Experimental design and optimization of raloxifene hydrochloride loaded nanotransfersomes for transdermal application
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 transferso...
| Main Authors: | , , |
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| Format: | Article |
| Language: | English English English |
| Published: |
DOVE Medical Press, Auckland
2014
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| Subjects: | |
| Online Access: | http://irep.iium.edu.my/38263/ http://irep.iium.edu.my/38263/ http://irep.iium.edu.my/38263/ http://irep.iium.edu.my/38263/1/IJN-65408-design-and-rsm-optimization-of-raloxifene-hcl-loaded-nanotra_091214.pdf http://irep.iium.edu.my/38263/4/WOS_Q1.pdf http://irep.iium.edu.my/38263/6/38263_Experimental%20design%20and%20optimization_Scopus.pdf |
| Summary: | 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 |
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