Comparison between the binding of chlorpheniramine maleate to poly(sodium 4-styrenesulfonate) and the binding to other polyelectrolytes

• Published in: Polymer (Guilford) 2005-08, Vol.46 (18), p.7240-7245
• Main Authors: Moreno-Villoslada, Ignacio, Oyarzún, Felipe, Miranda, Víctor, Hess, Susan, Rivas, Bernabé L.
• Format: Article
• Language: English
• Subjects: Applied sciences; Biological and medical sciences; Chlorpheniramine maleate; Exact sciences and technology; General pharmacology; Medical sciences; Organic polymers; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Physicochemistry of polymers; Properties and characterization; Solution and gel properties; Ultrafiltration-diafiltration; Water-soluble polymers
• ISSN: 0032-3861; 1873-2291
• DOI: 10.1016/j.polymer.2005.06.033

The interactions of the antihistaminic drug chlorpheniramine maleate (CPM) with the negatively charged polyelectrolytes poly(sodium 4-styrenesulfonate) (PSS) and poly(acrylic acid) (PAA) are studied by the washing method of the diafiltration technique at conditions simulating those of the small intestine such as pH 7.5 and 0.13 M NaCl. The results are compared with those already reported involving other pharmacologically important polyelectrolytes such as alginic acid (ALG), carboxymethylcellulose (CMC), and κ- and ι-carrageenan (κ- and ι-CAR). As in the case of ALG, CMC, and CAR, interactions of CPM with PAA appear to be electrostatic and are cleaved in the presence of 0.13 M NaCl. On the contrary, apart from electrostatic interactions, additional interactions are found with PSS and residual interactions are kept in the presence of 0.13 M NaCl, a fact that may be attributed to π–π interactions and hydrophobic forces. The effect of the addition of 4 M urea, branched poly(ethyleneimine) (BPEI), and poly(vinylpyrrolidone) (PVP) is also studied. The addition of urea 4 M or 0.001 M BPEI produces a decrease on the amounts of counterions bound to PSS at infinite elution, while the addition of PVP does not produce any change on the diafiltration profiles.