Papain-cyclodextrin complexes as an intestinal permeation enhancer
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Journal of Drug Delivery Science and Technology
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Oral drug delivery is the main route for drugs administration. However, some drugs have poor permeability
across the intestinal barrier. Papain has been widely used in pharmaceutical applications due to its debridement
properties and the ability to promote skin permeation of drugs. It is known that papain complexation with
cyclodextrins improves its biological stability. In this paper, the ability of the native papain-cyclodextrin complexes
is shown be an oral permeation enhancer to furosemide, using a Caco-2 monolayer system to evaluate
drug permeability and apparent permeability coefficient. Analysis of the in vitro cytotoxicity over CHO–K1, Hep
G2 and Caco-2 cell lines and genotoxicity over CHO–K1 and Hep G2 cell lines were also performed. Papaincyclodextrins
complexes did not show any cytotoxicity above 31 μg/mL. No significant genotoxic damage was
observed. Papain and cyclodextrin complexes induced almost 2.5-fold increase in furosemide permeation
compared to controls, and maintenance of the paracellular integrity of the Caco-2 cells monolayer was confirmed.
The papain complexes may be safely applied in pharmaceutical formulations, not only as a therapeutic
agent but also as a strategic pharmaceutical adjuvant, promoting permeation of low oral permeability drugs.
Como referenciar
CORAZZA, FULVIO G.; ERNESTO, JULIA V.; NAMBU, FELIPE A.N.; CARVALHO, LUMA R. de; LEITE-SILVA, VANIA R.; VARCA, GUSTAVO H.C.; CALIXTO, LEANDRO A.; VIEIRA, DANIEL P.; ANDREO-FILHO, NEWTON; LOPES, PATRICIA S. Papain-cyclodextrin complexes as an intestinal permeation enhancer: permeability and in vitro safety evaluation. Journal of Drug Delivery Science and Technology, v. 55, p. 1-11, 2020. DOI: 10.1016/j.jddst.2019.101413. Disponível em: http://repositorio.ipen.br/handle/123456789/31106. Acesso em: 30 Dec 2025.
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.