Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration

Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration

Pao-Hsien Huang,1,* Stephen Chu-Sung Hu,2,3,* Chiang-Wen Lee,4,5 An-Chi Yeh,6 Chih-Hua Tseng,7 Feng-Lin Yen1,8,9 1Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, 2Department of Dermatology, College of Medicine, Kaohsiung Medical University...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Huang PH, Hu SC, Lee CW, Yeh AC, Tseng CH, Yen FL
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2016
Materias:
7
3'
4'-trihydroxyisoflavone
nanoparticles
water solubility
skin penetration
topical delivery
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/462d3235a8f941158c43b73725cf4a23
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
id oai:doaj.org-article:462d3235a8f941158c43b73725cf4a23
record_format dspace
spelling oai:doaj.org-article:462d3235a8f941158c43b73725cf4a232021-12-02T00:12:16ZDesign of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration1178-2013https://doaj.org/article/462d3235a8f941158c43b73725cf4a232016-04-01T00:00:00Zhttps://www.dovepress.com/design-of-acid-responsive-polymeric-nanoparticles-for-7339439-trihydro-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Pao-Hsien Huang,1,* Stephen Chu-Sung Hu,2,3,* Chiang-Wen Lee,4,5 An-Chi Yeh,6 Chih-Hua Tseng,7 Feng-Lin Yen1,8,9 1Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, 2Department of Dermatology, College of Medicine, Kaohsiung Medical University, Kaohsiung, 3Department of Dermatology, Kaohsiung Medical University Hospital, Kaohsiung, 4Research Center for Industry of Human Ecology, Chang Gung University of Science and Technology, Kweishan, Taoyuan, 5Department of Nursing, Division of Basic Medical Sciences, Chang Gung University of Science and Technology, Chia-Yi, 6Department of Cosmetics and Fashion Styling, Cheng Shiu University, Kaohsiung, 7School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, 8Lipid Science and Aging Research Center, Kaohsiung Medical University, Kaohsiung, 9Institute of Biomedical Sciences, National Sun Yat-Sen University, Kaohsiung, Taiwan *These authors contributed equally to this work Abstract: 7,3',4'-Trihydroxyisoflavone (734THIF) is a secondary metabolite of daidzein and has been recently found to possess antioxidant, melanin inhibition, and skin cancer chemopreventive activities. However, the poor water solubility of 734THIF impedes its absorption and skin penetration and, therefore, limits its pharmacological effects when applied topically to the skin. We seek to use the nanoprecipitation method to prepare optimal eudragit E100 (EE)–polyvinyl alcohol (PVA)-loaded 734THIF nanoparticles (734N) to improve its physicochemical properties and thereby increase its water solubility, skin penetration, and biological activities. EE–PVA-loaded 734THIF nanoparticles (734N) were prepared, and their morphology and particle size were evaluated using a particle size analyzer and by electron microscopy. The drug loading and encapsulation efficiencies and in vitro solubility were determined using high-performance liquid chromatography. Hydrogen-bond formation was evaluated by 1H-nuclear magnetic resonance and Fourier transform infrared spectroscopy, and crystalline-to-amorphous transformation was determined by differential scanning calorimetry and X-ray diffractometry. In vitro skin penetration was analyzed using fresh pig skin mounted on Franz diffusion cells, and cytotoxicity against human keratinocyte HaCaT cells was evaluated using the MTT assay. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl-free radical scavenging ability. EE–PVA-loaded 734THIF nanoparticles showed good drug loading and encapsulation efficiencies and were characterized by improved physicochemical properties, including reduction in particle size, amorphous transformation, and intermolecular hydrogen-bond formation. This is associated with increased water solubility and enhanced in vitro skin penetration, with no cytotoxicity toward HaCaT cells. In addition, 734THIF nanoparticles retained their antioxidant activity. In conclusion, 734THIF nanoparticles are characterized by improved physicochemical properties, increased water solubility, and enhanced skin penetration, and these may have potential use in the future as a topical delivery formulation for the treatment of skin diseases. Keywords: 7,3',4'-trihydroxyisoflavone, nanoparticles, water solubility, skin penetration, topical deliveryHuang PHHu SCLee CWYeh ACTseng CHYen FLDove Medical Pressarticle73'4'-trihydroxyisoflavonenanoparticleswater solubilityskin penetrationtopical deliveryMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 1615-1627 (2016)
institution DOAJ
collection DOAJ
language EN
topic 7
3'
4'-trihydroxyisoflavone
nanoparticles
water solubility
skin penetration
topical delivery
Medicine (General)
R5-920
spellingShingle 7
3'
4'-trihydroxyisoflavone
nanoparticles
water solubility
skin penetration
topical delivery
Medicine (General)
R5-920
Huang PH
Hu SC
Lee CW
Yeh AC
Tseng CH
Yen FL
Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
description Pao-Hsien Huang,1,* Stephen Chu-Sung Hu,2,3,* Chiang-Wen Lee,4,5 An-Chi Yeh,6 Chih-Hua Tseng,7 Feng-Lin Yen1,8,9 1Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, 2Department of Dermatology, College of Medicine, Kaohsiung Medical University, Kaohsiung, 3Department of Dermatology, Kaohsiung Medical University Hospital, Kaohsiung, 4Research Center for Industry of Human Ecology, Chang Gung University of Science and Technology, Kweishan, Taoyuan, 5Department of Nursing, Division of Basic Medical Sciences, Chang Gung University of Science and Technology, Chia-Yi, 6Department of Cosmetics and Fashion Styling, Cheng Shiu University, Kaohsiung, 7School of Pharmacy, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, 8Lipid Science and Aging Research Center, Kaohsiung Medical University, Kaohsiung, 9Institute of Biomedical Sciences, National Sun Yat-Sen University, Kaohsiung, Taiwan *These authors contributed equally to this work Abstract: 7,3',4'-Trihydroxyisoflavone (734THIF) is a secondary metabolite of daidzein and has been recently found to possess antioxidant, melanin inhibition, and skin cancer chemopreventive activities. However, the poor water solubility of 734THIF impedes its absorption and skin penetration and, therefore, limits its pharmacological effects when applied topically to the skin. We seek to use the nanoprecipitation method to prepare optimal eudragit E100 (EE)–polyvinyl alcohol (PVA)-loaded 734THIF nanoparticles (734N) to improve its physicochemical properties and thereby increase its water solubility, skin penetration, and biological activities. EE–PVA-loaded 734THIF nanoparticles (734N) were prepared, and their morphology and particle size were evaluated using a particle size analyzer and by electron microscopy. The drug loading and encapsulation efficiencies and in vitro solubility were determined using high-performance liquid chromatography. Hydrogen-bond formation was evaluated by 1H-nuclear magnetic resonance and Fourier transform infrared spectroscopy, and crystalline-to-amorphous transformation was determined by differential scanning calorimetry and X-ray diffractometry. In vitro skin penetration was analyzed using fresh pig skin mounted on Franz diffusion cells, and cytotoxicity against human keratinocyte HaCaT cells was evaluated using the MTT assay. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl-free radical scavenging ability. EE–PVA-loaded 734THIF nanoparticles showed good drug loading and encapsulation efficiencies and were characterized by improved physicochemical properties, including reduction in particle size, amorphous transformation, and intermolecular hydrogen-bond formation. This is associated with increased water solubility and enhanced in vitro skin penetration, with no cytotoxicity toward HaCaT cells. In addition, 734THIF nanoparticles retained their antioxidant activity. In conclusion, 734THIF nanoparticles are characterized by improved physicochemical properties, increased water solubility, and enhanced skin penetration, and these may have potential use in the future as a topical delivery formulation for the treatment of skin diseases. Keywords: 7,3',4'-trihydroxyisoflavone, nanoparticles, water solubility, skin penetration, topical delivery
format article
author Huang PH
Hu SC
Lee CW
Yeh AC
Tseng CH
Yen FL
author_facet Huang PH
Hu SC
Lee CW
Yeh AC
Tseng CH
Yen FL
author_sort Huang PH
title Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
title_short Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
title_full Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
title_fullStr Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
title_full_unstemmed Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
title_sort design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration
publisher Dove Medical Press
publishDate 2016
url https://doaj.org/article/462d3235a8f941158c43b73725cf4a23
work_keys_str_mv AT huangph designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
AT husc designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
AT leecw designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
AT yehac designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
AT tsengch designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
AT yenfl designofacidresponsivepolymericnanoparticlesfor7339439trihydroxyisoflavonetopicaladministration
_version_ 1718403861924806656

Ejemplares similares