Evaluation of the antioxidant and antityrosinase activities of Prosopis juliflora fruit extract as a novel multifunctional bioactive ingredient and its potential applicability in pro-ageing and skin colour harmonization cosmetic products.

OBJECTIVE: Prosopis juliflora, commonly known as algaroba or mesquite, was introduced and has since proliferated throughout the semi-arid region of the Caatinga biome. Various studies have documented its properties, including antimicrobial, antioxidant, and antitumor activities, attributed to the presence of diverse secondary metabolites such as alkaloids, terpenoids, tannins, and flavonoids. The objective of this study was to evaluate the antioxidant and antityrosinase activities of P. juliflora fruit extract as a multifunctional active ingredient, and to develop cosmetic formulations containing this vegetal extract for potential applications in skincare products targeting pro-ageing and skin colour homogenization properties. METHODS: The extraction process followed established protocols. Chemical characterization of the extract involved quantification of total flavonoids and phenolic compounds, along with Liquid Chromatography-Mass Spectrometry (LC-MS) analysis. In vitro antioxidant activity was assessed using different methods. Antityrosinase activity was determined by employing enzymatic assays. Cosmetic formulations containing Disodium EDTA, Phenoxyethanol (and) Ethylhexyl Glycerin, Distilled Water, Sodium Acrylates Copolymer Lecithin, Polyacrylamide (and) C13-14 Isoparaffin (and) Laureth-7, and 3.0% of the investigated plant extract were subjected to preliminary and accelerated stability tests. RESULTS: The extract demonstrated a concentration of total flavonoids (1.71 ± 0.26 µg EQ/mg) and exhibited concentrations of phenolic compounds at 0.21 ± 0.01 mg EAG/g. Metabolites such as flavonoids and saponins were annotated, as well as some of their respective glycosidic derivatives. The extract showed antioxidant potential and the ability to inhibit the oxidation cascade in both the initiation and propagation phases. Moreover, the extract exhibited noteworthy inhibition of antityrosinase activity, presenting 62.48 ± 2.09 at a concentration of 30.00 mg/mL. The formulations were stable in accelerated stability tests over a 60-day period. CONCLUSION: This research not only demonstrates scientifically by demonstrating the potential of a plant from the Caatinga biome with antioxidant and antityrosinase properties in the development of cosmetic products aimed at pro-ageing effects and skin colour harmonization, but also adds value to the P. juliflora production chain. This valorization encompasses various aspects which include environmental, social, and biodiversity responsibilities.

OBJECTIF: Prosopis juliflora, communément appelée algaroba ou mesquite, a été introduite et s'est depuis proliférée dans la région semi­aride du biome de la Caatinga. Diverses études ont documenté ses propriétés, y compris des activités antimicrobiennes, antioxydantes et antitumorales, attribuées à la présence de divers métabolites secondaires tels que les alcaloïdes, les terpénoïdes, les tanins et les flavonoïdes. L'objectif de cette étude était d'évaluer les activités antioxydantes et antityrosinases de l'extrait de fruit de P. juliflora en tant qu'ingrédient actif multifonctionnel, et de développer des formulations cosmétiques contenant cet extrait végétal pour des applications potentielles dans des produits de soins de la peau ciblant les propriétés anti­âge et d'homogénéisation de la couleur de la peau. MÉTHODES: Le processus d'extraction a suivi des protocoles établis. La caractérisation chimique de l'extrait a impliqué la quantification des flavonoïdes totaux et des composés phénoliques, ainsi qu'une analyse par chromatographie liquide­spectrométrie de masse. L'activité antioxydante in vitro a été évaluée en utilisant différentes méthodes. L'activité antityrosinase a été déterminée en utilisant des essais enzymatiques. Les formulations cosmétiques contenant du Disodium EDTA, du Phenoxyethanol (et) Ethylhexyl Glycerin, de l'Eau Distillée, du Copolymère de Sodium Acrylates Lecithin, du Polyacrylamide (et) C13­14 Isoparaffin (et) Laureth­7, et 3.0 % de l'extrait végétal investigué ont été soumises à des tests de stabilité préliminaires et accélérés. RÉSULTATS: L'extrait a montré une concentration totale de flavonoïdes (1.71 ± 0.26 µg EQ/mg) et des concentrations de composés phénoliques à 0.21 ± 0.01 mg EAG/g. Des métabolites tels que les flavonoïdes et les saponines ont été annotés, ainsi que certains de leurs dérivés glycosidiques respectifs. L'extrait a montré un potentiel antioxydant et la capacité d'inhiber la cascade d'oxydation tant dans les phases d'initiation que de propagation. De plus, l'extrait a présenté une inhibition notable de l'activité antityrosinase, avec un résultat de 62.48 ± 2.09 à une concentration de 30.00 mg/mL. Les formulations ont été stables lors des tests de stabilité accélérés sur une période de 60 jours. CONCLUSION: Cette recherche démontre scientifiquement le potentiel d'une plante du biome de la Caatinga avec des propriétés antioxydantes et antityrosinases dans le développement de produits cosmétiques visant les effets anti­âge et l'harmonisation de la couleur de la peau, tout en ajoutant de la valeur à la chaîne de production de P. juliflora. Cette valorisation englobe divers aspects incluant des responsabilités environnementales, sociales et liées à la biodiversité.

In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model.

CONTEXT: Metformin is an important oral anti-hyperglycemic used in diabetes. Polylactic-co-glycolic acid (PLGA) has been widely used due to its reliability in controlling the release of drugs. OBJECTIVE: This study evaluates the in vitro-in vivo availability of metformin hydrochloride-loaded polylactic-co-glycolic acid. MATERIAL AND METHODS: In vitro metformin release (Met-free or PLGA + Met-12.5 mg/mL per 360 min) was evaluated using static Franz vertical diffusion cells. The in vivo study was performed with two control groups (validation bioanalytical method) and two experimental groups of diabetic male Wistar rats treated with PLGA + Met 10 mg/kg or Met 100 mg/kg by oral gavage. Diabetes was induced by streptozotocin (40 mg/kg) through the penile vein. Blood samples were collected 0.5, 1, 4, 7, 10, 12, 18, 24, 36, 48 and 72 h and analysed by high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). RESULTS: PLGA + Met 10 mg/kg was released in the in vitro assay suggesting a parabolic diffusion kinetic model (K -0.0619-0.5h) with a 100% release profile in 10 h by controlled diffusion. The in vivo assay showed the apparent volume of distribution Vz/F (PLGA + Met 10 mg/kg, 40971.8 mL/kg vs. Met 100 mg/kg, 2174.58 mL/kg) and mean residence time MRTinf (PLGA + Met 10 mg/kg, 37.66 h vs. Met 100 mg/kg, 3.34 h). DISCUSSION AND CONCLUSIONS: The formulation modifies pharmacokinetics parameters such as apparent distribution volume and mean residence time. The PLGA + Met 10 mg/kg had a slower elimination rate compared to Met 100 mg/kg in diabetic rats in a periodontal disease experimental model.

Sequential pore wall functionalization in covalent organic frameworks and application to stable camptothecin delivery systems.

Post-synthetic modification of covalent organic frameworks (COFs) is strongly demanded in order to provide additional functionalities to their structures. However, the introduction of functional groups during the synthesis of two dimensional COFs (2D COFs) is highly discouraged, as they can interfere with the π-π stacking forces, compromising framework integrity. Here, we show that direct incorporation of nucleophyllic groups (e.g., primary amines) on pore wall during the synthesis of a 2D-COF (COF-5) is possible by sequential substitution of original monomers. Subsequent bonding of the antitumor drug camptothecin results in a stable hydrophobic drug delivery system. Water adsorption isotherms modelling indicates that the insertion of CPT ligand in the framework promotes a hydrophobic effect that protects a region of COF chain from boronate ester hydrolysis and resulting degradation, which is also proven by stability testing in physiological conditions. Furthermore, this hydrophobic nature favors cell internalization kinetics by promoting interactions with the lipophilic cell membrane. To the best of our knowledge, this is the first case of a stable drug delivery system based on covalently conjugated COFs.