Propanediol (and) Caprylic Acid (and) Xylitol as a New Single Topical Active Ingredient against Acne: In Vitro and In Vivo Efficacy Assays.

In addition to dermatological complications, acne can affect the quality of life of individuals in numerous ways, such as employment, social habits and body dissatisfaction. According to our expertise, caprylic acid and propanediol would not have a direct action on Cutibacterium acnes. Despite this, we investigated the existence of a synergistic effect among xylitol, caprylic acid and propanediol as a mixture of compounds representing a single topical active ingredient that could benefit the treatment against acne. In vitro and in vivo assays were performed to challenge and to prove the efficacy of propanediol, xylitol and caprylic acid (PXCA) against acne. PXCA had its MIC challenged against C. acnes (formerly Propionibacterium acnes) and Staphylococcus aureus, resulting in concentrations of 0.125% and 0.25%, respectively, and it also developed antimicrobial activity against C. acnes (time-kill test). PXCA was able to reduce the 5-alpha reductase expression in 24% (p < 0.01) in comparison with the testosterone group. By the end of 28 days of treatment, the compound reduced the skin oiliness, porphyrin amount and the quantity of inflammatory lesions in participants. According to the dermatologist evaluation, PXCA improved the skin's general appearance, acne presence and size.

Vitamin E-loaded bigels and emulsions: Physicochemical characterization and potential biological application.

Bigels have been studied as topical formulations for its benefits over sensory and drug delivery parameters. However, there is still few evidences about the properties of the combination of organogelators, oily phases and bioactive molecules into rheological and stability behavior. We investigated the use of classical organogelators (candelilla wax and 12-hydroxystearic acid) and oily phases (sunflower and mineral oil) in 5/95 organogel/polymeric hydrogel ratio to compare vitamin E bigels with its corresponding emulsions. The rheological measurements, microstructure, physical and oxidative stability properties and biological behavior were evaluated. The obtained oil-in-water bigels and emulsions showed crystallization pattern at the interface with high thermal and centrifuge-stress stability. Viscoelastic weak gels were obtained with higher thixotropy and consistency of 12-hydroxystearic bigels. The diameter of the inner phase was increased by vitamin E, despite its little influence over physical and oxidative stability of bigels and emulsions. Those findings indicated that sensory attributes may be regulated by the organogel composition.

Coumaric acid derivatives as tyrosinase inhibitors: Efficacy studies through in silico, in vitro and ex vivo approaches.

p-Coumaric acid is a known inhibitor of tyrosinase, an enzyme involved in the initial steps of the melanin synthesis in human and other species. However, its low lipophilicity impairs its penetration through skin and efficacy as antimelanogenic agent indeed. Accordingly, this paper reports the assessment of several coumaric acid derivatives as tyrosinase inhibitors and antimelanogenic agents in in vitro, in silico and ex vivo assays. The compounds were designed with modifications in the aromatic and acid moieties of p-coumaric acid, being the coumarate esters the most promising derivatives. The compounds showed higher tyrosinase inhibitory activity (pIC50 3.7-4.2) than the parent acid, being compounds 1d, 1e and 1f the most potent inhibitors. Docking analysis showed that these esters are competitive inhibitors per se, and act independently of a redox mechanism as suggested by DPPH assays. Moreover, the esters showed efficacy in reducing the melanin deposition in human skin fragments at 0.1% concentration, especially compound 1e. In summary, there is an important equilibria between tyrosinase affinity and lipophilicity that must be considered to get effective antimelanogenic agents with adequate permeability in the skin.

Composto nutracêutico aumenta a síntese de colágeno, elastina e ácido hialurônico / Nutraceutical compound increases collagen, elastin and hyaluronic acid synthesis

Introdução: O uso de produtos nutracêuticos com a finalidade de atenuar os sinais do envelhecimento da pele tem sido proposto na literatura. O estímulo à síntese de elementos de sustentação da derme é um dos mecanismos relacionados a esse efeito. Objetivo: Avaliar a eficácia de um nutracêutico contendo luteína, licopeno, vitamina C e mangânes na síntese de colágeno, elastina e ácido hialurônico. Métodos: Estudo realizado in vitro, através de cultura de fibroblastos humanos tratadas com o produto investigado em diferentes concentrações não citotóxicas. A quantificação de elastina e colágeno foi determinada através de medidas espectrofotométricas enquanto que a de ácido hialurônico foi determinada por método imunoenzimático. Resultados: As culturas celulares tratadas com as diferentes concentrações do produto apresentaram quantidade sintetizada de colágeno, elastina e ácido hialurônico significativamente maior quando comparadas com a cultura não tratada (p<0,05). Conclusões: O uso de nutracêutico contendo licopeno, vitamina C, luteína e manganês demonstrou eficácia in vitro no estímulo à síntese de colágeno, elastina e ácido hialurônico, elementos essenciais na estrutura de sustentação da derme e responsáveis pelas características de firmeza e elasticidade da pele.

Introduction: The use of nutraceutical products in order to attenuate signs of skin aging has been proposed in the literature. The stimulus to the synthesis of substances that support the dermis is one of the mechanisms linked to this effect. Objective: To evaluate the effectiveness of a nutraceutical compound containing lutein, lycopene, vitamin C and manganese for the synthesis of collagen, elastin and hyaluronic acid. Methods: An in vitro study was carried out based on the culture of human fibroblasts treated with the investigated product in different non-cytotoxic concentrations. The quantification of the elastin and collagen was performed with the assistance of spectrophotometric measurements. Hyaluronic acid was measure using a immunoenzymatic method. Results: Cell cultures treated with the different concentrations of the product showed a significantly higher amount of synthesized collagen, elastin and hyaluronic acid as compared to the untreated culture (p <0.05). Conclusions: The use of the nutraceutical compound containing lycopene, vitamin C, lutein and manganese has shown in vitro efficacy for stimulating the synthesis of collagen, elastin and hyaluronic acid, components that are crucial for providing the dermis' supporting structure, being responsible for the skin's firmness and elasticity.