Double Drug Delivery Using Capped Mesoporous Silica Microparticles for the Effective Treatment of Inflammatory Bowel Disease

Fecha de publicación:

Autores de IIS La Fe

Participantes ajenos a IIS La Fe

  • Teruel, AH
  • Perez-Esteve, E
  • Gonzalez-Alvarez, I
  • Gonzalez-Alvarez, M
  • Costero, AM
  • Ferri, D
  • Gavina, P
  • Merino, V
  • Sancenon, F

Grupos

Abstract

Silica mesoporous microparticles loaded with both rhodamine B fluorophore (S1) or hydrocortisone (S2), and capped with an olsalazine derivative, are prepared and fully characterized. Suspensions of Si and S2 in water at an acidic and a neutral pH show negligible dye/drug release, yet a notable delivery took place when the reducing agent sodium dithionite is added because of hydrolysis of an azo bond in the capping ensemble. Additionally, olsalazine fragmentation induced 5-aminosalicylic acid (5-ASA) release. In vitro digestion models show that S1 and S2 solids are suitable systems to specifically release a pharmaceutical agent in the colon. In vivo pharmacokinetic studies in rats show a preferential rhodamine B release from Si in the colon. Moreover, a model of ulcerative colitis is induced in rats by oral administration of 2,4,6-trinitrobenzenesulfonic acid (TNBS) solutions, which was also used to prove the efficacy of S2 for colitis treatment. The specific delivery of hydrocortisone and 5-ASA from S2 material to the colon tissue in injured rats markedly lowers the colon/body weight ratio and the clinical activity score. Histological studies showed a remarkable reduction in inflammation, as well as an intensive regeneration of the affected tissues.

Datos de la publicación

ISSN/ISSNe:
1543-8384, 1543-8392

MOLECULAR PHARMACEUTICS  AMER CHEMICAL SOC

Tipo:
Article
Páginas:
2418-2429
Factor de Impacto:
1,213 SCImago
Cuartil:
Q1 SCImago

Citas Recibidas en Web of Science: 15

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Keywords

  • mesoporous silica microparticles; gated materials; smart drug delivery materials; colon targeted release; inflammatory bowel disease

Campos de estudio

Proyectos asociados

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Investigador Principal: RAMÓN MARTÍNEZ MÁÑEZ

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