Thermoresponsive mesoporous silica nanoparticles as a carrier for skin delivery of quercetin

Int J Pharm. 2016 Sep 10;511(1):446-454. doi: 10.1016/j.ijpharm.2016.07.024. Epub 2016 Jul 13.

Abstract

Recently, mesoporous silica nanoparticles (MSNs) have emerged as promising drug delivery systems able to preserve the integrity of the carried substance and/or to selectively reach a target site; however, they have rarely been explored for skin application. In this study, thermoresponsive MSNs, designed to work at physiologic cutaneous temperature, are proposed as innovative topical carriers for quercetin (Q), a well-known antioxidant. The thermosensitive nanoparticles were prepared by functionalizing two different types of matrices, with pore size of 3.5nm (MSNsmall) and 5.0nm (MSNbig), carrying out a free radical copolymerization of N-isopropylacrylamide (NIPAM) and 3-(methacryloxypropyl)trimethoxysilane (MPS) inside the mesopores. The obtained copolymer-grafted MSNs (copoly-MSNs) were physico-chemically characterized and their biocompatibility was attested on a human keratinocyte cell line (HaCaT). The release profiles were assessed and the functional activity of Q, free or loaded, was evaluated in terms of antiradical and metal chelating activities. Ex vivo accumulation and permeation through porcine skin were also investigated. The characterization confirmed the copolymer functionalization of the MSNs. In addition, both the bare and functionalized silica matrices were found to be biocompatible. Among the copolymer-grafted complexes, Q/copoly-MSNbig exhibited more evident thermoresponsive behavior proving the potential of these thermosensitive systems for advanced dermal delivery.

Keywords: Antioxidant; Biocompatibility; Controlled release; Copolymer; Cutaneous application; MCM-41; NIPAM.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antioxidants / administration & dosage
  • Antioxidants / metabolism
  • Cell Line, Transformed
  • Drug Carriers / administration & dosage*
  • Drug Carriers / metabolism
  • Drug Delivery Systems / methods*
  • Humans
  • Nanoparticles / administration & dosage*
  • Nanoparticles / metabolism
  • Organ Culture Techniques
  • Porosity
  • Quercetin / administration & dosage*
  • Quercetin / metabolism
  • Silicon Dioxide / administration & dosage*
  • Skin / drug effects*
  • Skin / metabolism
  • Swine

Substances

  • Antioxidants
  • Drug Carriers
  • Silicon Dioxide
  • Quercetin