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Pluronic P123-docetaxel conjugate micelles: synthesis, characterization, and antitumor activity.
- Source :
-
Journal of biomedical nanotechnology [J Biomed Nanotechnol] 2013 Dec; Vol. 9 (12), pp. 2007-16. - Publication Year :
- 2013
-
Abstract
- The purpose of this research is to develop and evaluate Pluronic P123 (P123)-docetaxel (DTX) conjugate that could form core-shell-type micelles in aqueous solution. DTX was covalently conjugated to P123 via ester bond after the activation of DTX by succinic anhydride. The structure of P123-DTX conjugate was confirmed by 1H-NMR. The self-assembly behavior of the P123-DTX conjugate in aqueous solution was characterized by the measurement of critical micelle concentration (CMC). The CMC of P123-DTX conjugate was (1.34 +/- 0.05) x 10(-5) mol/L, which was lower than that of P123 ((1.91 +/- 0.07) x 10(-5) mol/L). The DTX content in the conjugate could reach 13.69% (wt.%). TEM and DLS analysis showed that the conjugate formed approximately spherical micelles with mean particle size of 85.3 +/- 1.59 nm. In vitro release of DTX from the conjugate micelles showed pH dependence, being faster at lower pH value than that at pH 7.4. In vitro cytotoxicity of P123-DTX conjugate micelles was evaluated by MTT method against HepG2, MCF-7 and B16 cell lines and the result indicated that P123-DTX conjugate micelles showed lower cytotoxicity than the DTX injection-Duopafei. Compared with Duopafei, in vivo antitumor activity of P123-DTX conjugate micelles in Kunming mice bearing B16 tumor was more effective and less toxic. These results indicated that the P123-DTX conjugate micelles prepared in this study may be considered as an alternative and promising DTX delivery system.
- Subjects :
- Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacokinetics
Cell Line, Tumor
Docetaxel
Female
Hep G2 Cells
Humans
Mice
Nanoconjugates chemistry
Taxoids pharmacokinetics
Antineoplastic Agents administration & dosage
Drug Carriers chemistry
Micelles
Poloxalene chemistry
Taxoids administration & dosage
Subjects
Details
- Language :
- English
- ISSN :
- 1550-7033
- Volume :
- 9
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Journal of biomedical nanotechnology
- Publication Type :
- Academic Journal
- Accession number :
- 24266256
- Full Text :
- https://doi.org/10.1166/jbn.2013.1706