Pluronic F127 as a suitable carrier for preparing the imatinib base solid dispersions and its potential in development of a modified release dosage forms

摘要

AbstractIn recent years, considerable attention focuses on making sustained release dosage forms also containing solid dispersions. The objective of this study is evaluation of imatinib base (IMA) solid dispersion physicochemical properties which can be useful to controlled release solid dosage formation. The solid dispersions were obtained by kneading method, containing of 10–90% w/w Pluronic F127 (PLU). Drug dissolution test was determined by rotating-disc system method in 0.1?M hydrochloric acid (pH 1.2) and phosphate buffer (pH 6.8). XRD, DSC, FTIR, and SEM observations were performed to evaluate the physical characteristics of solid dispersions. These studies showed that there was no chemical interaction of the IMA with PLU in the solid state and revealed that IMA and PLU form a simple eutectic phase diagram. Our research has shown that the dynamics of the release of imatinib base from solid dispersions with Pluronic F127 depends on the pH of dissolution medium. At pH 1.2, the presence of polymer in solid dispersion causes delaying of drug release due to formation a viscous gel layer, whereas at pH 6.8 significant enhancement of the drug dissolution rate from solid dispersions has been observed compared to pure IMA. The highest improvement was observed in solid dispersions containing 20 and 30% w/w polymer. The present investigation confirmed that the hydrophilic polymer Pluronic F127 could be applied as a suitable matrix to design modified release formulations of imatinib base.