Synthesis and characterization of microparticles made of carboxymethyloxysuccinic-acid-modified PLA-PEG co-polymer

Haiyue Zhang Research Institute of Polymeric Materials, Tianjin University, Tianjin 300072, P. R. China

Li Chang Department of Polymer Science and Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China

Bin Zhang Department of Polymer Science and Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China

Peng Li Department of Polymer Science and Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China

Min Wang Department of Polymer Science and Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China

Kang De Yao Research Institute of Polymeric Materials, Tianjin University, Tianjin 300072, P. R. China

Jun Yang Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, P. R. China

Fanglian Yao Department of Polymer Science and Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China

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Abstract

A novel tri-block co-polymer, HO₂C-PLA-PEG-PLA-CO₂H (co-polymer II), with polybasic carboxylic acids as the end-groups was synthesized and characterized by IR and ¹H-NMR. Based on the successful synthesis of co-polymer II, water-soluble sodium salicylate and oil-soluble tetrandrine, used as model drugs, were loaded in the co-polymer microparticles prepared through a modified multiple emulsion method. The encapsulation efficiency and drug-releasing behaviour were also investigated. It is found that the microparticles of about 10 μm in size are porous and can be produced from co-polymer II in better encapsulation efficiency (up to 86.65% and 55.94%) compared to those made from PLA/PEG/PLA (co-polymer I) (77.50% and 44.01%). The drug-release behaviour of co-polymer II exhibits an extended continuous release behaviour and the initial burst was reduced obviously. The results show that such functionalised PLA/PEG/PLA carrier provides higher drug encapsulation efficiency and better profiles.

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Synthesis and characterization of microparticles made of carboxymethyloxysuccinic-acid-modified PLA-PEG co-polymer

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Synthesis and characterization of microparticles made of carboxymethyloxysuccinic-acid-modified PLA-PEG co-polymer

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