Abstract
The Ginoide Hydrolipodystrophy (GHLD), commonly known as cellulite, occurs in 80-90% of the female population after the puberty period and comes from a metabolic modification in the cutaneous adipose tissue. Caffeine has been used in topical formulations due to its lipolytic action. We studied a nanoemulsion (F3) containing caffeine with two surfactants (oleth-3 and oleth-20) by emulsification method by phase inversion temperature inversion (PIT). The polydispersion indices (PDI) showed the reduced deviation of 0.1. The mean droplet size was ~ 40 nm. The evaluated constant of Ostwald, in the refrigerator condition was the most favorable during the stability test. In the In Raman spectroscopy assay, the caffeine bands found in F3 were compatible with those found in the caffeine solution (1337, 652.5 and 558.2 cm-1). There was no interaction of caffeine anhydrous with other ingredients in nanoemulsion. In the in vitro safety assay the result of 1.4 ranked the F3 as slightly irritating. In the natural membrane, cutaneous permeation test (human skin) permeate concentrations did not exceed the saturation concentration of the PBS buffer (48.96 μg/3 mL). The caffeine solution and F3 permeated statistically equal, but the nanoemulsion visually and sensorially improved the caffeine precipitation.
Highlights
Gynoid Hydrolipodystrophy (GHLD), a modification of the cutaneous relief due to morphological, histochemical, biochemical and ultrastructural change in the skin, occurs around 80 to 90% of the female population after puberty, appearing in the pelvic, lower limb and abdomen regions (Santos et al, 2011).The dermoepidermal changes, with an increase in the size and number of adipocytes, are responsible for the skin alteration resulting in the orange peel appearance
The most widely used methylxanthine, acts on the metabolism of adipocytes and promotes the inhibition of the phosphodiesterase enzyme (Krupek, Costa, 2013; Bertin et al, 2001), which causes an increase in the cyclic adenosine monophosphate
By the graphs of intensity distribution, number and volume of F3, it could be concluded that the preparation method used was effective in obtaining monodisperse nanoemulsion
Summary
The dermoepidermal changes, with an increase in the size and number of adipocytes (hypertrophy and hyperplasia, respectively), are responsible for the skin alteration resulting in the orange peel appearance. The most widely used methylxanthine, acts on the metabolism of adipocytes and promotes the inhibition of the phosphodiesterase enzyme (Krupek, Costa, 2013; Bertin et al, 2001), which causes an increase in the cyclic adenosine monophosphate (cAMP). This mechanism results in lysis of triacylglycerol in fatty acid plus glycerol (lipolysis) (Rawlings, 2006; Ribeiro, 2010).
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