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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Papain-cyclodextrin complexes as an intestinal permeation enhancer: Permeability and in vitro safety evaluation

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Author(s):
Corazza, Fulvio G. [1] ; Ernesto, V, Julia ; Nambu, Felipe A. N. [2] ; de Carvalho, Luma R. [3] ; Leite-Silva, Vania R. [2] ; Varca, Gustavo H. C. [3] ; Calixto, Leandro A. [2] ; Vieira, Daniel P. [3] ; Andreo-Filho, Newton [2] ; Lopes, Patricia S. [2]
Total Authors: 10
Affiliation:
[1] Univ Fed Sao Paulo UNIFESP, Inst Ciencias Ambientais Quim & Farmaceut, Dept Ciencias Farmaceut, Campus Diadema, Rua Sao Nicolau 210, BR-09913030 Sao Paulo, SP - Brazil
[2] Ernesto, Julia, V, Univ Fed Sao Paulo UNIFESP, Inst Ciencias Ambientais Quim & Farmaceut, Dept Ciencias Farmaceut, Campus Diadema, Rua Sao Nicolau 210, BR-09913030 Sao Paulo, SP - Brazil
[3] Inst Pesquisas Energet & Nucl IPEN CNEN SP, Ave Prof Lineu Prestes 2242, Cidade Univ, BR-05508000 Sao Paulo, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY; v. 55, FEB 2020.
Web of Science Citations: 0
Abstract

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. Papain-cyclodextrins complexes did not show any cytotoxicity above 31 mu g/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. (AU)

FAPESP's process: 15/19212-3 - Papain permeability evaluation in oral pharmaceuticals formulations for treatment of intestinal diseases triple co-culture of Caco-2, HT29-MTX and Raji cells as in vitro model
Grantee:Fúlvio Gabriel Corazza
Support Opportunities: Scholarships in Brazil - Master
FAPESP's process: 10/10935-9 - Development of a nanostructured hydrogel containing a papain and cyclodextrin complex
Grantee:Gustavo Henrique Costa Varca
Support Opportunities: Scholarships in Brazil - Doctorate (Direct)
FAPESP's process: 16/22916-5 - Development of minitablets loading papain free and complexed with cyclodextrins and sodium alginate for delivery in small intestine and colon
Grantee:Newton Andréo Filho
Support Opportunities: Regular Research Grants
FAPESP's process: 15/19213-0 - Papain oral products for intestinal treatment evaluation using triple co-culture of Caco-2, HT29-MTX and Raji cells as an in vitro model
Grantee:Patricia Santos Lopes
Support Opportunities: Regular Research Grants