The effect of conjugation on different polymers in bioadhesive films of losartan


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3

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1

Abstract :

The objective of the present study was to develop mucoadhesive buccal films of losartan potassium using sodium alginate, chitosan, and their conjugated derivatives at different concentrations by solvent casting technique. Glycerin was used as plasticizer, at different weight ratios. The conjugation of polymers (sodium alginate-cysteine and chitosan-thioglycolic acid) was confirmed by FTIR study. The resulted conjugated sodium alginate and chitosan displayed 475.64±24.31 and 305±31.21 μmol thiol groups per g conjugate, respectively. The developed films were evaluated by different parameters such as weight uniformity, thickness, surface pH, swelling index, in vitro residence time, mucoadhesive strength, in vitro and ex vivo drug permeation. The results indicated that the formulations S5, C4, Cs and Cc showed better characteristic properties and drug permeation. Good results were obtained both in vitro and ex vivo conditions for optimized film. A higher glycerin percent in films increased the drug permeation, particularly at a polymer concentration of 10 to 30% w/v (S2-S4 and C2-C4). A further increase of glycerin (40 to 50% w/v) did not improve losartan potassium permeation (S6 and C6). Formulations Cs and Cc containing conjugated sodium alginate and chitosan resulted in a significantly higher bioadhesion, swelling with better drug permeation over long period than films comprising unmodified polymers. Stability studies on optimized formulations indicated that the formulations are stable as no significant difference was observed in either drug content or drug release.
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