- 3. Results and discussion
- 3.1. Characterization of the synthesized conjugates
- 3.2. Characterization of DOX-loaded NPs
- 3.3. Surface chemistry
- 3.4. In vitro drug release
- 3.5. In vitro cytotoxicity
- 3.6. In vitro cellular uptake of NPs
- 4. Conclusion
- Acknowledgements
- References
