Synthesis, characterization and Antifibrinolytic activity of Carboxylated Polyvinylpyrrolidone conjugation with Tranexamic acid
DOI:
https://doi.org/10.5281/zenodo.10270753Keywords:
Biologically Active Components, Polymer Conjugation, Vitro Clot LysisAbstract
Polymer conjugation with biologically active components has become a very attractive system as it could improve the efficacy of some drugs. this study aimed to prepare and formulate a topical polymer conjugate with a biologically active component for the treatment of bleeding using tranexamic acid as a drug model. this polymer conjugate leads to the release of the drug in a sustained manner in order to prolong the contact time of the drug with broken skin for the best antifibrinolytic activity. The polymeric matrix involved carboxylated Polyvinylpyrrolidone. Therefore, carboxylated polyvinylpyrrolidone was modified by amide bonding with tranexamic acid (P1), complexing of the resultant product with iodine (P2), synthesis of ether tranexamic acid (P3), synthesis of methylol tranexamic acid (P4), and esterification of methylol tranexamic acid (P5). These polymers were modified to improve their properties and to control the drug release. The FTIR and DSC spectroscopies and 1HNMR spectroscopies were used to determine the drug content of these derivatives. Thus, we aimed to study the antifibrinolytic activity of all compounds (P1–P5) evaluated at various concentrations using in vitro clot lysis assays in human plasma. When employed in high doses, the antifibrinolytic activity of compound P5 exhibits a higher level of antifibrinolytic activity compared to that of pure tranexamic acid.
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