PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery

The in vitro biochemical evaluation of the applicability of polymers carrying active substances (micelles and conjugates) was carried out. Previously designed amphiphilic graft copolymers with retinol or 4-<i>n</i>-butylresorcinol functionalized polymethacrylate backbone and poly(ethylen...

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Main Authors: Justyna Odrobińska, Magdalena Skonieczna, Dorota Neugebauer
Format: Article
Language:English
Published: MDPI AG 2020-12-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/12/12/1178
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author Justyna Odrobińska
Magdalena Skonieczna
Dorota Neugebauer
author_facet Justyna Odrobińska
Magdalena Skonieczna
Dorota Neugebauer
author_sort Justyna Odrobińska
collection DOAJ
description The in vitro biochemical evaluation of the applicability of polymers carrying active substances (micelles and conjugates) was carried out. Previously designed amphiphilic graft copolymers with retinol or 4-<i>n</i>-butylresorcinol functionalized polymethacrylate backbone and poly(ethylene glycol) (PEG) side chains that included Janus-type heterografted copolymers containing both PEG and poly(ε-caprolactone) (PCL) side chains were applied as micellar carriers. The polymer self-assemblies were convenient to encapsulate arbutin (ARB) as the selected active substances. Moreover, the conjugates of PEG graft copolymers with ferulic acid (FA) or lipoic acid (LA) were also investigated. The permeability of released active substances through a membrane mimicking skin was evaluated by conducting transdermal tests in Franz diffusion cells. The biological response to new carriers with active substances was tested across cell lines, including normal human dermal fibroblasts (NHDF), human epidermal keratinocyte (HaCaT), as well as cancer melanoma (Me45) and metastatic human melanoma (451-Lu), for comparison. These polymer systems were safe and non-cytotoxic at the tested concentrations for healthy skin cell lines according to the MTT test. Cytometric evaluation of cell cycles as well as cell death defined by Annexin-V apoptosis assays and senescence tests showed no significant changes under action of the delivery systems, as compared to the control cells. In vitro tests confirmed the biochemical potential of these antioxidant carriers as beneficial components in cosmetic products, especially applied in the form of masks and eye pads.
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spelling doaj.art-59452371219c40f6b78b084cd6da62232023-11-20T23:20:55ZengMDPI AGPharmaceutics1999-49232020-12-011212117810.3390/pharmaceutics12121178PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal DeliveryJustyna Odrobińska0Magdalena Skonieczna1Dorota Neugebauer2Department of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, PolandDepartment of Systems Biology and Engineering, Silesian University of Technology, Akademicka 16, 44-100 Gliwice, PolandDepartment of Physical Chemistry and Technology of Polymers, Faculty of Chemistry, Silesian University of Technology, 44-100 Gliwice, PolandThe in vitro biochemical evaluation of the applicability of polymers carrying active substances (micelles and conjugates) was carried out. Previously designed amphiphilic graft copolymers with retinol or 4-<i>n</i>-butylresorcinol functionalized polymethacrylate backbone and poly(ethylene glycol) (PEG) side chains that included Janus-type heterografted copolymers containing both PEG and poly(ε-caprolactone) (PCL) side chains were applied as micellar carriers. The polymer self-assemblies were convenient to encapsulate arbutin (ARB) as the selected active substances. Moreover, the conjugates of PEG graft copolymers with ferulic acid (FA) or lipoic acid (LA) were also investigated. The permeability of released active substances through a membrane mimicking skin was evaluated by conducting transdermal tests in Franz diffusion cells. The biological response to new carriers with active substances was tested across cell lines, including normal human dermal fibroblasts (NHDF), human epidermal keratinocyte (HaCaT), as well as cancer melanoma (Me45) and metastatic human melanoma (451-Lu), for comparison. These polymer systems were safe and non-cytotoxic at the tested concentrations for healthy skin cell lines according to the MTT test. Cytometric evaluation of cell cycles as well as cell death defined by Annexin-V apoptosis assays and senescence tests showed no significant changes under action of the delivery systems, as compared to the control cells. In vitro tests confirmed the biochemical potential of these antioxidant carriers as beneficial components in cosmetic products, especially applied in the form of masks and eye pads.https://www.mdpi.com/1999-4923/12/12/1178micellar carriersconjugatesgraft copolymerscytotoxicityartificial skin permeation testcosmetology
spellingShingle Justyna Odrobińska
Magdalena Skonieczna
Dorota Neugebauer
PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
Pharmaceutics
micellar carriers
conjugates
graft copolymers
cytotoxicity
artificial skin permeation test
cosmetology
title PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
title_full PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
title_fullStr PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
title_full_unstemmed PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
title_short PEG Graft Polymer Carriers of Antioxidants: In Vitro Evaluation for Transdermal Delivery
title_sort peg graft polymer carriers of antioxidants in vitro evaluation for transdermal delivery
topic micellar carriers
conjugates
graft copolymers
cytotoxicity
artificial skin permeation test
cosmetology
url https://www.mdpi.com/1999-4923/12/12/1178
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AT magdalenaskonieczna peggraftpolymercarriersofantioxidantsinvitroevaluationfortransdermaldelivery
AT dorotaneugebauer peggraftpolymercarriersofantioxidantsinvitroevaluationfortransdermaldelivery