Jm. Schierholz et al., NEW ANTIINFECTIOUS BIOMATERIALS - CIPROFLOXACIN CONTAINING POLYURETHANES AS POTENTIAL-DRUG DELIVERY SYSTEMS TO PREVENT FOREIGN-BODY INFECTIONS, Arzneimittel-Forschung, 47(1), 1997, pp. 70-74
Device related infections are an increasing problem since foreign mate
rials are used in modern medicine; Ciprofloxacin-HCl salt (CAS 86393;3
2-0) and lipophilic ciprofloxacin-betaine (Bay o 9867) incorporated in
to polyurethanes by solvent casting technique were studied in order to
develop antiinfectious properties of this biomaterial. Drug release r
ates, bacterial colonization and morphological features of the polymer
-ciprofloxacin combinations were studied and the physico-chemical mech
anisms of the delivery were discussed. Ciprofloxacin salt showed a fas
t initial release rare, whereas ciprofloxacin-betaine was characterize
d by a more continuous release behaviour. A higher diffusity of the li
pophilic ciprofloxacin-betaine in the polymer could be shown as compar
ed to its salt incorporated into the polyurethane. The high initial bu
rst effect of the hydrochloride antibiotic was caused by its high solu
bility in the elution medium. Bacterial colonization tb the antibiotic
-loaded polyurethanes was inhibited effectively only by preparations s
howing a slower but more sustained drug release. Scanning electron mic
roscopy (SEM) demonstrated that the polyurethane-antibiotic combinatio
n was most homogenous for ciprofloxacin-betaine. Polyurethane material
loaded with ciprofloxacin salt showed crystals at the surface and a g
ranular structure of the polymeric matrix. Crystalline structure of th
e drug on polymeric surfaces varied with loading concentration and lip
ophilicity. Physico-chemical similarity of the polymeric material and
the antibiotics is important for the homogeneity of the polymer-antibi
otic combinations. High homogeneity is required for a sustained and pr
olonged release and effective inhibition of bacterial colonization.