A NEW WATER-SOLUBLE SYNTHETIC-POLYMER, ALPHA,BETA-POLYASPARTHYDRAZIDE, AS POTENTIAL PLASMA EXPANDER AND DRUG CARRIER

被引:51
作者
GIAMMONA, G [1 ]
CARLISI, B [1 ]
CAVALLARO, G [1 ]
PITARRESI, G [1 ]
SPAMPINATO, S [1 ]
机构
[1] UNIV BOLOGNA,INST FARMACOL,BOLOGNA,ITALY
关键词
POLYASPARTHYDRAZIDE; PLASMA EXPANDER; DRUG CARRIER; OFLOXACIN; POLYMERIC PRODRUG;
D O I
10.1016/0168-3659(94)90122-8
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The reaction between a polysuccinimide (PSI) and hydrazine produces a water-soluble polymer alpha,beta-polyasparthydrazide (PAHy). Tests of the polymer on laboratory animals established its potential use as a plasma substitute. Acute toxicity studies revealed no death in the animals treated, and subacute toxicity studies recorded no notable difference between treated and control animals either in terms of body-weight or the principle haematological parameters. Haemodynamic studies likewise established no significant variation in systolic and diastolic pressure or in heart beat between the two groups. Solutions of PAHy administered to bled animals improved the lowering of blood values caused by the bleeding. Moreover, PAHy was not capable of inducing any immune response when administered intradermally to laboratory animals. The potential use of PAHy as a drug carrier was also investigated. PAHy was bonded with a model drug, the antibacterial Ofloxacin, by means of a water-soluble carbodiimide, N-ethyl-N'-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC). The resulting conjugate, PAHy-Ofloxacin is, like the polymeric carrier, water-soluble and contains a quantity of linked drug equivalent to 9% (w/w).
引用
收藏
页码:63 / 72
页数:10
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