Evaluation of different covalent crosslinking agents into valsartan-loaded sericin and alginate particles for modified release

Author(s)

Santinon, Caroline ^[1] ; Borges, Daniele ^[1] ; Carlos da Silva, Meuris Gurgel ^[1] ; Adeodato Vieira, Melissa Gurgel ^[1]

Affiliation

^[1] Univ Campinas UNICAMP, Dept Proc & Prod Design, Sch Chem Engn, Albert Einstein Ave 500, BR-13083852 Campinas, SP - Brazil

• Document type: Journal article
• Source: Powder Technology; v. 390, p. 240-255, SEP 2021.
• Web of Science Citations: 0

Abstract

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. (c) 2021 Elsevier B.V. All rights reserved. (AU)

• FAPESP's process: 16/05007-1 - Removal of residual drug in aqueous solution by alternative adsorbents
• Grantee: Meuris Gurgel Carlos da Silva
• Support Opportunities: Regular Research Grants
• FAPESP's process: 15/13505-9 - INCORPORATION AND RELEASE OF DRUGS BY SERICIN-ALGINATE MICROPARTICLES
• Grantee: Melissa Gurgel Adeodato Vieira
• Support Opportunities: Regular Research Grants