Background: Melanin plays an important role in protecting the skin against the harmful effects of solar radiation, but its abnormal accumulation may become an aesthetic problem, such as melasma and age spots. Aims: The aim of this study was to evaluate the antiangiogenic and whitening effects of a depigmentation formulation (BLTX) using an in vitro model of human cell and skin culture. Methods: Human fibroblasts, keratinocytes or melanocytes were treated with BLTX and subjected to oxidative stress by UV radiation or inflammatory stress with IL-1α for quantification of melanin, tyrosinase, endothelin-1, PAR-2, VEGF and iNOS. Fragments of human skin, from elective plastic surgery, were treated with BLTX and subjected to histological evaluation with hematoxylin/eosin associated with Fontana-Masson technique for melanin view. A parametric method, the one-way analysis of variance (ANOVA) followed by the Bonferroni test, was used to compare data among all groups. Results: The results demonstrated that BLTX promotes a reduction in VEGF and iNOS protein synthesis in cultured dermal fibroblasts, indicating an antiangiogenic property. In relation to whitening effect, BLTX was able to reduce the production of melanin in both systems, melanocytes and human skin cultures. The depigmenting action was also revealed by decreasing the levels of endothelin-1, PAR-2 and activity of tyrosinase, when compared to cultures exposed to UV radiation. Conclusion: The results allow us to infer that BLTX presents an antiangiogenic effect indicating a role in the vascular component of melasma. Furthermore, the whitening property observed reinforces its use in the prevention and treatment of melasma.