Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery

Raloxifene HCl loaded transfersomes were fabricated, optimized, and characterized as carrier for transdermal delivery to overcome the poor bioavailabilty issue with the drug. Response surface methodology (RSM) was applied for optimization of the formulation with Box-Behnken experimental design. Pho...

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Main Authors:	Mandal, Uttam Kumar, Syed, Mahmood, Bakhtiar, M. Taher
Format:	Conference or Workshop Item
Language:	English English
Published:	2014
Subjects:	RS Pharmacy and materia medica
Online Access:	http://irep.iium.edu.my/36438/ http://irep.iium.edu.my/36438/ http://irep.iium.edu.my/36438/1/PD_55_Abstract.pdf http://irep.iium.edu.my/36438/2/-P-D_55_Poster.pdf

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spelling	iium-364382018-06-19T08:17:34Z http://irep.iium.edu.my/36438/ Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery Mandal, Uttam Kumar Syed, Mahmood Bakhtiar, M. Taher RS Pharmacy and materia medica Raloxifene HCl loaded transfersomes were fabricated, optimized, and characterized as carrier for transdermal delivery to overcome the poor bioavailabilty issue with the drug. Response surface methodology (RSM) was applied for optimization of the formulation with Box-Behnken experimental design. Phospholipid PC90G (A), sodium deoxycholate (SDC) (B) and sonication time (C), each at three levels, were selected as independent variables while entrapment efficiency (EE%) (Y1), vesicle size (Y2), and transdermal flux (Y3) were the response variables. The optimized formulation was further characterized for vesicular size distribution, shape, surface morphology, and zeta-potential. Response variables data were analyzed by Design expert® software and the best model for all three response variables was found to be quadratic. Formulation No13 with composition of 300mg PC90G (A), 35mg SDC (B) and 15min sonication time (C) was predicted as the optimized formulation. The optimized formulation resulted a particle size of 134±9.0 nm with 91±4.9% EE%, 6.5±1.1μg/cm2/h transdermal flux, and -2.61±0.5 mV zeta potential. Transmission electron microscopy, scanning electron microscopy, and dynamic light scattering study defined transfersomes as spherical,unilamellar structures with a homogenous distribution and low polydispersity index (0.080±0.021). Transfersomal formulation proved significantly superior in terms of amount of drug permeated and deposited in the skin, with an enhancement ratio of 6.25±1.5 and 9.25±2.4 when compared with conventional liposomes and ethanolic phosphate buffer solution of the drug respectively. Confocal scanning laser microscopy proved an enhanced permeation of coumarin-6 loaded transfersomes to the deeper layers of the skin (160 μm) as compared to the rigid liposomes (60 μm). These in-vitro findings proved that raloxifene HCl loaded transfersomal formulation could be a superior alternative to oral delivery of the drug. 2014-04-13 Conference or Workshop Item PeerReviewed application/pdf en http://irep.iium.edu.my/36438/1/PD_55_Abstract.pdf application/pdf en http://irep.iium.edu.my/36438/2/-P-D_55_Poster.pdf Mandal, Uttam Kumar and Syed, Mahmood and Bakhtiar, M. Taher (2014) Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery. In: 5th FIP Pharmaceutical Sciences World Congress (PSWC 2014), 13th-16th Apr. 2014, Melbourne, Australia. http://www.eventure-online.com/eventure/publicSession.do?id=221738&test=221738
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English English
topic	RS Pharmacy and materia medica
spellingShingle	RS Pharmacy and materia medica Mandal, Uttam Kumar Syed, Mahmood Bakhtiar, M. Taher Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
description	Raloxifene HCl loaded transfersomes were fabricated, optimized, and characterized as carrier for transdermal delivery to overcome the poor bioavailabilty issue with the drug. Response surface methodology (RSM) was applied for optimization of the formulation with Box-Behnken experimental design. Phospholipid PC90G (A), sodium deoxycholate (SDC) (B) and sonication time (C), each at three levels, were selected as independent variables while entrapment efficiency (EE%) (Y1), vesicle size (Y2), and transdermal flux (Y3) were the response variables. The optimized formulation was further characterized for vesicular size distribution, shape, surface morphology, and zeta-potential. Response variables data were analyzed by Design expert® software and the best model for all three response variables was found to be quadratic. Formulation No13 with composition of 300mg PC90G (A), 35mg SDC (B) and 15min sonication time (C) was predicted as the optimized formulation. The optimized formulation resulted a particle size of 134±9.0 nm with 91±4.9% EE%, 6.5±1.1μg/cm2/h transdermal flux, and -2.61±0.5 mV zeta potential. Transmission electron microscopy, scanning electron microscopy, and dynamic light scattering study defined transfersomes as spherical,unilamellar structures with a homogenous distribution and low polydispersity index (0.080±0.021). Transfersomal formulation proved significantly superior in terms of amount of drug permeated and deposited in the skin, with an enhancement ratio of 6.25±1.5 and 9.25±2.4 when compared with conventional liposomes and ethanolic phosphate buffer solution of the drug respectively. Confocal scanning laser microscopy proved an enhanced permeation of coumarin-6 loaded transfersomes to the deeper layers of the skin (160 μm) as compared to the rigid liposomes (60 μm). These in-vitro findings proved that raloxifene HCl loaded transfersomal formulation could be a superior alternative to oral delivery of the drug.
format	Conference or Workshop Item
author	Mandal, Uttam Kumar Syed, Mahmood Bakhtiar, M. Taher
author_facet	Mandal, Uttam Kumar Syed, Mahmood Bakhtiar, M. Taher
author_sort	Mandal, Uttam Kumar
title	Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
title_short	Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
title_full	Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
title_fullStr	Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
title_full_unstemmed	Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
title_sort	formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery
publishDate	2014
url	http://irep.iium.edu.my/36438/ http://irep.iium.edu.my/36438/ http://irep.iium.edu.my/36438/1/PD_55_Abstract.pdf http://irep.iium.edu.my/36438/2/-P-D_55_Poster.pdf
first_indexed	2023-09-18T20:52:12Z
last_indexed	2023-09-18T20:52:12Z
_version_	1777410069010317312

Formulation and optimization of raloxifene loaded nanotransfersomes by response surface methodology for transdermal drug delivery

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