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Drug release from complexes with a series of poly(carboxyalkyl methacrylates), a new class of weak polyelectrolytes
Jose M Cornejo-Bravo1, Maria E Flores-Guillen, Eder Lugo-Medina
1Facultad de Ciencias Químicas e Ingeniería, Universidad Autónoma de Baja California, PMB 121, 2498 Roll Dr, San Diego, CA 92154, USA. jmcornejo@uabc.mx
Abstract:
Carboxyalkyl methacrylates, a new class of non-cross-linked, hydrophobic weak polyelectrolytes, were synthesized, and then bound to cationic drugs (propranolol.HCl, diltiazem.HCl and verapamil.HCl) to form water-insoluble complexes that release the bound drug only in ionic media (pH 7.4). Compressed tablets were prepared from these cation exchange polyelectrolytes. Release profiles followed zero order kinetics (n>0.90; n is the release exponent). As the hydrophobicity of the polyelectrolytes increased, the rate of release decreased and deviated from linearity (n=0.7). Both the ionic strength of the medium as well as the solubility of the drug affected the rate of release. In acidic media (pH 1.2) a burst of drug was released but the release was halted by a layer of non-ionized polymer precipitated on the surface of the tablets. The results indicate that it is possible to "tailor-make" the release kinetics by using a polyelectrolyte from the series with the suitable hydrophobicity.
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