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. 2015:2015:304591.
doi: 10.1155/2015/304591. Epub 2015 Feb 15.

Structural characterization and in vitro antioxidant activity of kojic dipalmitate loaded w/o/w multiple emulsions intended for skin disorders

Maíra Lima Gonçalez  1 , Diana Gleide Marcussi  1 , Giovana Maria Fioramonti Calixto  1 , Marcos Antonio Corrêa  1 , Marlus Chorilli  1
Affiliations

Structural characterization and in vitro antioxidant activity of kojic dipalmitate loaded w/o/w multiple emulsions intended for skin disorders

Maíra Lima Gonçalez et al. Biomed Res Int. 2015.

Abstract

Multiple emulsions (MEs) are intensively being studied for drug delivery due to their ability to load and increase the bioavailability of active lipophilic antioxidant, such as kojic dipalmitate (KDP). The aim of this study was to structurally characterize developed MEs by determining the average droplet size (Dnm) and zeta potential (ZP), performing macroscopic and microscopic analysis and analyzing their rheological behavior and in vitro bioadhesion. Furthermore, the in vitro safety profile and antioxidant activity of KDP-loaded MEs were evaluated. The developed MEs showed a Dnm of approximately 1 micrometer and a ZP of -13 mV, and no change was observed in Dnm or ZP of the system with the addition of KDP. KDP-unloaded MEs exhibited ''shear thinning" flow behavior whereas KDP-loaded MEs exhibited Newtonian behavior, which are both characteristic of antithixotropic materials. MEs have bioadhesion properties that were not influenced by the incorporation of KDP. The results showed that the incorporation of KDP into MEs improved the safety profile of the drug. The in vitro antioxidant activity assay suggested that MEs presented a higher capacity for maintaining the antioxidant activity of KDP. ME-based systems may be a promising platform for the topical application of KDP in the treatment of skin disorders.

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Figures

Figure 1
Figure 1
Structural formula of kojic dipalmitate (KDP) [12].
Figure 2
Figure 2
Microscopy of KDP-unloaded MEs (100x) at 25 ± 0.5°C.
Figure 3
Figure 3
Size distribution of droplets of KDP-unloaded MEs analyzed by optical microscope.
Figure 4
Figure 4
Flow rheograms of KDP-unloaded ME (○) and KDP-loaded ME (□). Closed symbol represents up curve and open symbol represents down curve. η * (◊) is viscosity. Standard deviations have been omitted for clarity; however, in all cases, the coefficient of variation of triplicate analyses was less than 10%. Data were collected at 32 ± 0.25°C.
Figure 5
Figure 5
Percentage of hemolysis of red blood cells after treatment with free KDP, KDP-unloaded MEs, and KDP-loaded MEs.
Figure 6
Figure 6
Percentage of cell viability after treatment with free KDP, KDP-unloaded MEs, and KDP-loaded MEs.
Figure 7
Figure 7
Percent inhibition of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical by the formulations over a period of 28 days.
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