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Preparation and in vitro evaluation of novel poly(anhydride-ester)-based amphiphilic copolymer curcumin-loaded micelles.
- Source :
-
Journal of biomedical nanotechnology [J Biomed Nanotechnol] 2014 Feb; Vol. 10 (2), pp. 324-35. - Publication Year :
- 2014
-
Abstract
- Novel poly(anhydride-ester)-b-poly(ethylene glycol) copolymers (PAE-b-PEGs) were synthesized by esterization of methyl poly(ethylene glycol) and poly(anhydride-ester), which were obtained by the melt polycondensation of alpha,omega-acetic anhydride-terminated poly(L-lactic acid), and characterized by 1H-NMR and gel permeation chromatography. The two poly(anhydride-ester)-b-poly(ethylene glycols) (denoted as PAE-b-PEG2k and PAE-b-PEG5k) thus obtained can self-assemble in water to form micelles with hydrodynamic diameters of 92.5 and 97.5 nm above their critical micelle concentrations of 3.78 and 2.36 microg/mL, respectively. The curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles were prepared by the solid dispersion method, and they could encapsulate approximately 7% (w/w) curcumin. The diameters of the micelles were stable for 5 days. Curcumin is released faster from the micelles at pH 5.0 than at pH 7.4. Curcumin is released from the micelles at a fast rate during the initial 12 h, followed by a zero-order release during the subsequent 200 h, both at pH 5.0 and 7.4. The IC50 values of the curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles against HeLa cells are 12.41 and 15.31 microg/mL, respectively, which is lower than that of free curcumin (25.90 microg/mL). The PAE-b-PEG2k micelles are taken up faster than the PAE-b-PEG5k micelles by HeLa cells. Curcumin-loaded micelles can induce G2/M phase cell cycle arrest and apoptosis of HeLa cells.
- Subjects :
- Animals
Cell Cycle drug effects
Cell Death drug effects
Endocytosis drug effects
Esters chemistry
HeLa Cells
Hemolysis drug effects
Humans
Hydrodynamics
Kinetics
Lactic Acid chemical synthesis
Lactic Acid chemistry
Magnetic Resonance Spectroscopy
Microscopy, Electron, Transmission
Polyanhydrides chemistry
Polyesters
Polyethylene Glycols chemical synthesis
Polyethylene Glycols chemistry
Polymers chemical synthesis
Polymers chemistry
Rats
Rats, Sprague-Dawley
Spectrometry, Fluorescence
Surface-Active Agents chemistry
X-Ray Diffraction
Curcumin pharmacology
Esters chemical synthesis
Micelles
Polyanhydrides chemical synthesis
Surface-Active Agents chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1550-7033
- Volume :
- 10
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of biomedical nanotechnology
- Publication Type :
- Academic Journal
- Accession number :
- 24738340
- Full Text :
- https://doi.org/10.1166/jbn.2014.1789