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

[Display omitted] ⿢Copolymer-grafted MSNs to control the release of quercetin on the skin.⿢Matrix biocompatibility in vitro assessed on human keratinocyte cell line.⿢Q complex antioxidant efficacy confirmed by DPPH and Fe2+-Ferrozine assays.⿢Porcine skin accumulation of Q evaluated by Franz cells. R...

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Veröffentlicht in:International journal of pharmaceutics 2016-09, Vol.511 (1), p.446-454
Hauptverfasser: Ugazio, Elena, Gastaldi, Lucia, Brunella, Valentina, Scalarone, Dominique, Jadhav, Sushilkumar A., Oliaro-Bosso, Simonetta, Zonari, Daniele, Berlier, Gloria, Miletto, Ivana, Sapino, Simona
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container_end_page 454
container_issue 1
container_start_page 446
container_title International journal of pharmaceutics
container_volume 511
creator Ugazio, Elena
Gastaldi, Lucia
Brunella, Valentina
Scalarone, Dominique
Jadhav, Sushilkumar A.
Oliaro-Bosso, Simonetta
Zonari, Daniele
Berlier, Gloria
Miletto, Ivana
Sapino, Simona
description [Display omitted] ⿢Copolymer-grafted MSNs to control the release of quercetin on the skin.⿢Matrix biocompatibility in vitro assessed on human keratinocyte cell line.⿢Q complex antioxidant efficacy confirmed by DPPH and Fe2+-Ferrozine assays.⿢Porcine skin accumulation of Q evaluated by Franz cells. 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.
doi_str_mv 10.1016/j.ijpharm.2016.07.024
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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). 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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. 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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.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>27421910</pmid><doi>10.1016/j.ijpharm.2016.07.024</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0001-5335-8442</orcidid></addata></record>
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subjects Administration, Cutaneous
Animals
Antioxidant
Antioxidants - administration & dosage
Antioxidants - metabolism
Biocompatibility
Cell Line, Transformed
Controlled release
Copolymer
Cutaneous application
Drug Carriers - administration & dosage
Drug Carriers - metabolism
Drug Delivery Systems - methods
Humans
MCM-41
Nanoparticles - administration & dosage
Nanoparticles - metabolism
NIPAM
Organ Culture Techniques
Porosity
Quercetin - administration & dosage
Quercetin - metabolism
Silicon Dioxide - administration & dosage
Skin - drug effects
Skin - metabolism
Swine
title Thermoresponsive mesoporous silica nanoparticles as a carrier for skin delivery of quercetin
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