Synthesis and characterisation of poly(D,L-lactic acid) idoxuridine conjugate

被引：27

作者：

Rimoli, MG

Avallone, L

de Caprariis, P

Galeone, A

Forni, F

Vandelli, MA

机构：

[1] Univ Naples Federico II, Fac Farm, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy

[2] Univ Sassari, Fac Farm, Ist Analit Farmaceut, I-07100 Sassari, Italy

[3] Univ Naples Federico II, Fac Farm, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy

[4] Univ Modena, Fac Farm, Dipartimento Sci Farmaceut, I-41100 Modena, Italy

来源：

JOURNAL OF CONTROLLED RELEASE | 1999年 / 58卷 / 01期

关键词：

idoxuridine; poly(D; L-lactic acid); polymeric prodrug; chemical hydrolysis; enzymatic degradation;

D O I：

10.1016/S0168-3659(98)00129-1

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A new polymeric prodrug was prepared coupling 5-iodo-2'-deoxyuridine (IDU) to poly(D,L-lactic acid) (PLA) via a succinic acid spacer. The PLA-IDU conjugate was characterised by thermal analysis, IR and H-1 and C-13 NMR spectroscopy. The IDU content (0.024 mequiv. g(-1) of PLA) was consistent with the carboxylic acid endgroup present in the polymer sample (0.025 mequiv. g(-1) of polymer). The PLA-IDU conjugate was susceptible to degradation in biological environments containing esterase, whereas IDU was not detected by chemical hydrolysis in pH 7.4 phosphate buffer. The conjugate should be used to prepare injectable microspheres and nanospheres containing IDU chemically coupled to the polymer carrier. (C) 1999 Elsevier Science B.V. All rights reserved.

引用

页码：61 / 68

页数：8

共 12 条

[1] CHARACTERIZATION OF DRUG-LOADED POLY(D,L-LACTIDE) MICROSPHERES [J].