Preparation, characterization, and evaluation of anti‐tyrosinase activity of solid lipid nanoparticles containing Undecylenoyl phenylalanine (Sepiwhite®)

Abstract

Background: Hyperpigmentation is darkened patches or spots on the skin occurred by increased melanin. Undecylenoyl phenylalanine (Sepiwhite®), as a commercial lipophilic derivative of phenylalanine, is a powerful new brightener that can be used in the treatment of skin pigmentation disorders.Aims: Solid lipid nanoparticles (SLNs) increase the efficiency of hydrophobic drugs. The current study aimed to prepare and characterize SLNs containing Sepiwhite (SEPI-SLN).Methods: In this study, an optimized SEPI-SLN formulation was selected by applying the response surface method. In vitro drug loading content, the release profile of SEPI, and cell viability were investigated. The permeation rate of SEPI-SLN was also compared to conventional cream containing Sepiwhite (SEPI-CREAM). Furthermore, the anti-tyrosinase activity of Sepiwhite was also evaluated. Results:The optimized formulation showed a spherical morphology with particle size and entrapment efficiency of 218.6 ± 11.1 nm and % 87.31 ± 0.65, respectively. Differential scanning calorimetry (DSC) analysis confirmed SEPI-loaded SLN formulation with no drug-lipid incompatibility. The in vitro permeation experiment revealed the enhanced cutaneous uptake of SEPI-SLN. The results also showed that Sepiwhite could stop melanogenesis with inhibition of the tyrosinase enzyme. Conclusion:Our findings confirm that SLNs could be a proper nanocarrier for the relevant usage of Sepiwhite as a powerful brightener agent.

Nanosystems with potential application as carriers for skin depigmenting actives

“…The work presented demonstrates the growing interest in the use of lipid nanoparticles in the treatment of skin hyperchromias, due to their benefits of controlled release of whitening actives and also their occlusive effect on the skin, due to their composition. Other works found in the literature regarding lipid nanoparticles for the treatment of cutaneous hyperpigmentation involve the encapsulation of the following depigmenting actives: retinoic acid [80], arbutin [81], resveratrol [82], undecylenoyl phenylalanine [83] and ginger oil and hexylresorcinol [84]. Table 4 presents the main studies of recent years involving lipid nanoparticles for the delivery of depigmenting actives.…”