ABSTRACT
Polymeric films with enhanced mechanical performance were fabricated by incorporation of bone ash (BA) at various concentrations (0-25 v. %) into chitosan/gelatin (CTS/GEL) polymeric structure as a wound healing-dressing. The test results for mechanical performance of polymeric films proved that the encapsulation of BA into the polymeric films enhances the elastic modulus and tensile strength of polymeric films significantly. Oxygen permeability and water vapor transmission rate (WVTR) of films were also improved by BA reinforcement. Ciprofloxacin was chosen as the antibacterial model drug. The release of ciprofloxacin was provided in a more controlled manner at pH 7.4 owing to the incorporation of bone ash into the polymeric films. Also, drug loaded films showed great antibacterial activity against Escherichia coli and Bacillus subtilis bacteria. The results prove that ciprofloxacin loaded BA reinforced CTS/GEL composite films are potentially applicable in controlled drug delivery as wound dressings.
Subject(s)
Anti-Bacterial Agents/pharmacology , Bandages , Chitosan/chemistry , Ciprofloxacin/pharmacology , Gelatin/chemistry , Minerals/chemistry , Animals , Bacillus subtilis/drug effects , Cell Line , Chitosan/toxicity , Drug Liberation , Elastic Modulus , Escherichia coli/drug effects , Gelatin/toxicity , Mice , Microbial Sensitivity Tests , Minerals/toxicity , Oxygen/chemistry , Permeability , Tensile StrengthABSTRACT
A new series of flavonyl-2,4-thiazolidinediones (Va-c, VIa-c) was prepared by Knoevenagel reaction. The synthesized compounds were tested for their ability to inhibit rat kidney aldose reductase (AR) and for their insulinotropic activities in INS-1 cells. Compound Vb was able to increase insulin release in the presence of 5.6mmol/l glucose. Compounds VIa-c displayed moderate to high AR inhibitory activity levels. Particularly, compound VIa showed the highest AR inhibitory activity (86.57%).
Subject(s)
Hypoglycemic Agents/chemistry , Thiazolidinediones/chemistry , Thiazolidinediones/pharmacology , Aldehyde Reductase/antagonists & inhibitors , Animals , Cell Line , Glucose/pharmacology , Humans , Hypoglycemic Agents/pharmacology , Insulin/metabolism , Insulin Secretion , Kidney/enzymology , Male , Mice , RatsABSTRACT
As it is known that still, there were no any confident ARIs on the market and they have several side effects, we need to approve new ARIs to reduce diabetic complications especially which have effect on the cataract formation. In this study, a new series of chromonyl-2,4-thiazolidinediones (Ia-e, IIa-e, IIIa-e) were prepared by Knoevenagel reaction with substituted 3-formylchromones (3a-e) and unsubstituted (1) or substituted 2,4-thiazolidinedione (2). The synthesized compounds were tested for their ability to inhibit rat kidney AR by an in vitro spectrophotometric assay. Compound IIIe showed the highest inhibitory activity (82.43+/-0.76%). Compounds Ia-e and IIIa-d also showed significant inhibitory activity (42.40+/-5.78, 52.71+/-3.31, 49.69+/-1.55, 50.80+/-3.62, 46.70+/-2.33, 49.44+/-4.53, 61.17+/-4.74, 68.58+/-2.05, 77.28+/-0.26%, respectively).
