The present study aimed at proposing a safe drug delivery system comprising of chitosan, as a natural polymer, and cyanocobalamin (Cbl) in compliance with the biological system to improve oral administration of ticagrelor (TCG). To this end, the drug loading, in‐vitro drug release, and in‐vitro cytotoxicity were assessed after fabricating the drug‐loaded carrier. Drug transfer could be improved due to the inherent features of mucoadhesive chitosan and the existence of a specific receptor for Cbl in the intestine. Given the results, a maximum drug loading efficiency of 80 % was obtained for TCG, and a controlled release profile was achieved for the drug‐loaded carrier in 0.2 % w/v polysorbate 80 in water. Biocompatibility studies of the TCG‐loaded carrier showed similar cytotoxicity compared to the free drug. The proposed safe drug delivery system has the potentials to overcome the constraints that might preclude the use of the TCG formulation in oral dosage forms.
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