Skin barrier modulation by hibiscus rosa-sinensis mucilage for transdermal drug delivery / Nor Maziah Saidin

Saidin, Nor Maziah (2020) Skin barrier modulation by hibiscus rosa-sinensis mucilage for transdermal drug delivery / Nor Maziah Saidin. Masters thesis, Universiti Teknologi MARA.


Transdermal drug delivery system provides continuous controlled delivery of active
ingredients through the human skin and into the bloodstream. Poor penetration of most
drugs into the skin has led to numerous studies being conducted to increase their
permeability. The present study investigated the ability of Hibiscus rosa-sinensis (HRS)
leaves mucilage in modifying skin barrier for transdermal drug delivery. The mucilage
obtained from HRS leaves is a novel source of polysaccharides, and its skin permeation
modulating effect has yet to be explored. Dried-powdered mucilage was extracted from
the leaves of HRS, and its physicochemical properties were analysed. The HRS gels
were formulated with three concentrations of HRS mucilage, namely 1 (CL1), 1.5
(CL1.5), and 2 (CL2) %(w/w) using caffeine as a model drug. The in vitro drug release
and permeation profiles of caffeine were examined using vertical diffusion cells.
Physicochemical properties of HRS mucilage and HRS gels were characterised by
molecular weight analysis, differential scanning calorimetry (DSC), particle size,
viscosity, pH, attenuated total reflectance Fourier transform infrared (ATR-FTIR)
spectroscopy, and X-ray diffractometry (XRD), while the mechanisms of drug
permeation were evaluated by subjecting the rat skin to scanning electron microscopy
(SEM), ATR-FTIR, and DSC. The results indicated that the releases of caffeine from
HRS gels in 24 hours were 47.17 ± 5.72, 46.90 ± 2.25 and 48.63 ± 2.33 % of CL1,
CL1.5 and CL2, respectively (ANOVA: p > 0.05). Nevertheless, the CL2 gel
demonstrated a significantly highest drug permeation (2029.44 ± 313.39 μg cm-2
) when

compared to caffeine solution (1400.48 ± 167.15 μg cm-2

), CL1 (1129.53 ± 425.64 μg

), and CL1.5 (1007.27 ± 588.73 μg cm-2

) (ANOVA: p < 0.05). The CL2 possessed
a combination of higher viscosity, higher amorphous property and smaller particle size
than CL1 and CL1.5. High viscosity resulted in prolonged contact with the skin. High
amorphous denotesthat the particles exist as high energy compound with enhanced drug
solubility and thermodynamic activity, thus facilitated the drug permeation. In addition,
small particle size enabled greater contact and interaction with the stratum corneum.
HRS gels generally altered the barrier and permeability of the skin by perturbing the
lipid and protein structures, acting on the helical keratin filaments as well as through
the O–H and/or N–H interactions. These were then reduced the diffusional resistance
for drug transport and increased the drug permeation. The optimal concentration of HRS
mucilage at 2 %(w/w) (CL2) was deemed useful in facilitating the transdermal delivery
of caffeine.


Item Type: Thesis (Masters)
Email / ID Num.
Saidin, Nor Maziah
Email / ID Num.
Thesis advisor
Anuar, Nor Khaizan (Dr.)
Subjects: R Medicine > RM Therapeutics. Pharmacology > Drugs and their actions
Divisions: Universiti Teknologi MARA, Shah Alam > Faculty of Pharmacy
Programme: Master of Science (Pharmaceutics)
Keywords: TDDS; polysaccharides; Hibiscus Rosa-Sinensis; caffeine
Date: August 2020
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