Proretinal nanoparticles: stability, release, efficacy, and irritation

Pimolphan Pisetpackdeekul,1 Piyapan Supmuang,2 Porntip Pan-In,3 Wijit Banlunara,4,* Benchaphorn Limcharoen,4 Chayada Kokpol,5,* Supason Wanichwecharungruang3,6,* 1Program in Technopreneurship and Innovation Management, Graduate School, 2Program in Biotechnology, 3Department of Chemistry, Faculty of...

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Autores principales:	Pisetpackdeekul P, Supmuang P, Pan-In P, Banlunara W, Limcharoen B, Kokpol C, Wanichwecharungruang S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	anti-aging sebum release drug delivery skin Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/db329f0c1357442eaa916691c6ee7cc0
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spelling	oai:doaj.org-article:db329f0c1357442eaa916691c6ee7cc02021-12-02T05:14:21ZProretinal nanoparticles: stability, release, efficacy, and irritation1178-2013https://doaj.org/article/db329f0c1357442eaa916691c6ee7cc02016-07-01T00:00:00Zhttps://www.dovepress.com/proretinal-nanoparticles-stability-release-efficacy-and-irritation-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Pimolphan Pisetpackdeekul,1 Piyapan Supmuang,2 Porntip Pan-In,3 Wijit Banlunara,4,* Benchaphorn Limcharoen,4 Chayada Kokpol,5,* Supason Wanichwecharungruang3,6,* 1Program in Technopreneurship and Innovation Management, Graduate School, 2Program in Biotechnology, 3Department of Chemistry, Faculty of Science, 4Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University, 5Division of Dermatology, Department of Medicine, Faculty of Medicine, Ramathibodi Hospital, 6Nanotec-Chulalongkorn University Center of Excellence on Food and Agriculture, Chulalongkorn University, Bangkok, Thailand *These authors contributed equally to this work Abstract: Despite many potent biological activities, retinoids such as retinoic acid (RA) and retinal possess dose-related broad side effects. In this study, we show that this problem, which has been unsolvable for a long time, can be tackled through a controlled release strategy in which retinal is continuously delivered to the skin via sustained release from proretinal nanoparticles. The water dispersible proretinal nanoparticles are stable when kept in water at neutral pH and at room temperature for 8 months under light-proof conditions, and show sustained release of retinal into human synthetic sebum at a pH of 5. In the daily topical application tests performed for 4 weeks on rats’ skin, the nanoparticles showed superior ability to increase epidermal thickness compared to RA and retinal, with no skin irritation observed for the proretinal particles, but severe skin irritation observed for RA and free retinal. When tested under occlusion conditions in human volunteers, insignificant skin irritation was observed for the proretinal nanoparticles. The 12-week, double-blind, split-face study on human volunteers indicates better antiaging efficacy of the particles as compared to the free RA. Keywords: antiaging, sebum, release, drug delivery, skinPisetpackdeekul PSupmuang PPan-In PBanlunara WLimcharoen BKokpol CWanichwecharungruang SDove Medical Pressarticleanti-agingsebumreleasedrug deliveryskinMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 3277-3286 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	anti-aging sebum release drug delivery skin Medicine (General) R5-920
spellingShingle	anti-aging sebum release drug delivery skin Medicine (General) R5-920 Pisetpackdeekul P Supmuang P Pan-In P Banlunara W Limcharoen B Kokpol C Wanichwecharungruang S Proretinal nanoparticles: stability, release, efficacy, and irritation
description	Pimolphan Pisetpackdeekul,1 Piyapan Supmuang,2 Porntip Pan-In,3 Wijit Banlunara,4,* Benchaphorn Limcharoen,4 Chayada Kokpol,5,* Supason Wanichwecharungruang3,6,* 1Program in Technopreneurship and Innovation Management, Graduate School, 2Program in Biotechnology, 3Department of Chemistry, Faculty of Science, 4Department of Pathology, Faculty of Veterinary Science, Chulalongkorn University, 5Division of Dermatology, Department of Medicine, Faculty of Medicine, Ramathibodi Hospital, 6Nanotec-Chulalongkorn University Center of Excellence on Food and Agriculture, Chulalongkorn University, Bangkok, Thailand *These authors contributed equally to this work Abstract: Despite many potent biological activities, retinoids such as retinoic acid (RA) and retinal possess dose-related broad side effects. In this study, we show that this problem, which has been unsolvable for a long time, can be tackled through a controlled release strategy in which retinal is continuously delivered to the skin via sustained release from proretinal nanoparticles. The water dispersible proretinal nanoparticles are stable when kept in water at neutral pH and at room temperature for 8 months under light-proof conditions, and show sustained release of retinal into human synthetic sebum at a pH of 5. In the daily topical application tests performed for 4 weeks on rats’ skin, the nanoparticles showed superior ability to increase epidermal thickness compared to RA and retinal, with no skin irritation observed for the proretinal particles, but severe skin irritation observed for RA and free retinal. When tested under occlusion conditions in human volunteers, insignificant skin irritation was observed for the proretinal nanoparticles. The 12-week, double-blind, split-face study on human volunteers indicates better antiaging efficacy of the particles as compared to the free RA. Keywords: antiaging, sebum, release, drug delivery, skin
format	article
author	Pisetpackdeekul P Supmuang P Pan-In P Banlunara W Limcharoen B Kokpol C Wanichwecharungruang S
author_facet	Pisetpackdeekul P Supmuang P Pan-In P Banlunara W Limcharoen B Kokpol C Wanichwecharungruang S
author_sort	Pisetpackdeekul P
title	Proretinal nanoparticles: stability, release, efficacy, and irritation
title_short	Proretinal nanoparticles: stability, release, efficacy, and irritation
title_full	Proretinal nanoparticles: stability, release, efficacy, and irritation
title_fullStr	Proretinal nanoparticles: stability, release, efficacy, and irritation
title_full_unstemmed	Proretinal nanoparticles: stability, release, efficacy, and irritation
title_sort	proretinal nanoparticles: stability, release, efficacy, and irritation
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/db329f0c1357442eaa916691c6ee7cc0
work_keys_str_mv	AT pisetpackdeekulp proretinalnanoparticlesstabilityreleaseefficacyandirritation AT supmuangp proretinalnanoparticlesstabilityreleaseefficacyandirritation AT paninp proretinalnanoparticlesstabilityreleaseefficacyandirritation AT banlunaraw proretinalnanoparticlesstabilityreleaseefficacyandirritation AT limcharoenb proretinalnanoparticlesstabilityreleaseefficacyandirritation AT kokpolc proretinalnanoparticlesstabilityreleaseefficacyandirritation AT wanichwecharungruangs proretinalnanoparticlesstabilityreleaseefficacyandirritation
_version_	1718400500785741824

Proretinal nanoparticles: stability, release, efficacy, and irritation

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