Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine

Hamdy Abdelkader,1,2 Michael R Longman,1 Raid G Alany,1,3 Barbara Pierscionek4 1Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston Upon Thames, London, UK; 2Department of Pharmaceutics, Faculty of Pharmacy,...

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Autores principales: Abdelkader H, Longman MR, Alany RG, Pierscionek B
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Publicado: Dove Medical Press 2016
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spelling oai:doaj.org-article:9ea3b22a0f8a45a192364e11bf9ad0622021-12-02T07:36:57ZPhytosome-hyaluronic acid systems for ocular delivery of L-carnosine1178-2013https://doaj.org/article/9ea3b22a0f8a45a192364e11bf9ad0622016-06-01T00:00:00Zhttps://www.dovepress.com/phytosome-hyaluronic-acid-systems-for-ocular-delivery-of-l-carnosine-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Hamdy Abdelkader,1,2 Michael R Longman,1 Raid G Alany,1,3 Barbara Pierscionek4 1Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston Upon Thames, London, UK; 2Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Mina, Egypt; 3School of Pharmacy, The University of Auckland, Auckland, New Zealand; 4Vision Cognition and Neuroscience Theme, Faculty of Science, Engineering and Computing, Kingston University London, Kingston Upon Thames, London, UK Abstract: This study reports on L-carnosine phytosomes as an alternative for the prodrug N-acetyl-L-carnosine as a novel delivery system to the lens. L-carnosine was loaded into lipid-based phytosomes and hyaluronic acid (HA)-dispersed phytosomes. L-carnosine-phospholipid complexes (PC) of different molar ratios, 1:1 and 1:2, were prepared by the solvent evaporation method. These complexes were characterized with thermal and spectral analyses. PC were dispersed in either phosphate buffered saline pH 7.4 or HA (0.1% w/v) in phosphate buffered saline to form phytosomes PC1:1, PC1:2, and PC1:2 HA, respectively. These phytosomal formulations were studied for size, zeta potential, morphology, contact angle, spreading coefficient, viscosity, ex vivo transcorneal permeation, and cytotoxicity using primary human corneal cells. L-carnosine-phospholipid formed a complex at a 1:2 molar ratio and phytosomes were in the size range of 380–450 nm, polydispersity index of 0.12–0.2. The viscosity of PC1:2 HA increased by 2.4 to 5-fold compared with HA solution and PC 1:2, respectively; significantly lower surface tension, contact angle, and greater spreading ability for phytosomes were also recorded. Ex vivo transcorneal permeation parameters showed significantly controlled corneal permeation of L-carnosine with the novel carrier systems without any significant impact on primary human corneal cell viability. Ex vivo porcine lenses incubated in high sugar media without and with L-carnosine showed concentration-dependent marked inhibition of lens brunescence indicative of the potential for delaying changes that underlie cataractogenesis that may be linked to diabetic processes. Keywords: lipoid S 75, phytosomes, L-carnosine, cataract, hyaluronate sodium, ocular deliveryAbdelkader HLongman MRAlany RGPierscionek BDove Medical PressarticleLipoid S 75PhytosomesL-carnosinecataractHyaluronate sodiumOcular deliveryMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2815-2827 (2016)
institution DOAJ
collection DOAJ
language EN
topic Lipoid S 75
Phytosomes
L-carnosine
cataract
Hyaluronate sodium
Ocular delivery
Medicine (General)
R5-920
spellingShingle Lipoid S 75
Phytosomes
L-carnosine
cataract
Hyaluronate sodium
Ocular delivery
Medicine (General)
R5-920
Abdelkader H
Longman MR
Alany RG
Pierscionek B
Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
description Hamdy Abdelkader,1,2 Michael R Longman,1 Raid G Alany,1,3 Barbara Pierscionek4 1Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston Upon Thames, London, UK; 2Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Mina, Egypt; 3School of Pharmacy, The University of Auckland, Auckland, New Zealand; 4Vision Cognition and Neuroscience Theme, Faculty of Science, Engineering and Computing, Kingston University London, Kingston Upon Thames, London, UK Abstract: This study reports on L-carnosine phytosomes as an alternative for the prodrug N-acetyl-L-carnosine as a novel delivery system to the lens. L-carnosine was loaded into lipid-based phytosomes and hyaluronic acid (HA)-dispersed phytosomes. L-carnosine-phospholipid complexes (PC) of different molar ratios, 1:1 and 1:2, were prepared by the solvent evaporation method. These complexes were characterized with thermal and spectral analyses. PC were dispersed in either phosphate buffered saline pH 7.4 or HA (0.1% w/v) in phosphate buffered saline to form phytosomes PC1:1, PC1:2, and PC1:2 HA, respectively. These phytosomal formulations were studied for size, zeta potential, morphology, contact angle, spreading coefficient, viscosity, ex vivo transcorneal permeation, and cytotoxicity using primary human corneal cells. L-carnosine-phospholipid formed a complex at a 1:2 molar ratio and phytosomes were in the size range of 380–450 nm, polydispersity index of 0.12–0.2. The viscosity of PC1:2 HA increased by 2.4 to 5-fold compared with HA solution and PC 1:2, respectively; significantly lower surface tension, contact angle, and greater spreading ability for phytosomes were also recorded. Ex vivo transcorneal permeation parameters showed significantly controlled corneal permeation of L-carnosine with the novel carrier systems without any significant impact on primary human corneal cell viability. Ex vivo porcine lenses incubated in high sugar media without and with L-carnosine showed concentration-dependent marked inhibition of lens brunescence indicative of the potential for delaying changes that underlie cataractogenesis that may be linked to diabetic processes. Keywords: lipoid S 75, phytosomes, L-carnosine, cataract, hyaluronate sodium, ocular delivery
format article
author Abdelkader H
Longman MR
Alany RG
Pierscionek B
author_facet Abdelkader H
Longman MR
Alany RG
Pierscionek B
author_sort Abdelkader H
title Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
title_short Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
title_full Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
title_fullStr Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
title_full_unstemmed Phytosome-hyaluronic acid systems for ocular delivery of L-carnosine
title_sort phytosome-hyaluronic acid systems for ocular delivery of l-carnosine
publisher Dove Medical Press
publishDate 2016
url https://doaj.org/article/9ea3b22a0f8a45a192364e11bf9ad062
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AT alanyrg phytosomehyaluronicacidsystemsforoculardeliveryoflcarnosine
AT pierscionekb phytosomehyaluronicacidsystemsforoculardeliveryoflcarnosine
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