聚酯和聚（酯-碳酸酯）-紫杉醇缀合物的制备与表征

Preparation and characterization of polyester- and poly(ester-carbonate)-paclitaxel conjugates.

作者信息

Sobczak Marcin, Korzeniowska Agnieszka, Goś Piotr, Kolodziejski Waclaw L

机构信息

Medical University of Warsaw, Faculty of Pharmacy, Department of Inorganic and Analytical Chemistry, ul. Banacha 1, 02-097 Warsaw, Poland.

出版信息

Eur J Med Chem. 2011 Jul;46(7):3047-51. doi: 10.1016/j.ejmech.2011.04.046. Epub 2011 Apr 22.

DOI:10.1016/j.ejmech.2011.04.046

PMID:21555165

Abstract

The polyester- and poly(ester-carbonate)-paclitaxel conjugates with low molecular weight were synthesized using dicyclohexylcarbodiimide (DCC) and dimethylaminopyridine (DMAP) as catalysts. Polymeric matrices were obtained by ring-opening polymerization of ɛ-caprolactone (CL), rac-lactide (rac-LA), l-lactide (LLA) and trimethylene carbonate (TMC). The macromolecular conjugates were characterized by using spectroscopic techniques, such as (1)H, (13)C NMR and FTIR. The degree of degradation of polyester- and poly(ester-carbonate)-paclitaxel conjugates was tested in vitro under different conditions. The preliminary results of drug release were discussed.

摘要

以二环己基碳二亚胺（DCC）和二甲基氨基吡啶（DMAP）作为催化剂，合成了低分子量的聚酯-紫杉醇和聚（酯-碳酸酯）-紫杉醇共轭物。通过ε-己内酯（CL）、外消旋丙交酯（rac-LA）、左旋丙交酯（LLA）和碳酸三亚甲酯（TMC）的开环聚合反应制备了聚合物基质。利用诸如¹H、¹³C NMR和FTIR等光谱技术对大分子共轭物进行了表征。在不同条件下体外测试了聚酯-紫杉醇和聚（酯-碳酸酯）-紫杉醇共轭物的降解程度，并对药物释放的初步结果进行了讨论。