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Abstract
Objectives: While p-synephrine exhibits lipolytic activity, it also has a low oral bioavailability as well as hydrophilic characteristic, so it is difficult forit to penetrate the epidermis if it is made into transdermal preparation. The purpose of this research was to increase the penetration of p-synephrineby preparing it as transfersome gel.Materials and Methods: Three transfersome formulas were prepared—F1, F2, and F3—with the surfactants used at Tween 80, Span 80, and thecombination of Tween 80 and Span 80 with a ratio of 1:1, respectively.Results: The results showed that F1 was the best formula, with the highest entrapment efficiency, of 64.058±0.754%, a particle size average of103.3 nm, polydispersity index 0.269±0.05, and zeta potential of −36.2±0.64 mV, so this formula was employed for the gel formulation. Two gelformulas were then prepared, transfersome gel (GT) and non transfersome gel (GNT).Conclusions: The two gels were evaluated for their physical stability, and GT was found to be more stable than GNT.
Highlights
There is an increasing prevalence of overweight and obesity, which is considered a health problem
A compound that reduces cellulite is p-synephrine, which has a lipolysis effect; it binds to β-3 adrenoceptors, increasing thermogenesis and lipolysis in adipose tissue [4]
Because p-synephrine is a hydrophilic compound, issues arise when it is used as an anti-cellulite gel in transdermal preparations
Summary
There is an increasing prevalence of overweight and obesity, which is considered a health problem. An undesirable physical condition caused by overweight is the production and retention of cellulite, a result of fat deposits, typically in the thighs, buttocks, and hips, which create a dimpling, orange peel appearance on the skin [2]. Cellulite results from non-metabolized components including glucose, lipids, and proteins, causing a synthesis and accumulation of triglyceride in the adipocyte that leads to changes in the lipolysis mechanism. A compound that reduces cellulite is p-synephrine, which has a lipolysis effect; it binds to β-3 adrenoceptors, increasing thermogenesis and lipolysis in adipose tissue [4]. Because p-synephrine is a hydrophilic compound, issues arise when it is used as an anti-cellulite gel in transdermal preparations. The lipid bilayer in the stratum corneum of the epidermis is hydrophobic, making it an obstacle to an active, hydrophilic compound, which it prevents from penetrating into the deepest layers of the skin [5]
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