MCM-41 as a useful vector for rutin topical formulations: synthesis, characterization and testing

Int J Pharm. 2013 Nov 30;457(1):177-86. doi: 10.1016/j.ijpharm.2013.09.018. Epub 2013 Sep 26.

Abstract

Rutin, the glycoside of quercetin, could be used in topical preparations because of its antioxidant and radical scavenging properties, but its employ in cosmetic and pharmaceutical products is limited by poor physico-chemical stability. These issues were addressed by preparing, characterizing and testing rutin inclusion complexes with MCM-41 mesoporous silica. The effect of surface functionalization with aminopropyl groups (NH₂-MCM-41) on the molecules properties was studied. The organic/inorganic interaction was confirmed by many techniques. In particular, the high inclusion of rutin in the pores of NH₂-MCM-41 was assessed by XRD, TGA, gas-volumetric analysis (BET), while FTIR spectroscopy allowed to analyse with great detail the molecular interaction with the inorganic surface. Rutin was stabilized against UV degradation, mostly by its inclusion in NH₂-MCM-41. Ex vivo studies showed a greater accumulation in porcine skin in the case of rutin complexed with NH₂-MCM-41. Not only antioxidant properties of rutin were maintained after immobilization but, with aminopropyl silica, the metal-chelating activity increased noticeably. The immobilization of rutin in aminopropyl silica resulted in better performance in terms of activity and photostability, suggesting the importance of functionalization in stabilizing organic molecules within silica pores.

Keywords: Antiradical activity; Flavonoids; Mesoporous silica nanoparticles; Photostability; Skin permeation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / chemistry*
  • Antioxidants / radiation effects
  • Chelating Agents / administration & dosage
  • Chelating Agents / chemistry*
  • Chelating Agents / radiation effects
  • Ferrozine / chemistry
  • In Vitro Techniques
  • Rutin / administration & dosage
  • Rutin / chemistry*
  • Rutin / radiation effects
  • Silicon Dioxide / administration & dosage
  • Silicon Dioxide / chemistry*
  • Silicon Dioxide / radiation effects
  • Skin / metabolism
  • Skin Absorption
  • Surface Properties
  • Swine
  • Ultraviolet Rays

Substances

  • Antioxidants
  • Chelating Agents
  • MCM-41
  • Ferrozine
  • Rutin
  • Silicon Dioxide