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Delivery of a hydrophobic drug into the lower gastrointestinal system via an endogenous enzyme-mediated carrier mechanism: An in vitro study.
Bannigan, Pauric; Durack, Edel; Mathur, Harsh; Rea, Mary C; Ross, R Paul; Hudson, Sarah P.
Afiliación
  • Bannigan P; Department of Chemical Sciences, Synthesis and Solid State Pharmaceutical Centre, Bernal Institute, University of Limerick, Ireland. Electronic address: pauric.bannigan@ul.ie.
  • Durack E; Department of Chemical Sciences, Synthesis and Solid State Pharmaceutical Centre, Bernal Institute, University of Limerick, Ireland. Electronic address: edel.durack@ul.ie.
  • Mathur H; Teagasc Food Research Centre, Moorepark, Fermoy, Co. Cork, Ireland; APC Microbiome Ireland, University College Cork, Ireland. Electronic address: Harsh.Mathur@teagasc.ie.
  • Rea MC; Teagasc Food Research Centre, Moorepark, Fermoy, Co. Cork, Ireland; APC Microbiome Ireland, University College Cork, Ireland. Electronic address: Mary.Rea@teagasc.ie.
  • Ross RP; Teagasc Food Research Centre, Moorepark, Fermoy, Co. Cork, Ireland; APC Microbiome Ireland, University College Cork, Ireland; College of Science, Engineering and Food Science, University College Cork, Ireland. Electronic address: p.ross@ucc.ie.
  • Hudson SP; Department of Chemical Sciences, Synthesis and Solid State Pharmaceutical Centre, Bernal Institute, University of Limerick, Ireland. Electronic address: sarah.hudson@ul.ie.
Eur J Pharm Biopharm ; 133: 12-19, 2018 Dec.
Article en En | MEDLINE | ID: mdl-30267836
Clofazimine (CFZ) is a hydrophobic antibiotic agent which exhibits poor solubility. This poor solubility was overcome herein by the formulation of CFZ with the digestive enzyme pepsin. It is shown that pepsin can actively bind 11 CFZ molecules in the protein's native gastric environment, forming a CFZ-pepsin complex. A dynamic dissolution system, representing both the gastric and intestinal system, was used to analyze this CFZ-pepsin complex, revealing that only CFZ which binds to pepsin in the gastric environment remains in solution in the intestinal environment. The CFZ-pepsin complex displays adequate solution stability for the delivery of CFZ into the lower intestinal system. In vitro bioactivity assays against Clostridium difficile demonstrated the effectiveness of this CFZ-pepsin complex for the treatment of infectious diseases in the lower intestinal system.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Pepsina A / Clofazimina / Tracto Gastrointestinal Límite: Humans Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2018 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Pepsina A / Clofazimina / Tracto Gastrointestinal Límite: Humans Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2018 Tipo del documento: Article Pais de publicación: Países Bajos