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

Citation
G. Giammona et al., A NEW WATER-SOLUBLE SYNTHETIC-POLYMER, ALPHA,BETA-POLYASPARTHYDRAZIDE, AS POTENTIAL PLASMA EXPANDER AND DRUG CARRIER, Journal of controlled release, 29(1-2), 1994, pp. 63-72
Citations number
37
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
ISSN journal
01683659
Volume
29
Issue
1-2
Year of publication
1994
Pages
63 - 72
Database
ISI
SICI code
0168-3659(1994)29:1-2<63:ANWSA>2.0.ZU;2-1
Abstract
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 p lasma substitute. Acute toxicity studies revealed no death in the anim als treated, and subacute toxicity studies recorded no notable differe nce between treated and control animals either in terms of body-weight or the principle haematological parameters. Haemodynamic studies like wise established no significant variation in systolic and diastolic pr essure or in heart beat between the two groups. Solutions of PAHy admi nistered 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 p otential 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) carbodi imide 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).