Enhancing the furosemide permeability by papain minitablets through a triple co-culture in vitro intestinal cell model
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2020
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AAPS PharmSciTech
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The administration of medicines by the oral route is the most used approach for
being very convenient. Although it is the most popular, this route also has absorption, and
consequently, bioavailability limitations. In this sense, several pharmacotechnical strategies
have been used to improve drug absorption, one of which is the use of permeation
promoters. Papain is a very versatile plant enzyme that can be used as a permeation
promoter of various active compounds. This study aimed to evaluate the safety of papain and
the formulation of native papain minitablets to promote in vitro permeation of furosemide
through an innovative biomimetic triple co-culture model of Caco-2, HT29-MTX, and Raji
cells. Regarding permeation, furosemide and metaprolol concentrations are determined with
HPLC; those are used to calculate Papp. Monolayer integrity was evaluated using TEER and
Lucifer Yellow. In the presence of papain, TEER decreased two-fold and the Papp of
furosemide increased six-fold. The results suggest that native papain minitablets can be used
as therapeutic adjuvants to enhance the permeation of drugs significantly improving
bioavailability.
Como referenciar
CORAZZA, FULVIO G.; ERNESTO, JULIA V.; NAMBU, FELIPE A.N.; CALIXTO, LEANDRO A.; VARCA, GUSTAVO H.C.; VIEIRA, DANIEL P.; LEITE-SILVA, VANIA R.; ANDREO-FILHO, NEWTON; LOPES, PATRICIA S. Enhancing the furosemide permeability by papain minitablets through a triple co-culture in vitro intestinal cell model. AAPS PharmSciTech, v. 21, n. 7, p. 1-10, 2020. DOI: 10.1208/s12249-020-01796-9. Disponível em: http://200.136.52.105/handle/123456789/31584. Acesso em: 19 Apr 2024.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.