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In Vitro Skin Penetration of Dendrimer Nanoparticles

In Vitro Skin Penetration of Dendrimer Nanoparticles AbstractIntroduction: Dendrimers are highly branched, stable polymeric nanoparticles with functional groups capable of binding other molecules and may increase delivery of chemicals into skin.Materials and Methods: We examined the skin penetration of generation 3 (G3) to generation 6 (G6) polyamidoamine (PAMAM) amine-terminated (positively charged) dendrimer nanoparticles conjugated with a fluorophore (Alexa Fluor 568) for confocal imaging. The PAMAM dendrimers were further conjugated with succinic anhydride (negative surface charge) or glycidol to impart no charge (neutral). Dendrimers were applied (0.2% concentration) in aqueous solutions or cosmetic formulation onto viable pig or human cadaver skin assembled in diffusion cells.Results: After a 24-hour exposure, most fluorescence appeared in the stratum corneum (SC) or in hair follicles of both pig and human skin. We then examined the skin penetration of radiolabeled generation 4 (G4) dendrimer (0.2% concentration), conjugated with glycidol (OH) and G4 dendrimer bound to glycolic acid (GA), to determine if enhanced skin penetration of GA could occur. The skin penetration of a radiolabeled GA solution and a GA G4-OH dendrimer solution mixture was also evaluated. Most of the radioactive G4-OH dendrimer penetrating human skin remained in the SC (4.7%), with less than 1% absorbing into the epidermis and dermis. When the radiolabeled G4 dendrimer was bound to GA, penetration into SC increased significantly to 29%, and to 4% in the epidermis and dermis compared with the radiolabeled GA treatment alone (4.6%) and the radiolabeled GA G4-OH dendrimer mixture (3.4%). Using radioactivity as a marker, when labeled G4 dendrimer was bound to GA and applied to skin, there was an increase in total skin levels and total penetration levels when compared with GA and GA-dendrimer mixture.Discussion and Conclusion: It appears that the G4 dendrimer may increase the penetration of GA, demonstrating that dendrimer terminal group functionality and charge may alter skin absorption of associated chemicals. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Applied In Vitro Toxicology Mary Ann Liebert

In Vitro Skin Penetration of Dendrimer Nanoparticles

Applied In Vitro Toxicology , Volume 5 (3): 16 – Sep 1, 2019

Abstract

AbstractIntroduction: Dendrimers are highly branched, stable polymeric nanoparticles with functional groups capable of binding other molecules and may increase delivery of chemicals into skin.Materials and Methods: We examined the skin penetration of generation 3 (G3) to generation 6 (G6) polyamidoamine (PAMAM) amine-terminated (positively charged) dendrimer nanoparticles conjugated with a fluorophore (Alexa Fluor 568) for confocal imaging. The PAMAM dendrimers were further conjugated with succinic anhydride (negative surface charge) or glycidol to impart no charge (neutral). Dendrimers were applied (0.2% concentration) in aqueous solutions or cosmetic formulation onto viable pig or human cadaver skin assembled in diffusion cells.Results: After a 24-hour exposure, most fluorescence appeared in the stratum corneum (SC) or in hair follicles of both pig and human skin. We then examined the skin penetration of radiolabeled generation 4 (G4) dendrimer (0.2% concentration), conjugated with glycidol (OH) and G4 dendrimer bound to glycolic acid (GA), to determine if enhanced skin penetration of GA could occur. The skin penetration of a radiolabeled GA solution and a GA G4-OH dendrimer solution mixture was also evaluated. Most of the radioactive G4-OH dendrimer penetrating human skin remained in the SC (4.7%), with less than 1% absorbing into the epidermis and dermis. When the radiolabeled G4 dendrimer was bound to GA, penetration into SC increased significantly to 29%, and to 4% in the epidermis and dermis compared with the radiolabeled GA treatment alone (4.6%) and the radiolabeled GA G4-OH dendrimer mixture (3.4%). Using radioactivity as a marker, when labeled G4 dendrimer was bound to GA and applied to skin, there was an increase in total skin levels and total penetration levels when compared with GA and GA-dendrimer mixture.Discussion and Conclusion: It appears that the G4 dendrimer may increase the penetration of GA, demonstrating that dendrimer terminal group functionality and charge may alter skin absorption of associated chemicals.

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Publisher
Mary Ann Liebert
Copyright
Copyright 2019, Mary Ann Liebert, Inc., publishers
ISSN
2332-1512
eISSN
2332-1539
DOI
10.1089/aivt.2019.0004
Publisher site
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Abstract

AbstractIntroduction: Dendrimers are highly branched, stable polymeric nanoparticles with functional groups capable of binding other molecules and may increase delivery of chemicals into skin.Materials and Methods: We examined the skin penetration of generation 3 (G3) to generation 6 (G6) polyamidoamine (PAMAM) amine-terminated (positively charged) dendrimer nanoparticles conjugated with a fluorophore (Alexa Fluor 568) for confocal imaging. The PAMAM dendrimers were further conjugated with succinic anhydride (negative surface charge) or glycidol to impart no charge (neutral). Dendrimers were applied (0.2% concentration) in aqueous solutions or cosmetic formulation onto viable pig or human cadaver skin assembled in diffusion cells.Results: After a 24-hour exposure, most fluorescence appeared in the stratum corneum (SC) or in hair follicles of both pig and human skin. We then examined the skin penetration of radiolabeled generation 4 (G4) dendrimer (0.2% concentration), conjugated with glycidol (OH) and G4 dendrimer bound to glycolic acid (GA), to determine if enhanced skin penetration of GA could occur. The skin penetration of a radiolabeled GA solution and a GA G4-OH dendrimer solution mixture was also evaluated. Most of the radioactive G4-OH dendrimer penetrating human skin remained in the SC (4.7%), with less than 1% absorbing into the epidermis and dermis. When the radiolabeled G4 dendrimer was bound to GA, penetration into SC increased significantly to 29%, and to 4% in the epidermis and dermis compared with the radiolabeled GA treatment alone (4.6%) and the radiolabeled GA G4-OH dendrimer mixture (3.4%). Using radioactivity as a marker, when labeled G4 dendrimer was bound to GA and applied to skin, there was an increase in total skin levels and total penetration levels when compared with GA and GA-dendrimer mixture.Discussion and Conclusion: It appears that the G4 dendrimer may increase the penetration of GA, demonstrating that dendrimer terminal group functionality and charge may alter skin absorption of associated chemicals.

Journal

Applied In Vitro ToxicologyMary Ann Liebert

Published: Sep 1, 2019

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