Evaluation of different covalent crosslinking agents into valsartan-loaded sericin and alginate particles for modified release
2021
Santinon, Caroline | Borges, Danielle | da Silva, Meuris Gurgel Carlos | Vieira, Melissa Gurgel Adeodato
Valsartan is a drug indicated for hypertension and heart failure treatment, being administered for many years by the patient. Its release modification by incorporation into a polymeric blend, such as sericin and alginate, brings benefits as the marked decrease in side effects and the possibility of decreasing the dose administration frequency. Four covalent crosslinking agents were tested in the incorporation stage, in order to optimize the formulation. Proanthocyanidin was the most promising crosslinker and its concentration was varied to assess the influence on drug diffusion. A 2% (w/V) content promoted 40% of incorporation efficiency increase. The in vitro dissolution exhibited a prolonged profile and the drug loading was closer to the theoretical calculated than the formulation without crosslinking agent. Proanthocyanidin promoted the non-interaction of the particles with the gelatinous capsule and ensured the stability of valsartan. Particles characterizations confirmed the effective drug incorporation and a thermal behavior improvement.
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