Enhancing the Furosemide Permeability by Papain Minitablets Through a Triple Co-culture In Vitro Intestinal Cell Model
| Autor: | Felipe A. N. Nambu, Newton Andréo-Filho, Gustavo H.C. Varca, Patricia Santos Lopes, Leandro Augusto Calixto, Daniel Perez Vieira, Vânia Rodrigues Leite-Silva, Julia V. Ernesto, Fulvio G. Corazza |
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| Rok vydání: | 2020 |
| Předmět: |
Absorption (pharmacology)
Pharmaceutical Science Biological Availability 02 engineering and technology Aquatic Science In Vitro Techniques 030226 pharmacology & pharmacy Permeability 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Furosemide Drug Discovery Papain medicine Humans Intestinal Mucosa Diuretics Ecology Evolution Behavior and Systematics Lucifer yellow Chromatography Ecology General Medicine Permeation 021001 nanoscience & nanotechnology In vitro Coculture Techniques Bioavailability Intestinal cell chemistry Intestinal Absorption Caco-2 Cells 0210 nano-technology Agronomy and Crop Science HT29 Cells medicine.drug Tablets |
| Zdroj: | AAPS PharmSciTech. 21(7) |
| ISSN: | 1530-9932 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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