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Paclitaxel-loaded poly(gamma-glutamic acid)-poly(lactide) nanoparticles as a targeted drug delivery system against cultured HepG2 cells.
- Source :
-
Bioconjugate chemistry [Bioconjug Chem] 2006 Mar-Apr; Vol. 17 (2), pp. 291-9. - Publication Year :
- 2006
-
Abstract
- The study was to develop paclitaxel-loaded formulations using a novel type of self-assembled nanoparticles that was composed of block copolymers synthesized from poly(gamma-glutamic acid) and poly(lactide) via a simple coupling reaction. The nanoparticles (the NPs) were prepared with various feed weight ratios of paclitaxel to block copolymer (the P/BC ratio). The morphology of all prepared nanoparticles was spherical and the surfaces were smooth. Increasing the P/BC ratio significantly increased the drug loading content of the prepared nanoparticles, but remarkably reduced the drug loading efficiency. The release rate of paclitaxel from the NPs decreased significantly as the P/BC ratio increased. For the potential of targeting liver cancer cells, galactosamine was further conjugated on the prepared nanoparticles (the Gal-NPs) as a targeting moiety. It was found that the activity in inhibiting the growth of HepG2 cells (a liver cancer cell line) by the Gal-NPs was comparable to that of a clinically available paclitaxel formulation, while the NPs displayed a significantly less activity. This may be attributed to the fact that the Gal-NPs had a specific interaction with HepG2 cells via ligand-receptor recognition. Cells treated with distinct paclitaxel formulations resulted in arrest in the G2/M phase. The arrest of cells in the G2/M phase was highly suggestive of interference by paclitaxel with spindle formation and was consistent with the morphological findings presented herein. In conclusion, the active targeting nature of the Gal-NPs prepared in the study may be used as a potential drug delivery system for the targeted delivery to liver cancers.
- Subjects :
- Antineoplastic Agents, Phytogenic chemistry
Antineoplastic Agents, Phytogenic therapeutic use
Galactosamine chemistry
Humans
Molecular Structure
Nanostructures chemistry
Paclitaxel analogs & derivatives
Polyesters chemistry
Polyesters therapeutic use
Polyglutamic Acid chemistry
Polyglutamic Acid metabolism
Polyglutamic Acid therapeutic use
Taxoids chemistry
Taxoids therapeutic use
Antineoplastic Agents, Phytogenic metabolism
Cell Line, Tumor
Drug Delivery Systems
Polyesters metabolism
Taxoids metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1043-1802
- Volume :
- 17
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioconjugate chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 16536458
- Full Text :
- https://doi.org/10.1021/bc0502107