Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

Syed Mahmood, Muhammad Taher, Uttam Kumar Mandal Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM), Pahang Darul Makmur, Malaysia Abstract: Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer...

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Autores principales:	Mahmood S, Taher M, Mandal UK
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/418dab7a722d41e3a1182d5e68813c22
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spelling	oai:doaj.org-article:418dab7a722d41e3a1182d5e68813c222021-12-02T02:01:32ZExperimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application1178-2013https://doaj.org/article/418dab7a722d41e3a1182d5e68813c222014-09-01T00:00:00Zhttp://www.dovepress.com/experimental-design-and-optimization-of-raloxifene-hydrochloride-loade-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Syed Mahmood, Muhammad Taher, Uttam Kumar Mandal Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM), Pahang Darul Makmur, Malaysia Abstract: Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 µg/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 µM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug. Keywords: transfersomes, raloxifene hydrochloride, RSM, Box-Behnken, transdermal fluxMahmood STaher MMandal UKDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 4331-4346 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Mahmood S Taher M Mandal UK Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
description	Syed Mahmood, Muhammad Taher, Uttam Kumar Mandal Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia (IIUM), Pahang Darul Makmur, Malaysia Abstract: Raloxifene hydrochloride, a highly effective drug for the treatment of invasive breast cancer and osteoporosis in post-menopausal women, shows poor oral bioavailability of 2%. The aim of this study was to develop, statistically optimize, and characterize raloxifene hydrochloride-loaded transfersomes for transdermal delivery, in order to overcome the poor bioavailability issue with the drug. A response surface methodology experimental design was applied for the optimization of transfersomes, using Box-Behnken experimental design. Phospholipon® 90G, sodium deoxycholate, and sonication time, each at three levels, were selected as independent variables, while entrapment efficiency, vesicle size, and transdermal flux were identified as dependent variables. The formulation was characterized by surface morphology and shape, particle size, and zeta potential. Ex vivo transdermal flux was determined using a Hanson diffusion cell assembly, with rat skin as a barrier medium. Transfersomes from the optimized formulation were found to have spherical, unilamellar structures, with a homogeneous distribution and low polydispersity index (0.08). They had a particle size of 134±9 nM, with an entrapment efficiency of 91.00%±4.90%, and transdermal flux of 6.5±1.1 µg/cm2/hour. Raloxifene hydrochloride-loaded transfersomes proved significantly superior in terms of amount of drug permeated and deposited in the skin, with enhancement ratios of 6.25±1.50 and 9.25±2.40, respectively, when compared with drug-loaded conventional liposomes, and an ethanolic phosphate buffer saline. Differential scanning calorimetry study revealed a greater change in skin structure, compared with a control sample, during the ex vivo drug diffusion study. Further, confocal laser scanning microscopy proved an enhanced permeation of coumarin-6-loaded transfersomes, to a depth of approximately160 µM, as compared with rigid liposomes. These ex vivo findings proved that a raloxifene hydrochloride-loaded transfersome formulation could be a superior alternative to oral delivery of the drug. Keywords: transfersomes, raloxifene hydrochloride, RSM, Box-Behnken, transdermal flux
format	article
author	Mahmood S Taher M Mandal UK
author_facet	Mahmood S Taher M Mandal UK
author_sort	Mahmood S
title	Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
title_short	Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
title_full	Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
title_fullStr	Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
title_full_unstemmed	Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
title_sort	experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/418dab7a722d41e3a1182d5e68813c22
work_keys_str_mv	AT mahmoods experimentaldesignandoptimizationofraloxifenehydrochlorideloadednanotransfersomesfortransdermalapplication AT taherm experimentaldesignandoptimizationofraloxifenehydrochlorideloadednanotransfersomesfortransdermalapplication AT mandaluk experimentaldesignandoptimizationofraloxifenehydrochlorideloadednanotransfersomesfortransdermalapplication
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Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application

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