Tri-component diblock copolymers of poly(ethylene glycol)–poly(ε-caprolactone-co-lactide): synthesis, characterization and loading camptothecin

Springer Science and Business Media LLC - Tập 283 - Trang 1246-1252 - 2005
Yan Zhang1,2, Changchun Wang1, Wuli Yang1, Bin Shi3, Shoukuan Fu1
1Department of Macromolecular Science of Fudan University and the Key Laboratory of Molecular Engineering of Polymers, Ministry of Education, Shanghai, China
2Modern Experiment Technology Center, Anhui University, Hefei, China
3 School of Pharmacy of Fudan University, Shanghai, China

Tóm tắt

Biodegradable tri-component diblock copolymer was synthesized by bulk copolymerization of ε-caprolactone (CL) and D, L-lactide (LA) in the presence of methoxy poly(ethylene glycol) (MePEG), using stannous octoate as catalyst. Their chemical structure and physical properties were investigated by GPC, NMR, DSC, TGAand XRD. The increase of CL/LA ratio in the diblock copolymer leads to lower T g, higher decomposition temperature and crystallinity. Nanoparticles formulated from MePEG–poly(CL-co-LA) (PCAE) possess spherical structure, which was characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The DLS results indicate that the particle size increased with the increase of CL/LA ratio and the hydrophobic fragment length in the copolymer. The drug encapsulation efficiency and the drug release behavior in vitro conditions of camptothecin were measured by high performance liquid chromatography (HPLC). The encapsulation efficiency can be achieved as high as 84.4% and the release behavior can be made well-controlled. MePEG–poly(CL-co-LA) nanoparticles might have a great potential as carriers for hydrophobic drugs.

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