Spheres with antioxidant properties

Description

1 / 7 SPHERES WITH ANTIOXIDANT PROPERTIES Field of invention

[001] The present invention relates to spheres synthesized from a sodium alginate solution supplemented with concentrations of 10%, 15% and 25% (w / w) of copper(II) crystal, 1,10-phenanthroline and L-isoleucine, and with various antioxidant properties, including the ability to eliminate DPPH and ABTS radicals, indicating that the material has the potential to reduce oxidative stress and prevent diseases such as arthritis, arteriosclerosis, cataracts, Alzheimer's, Parkinson's, heart attacks, and even premature aging. Fundamentals of the invention

[002] The properties of L-isoleucine when complexed with transition metals can increase antioxidant and even immunological capacity by reducing the activities of superoxide dismutase (SOD) and glutathione peroxidase. Studies also point to the accumulation of anthocyanin favoring the antidiabetic effect. (Zhao J, Feng L, Liu Y, Jiang W, Wu P, Jiang J, et al. Effect of dietary isoleucine on immunity, antioxidant status, tight junctions and gut microflora of juvenile Jian meat (Cyprinus carpio var. Jian). Fish and Shellfish Immunology. 2014;41(2):663-73.)

[003] The copper(II), 1,10-phenanthroline and Lysoleucine crystal was synthesized by Chen Shi and collaborators (Chen Shi, Le Xueyi, Zhou Xiaohua, Liu Xiaoping, Liu Guang CCDC 213583: Petition 870250013330, dated 02 / 18 / 2025, p. 7 / 18 2 / 7 Experimental Determination of Crystal Structure, 2005, DOI: 10.5517 / cc757sd.

[004] The literature indicates that the transport of drugs to specific application sites is favored through encapsulation in gelling agents that have low toxicity, high solubility, bioavailability, and that can promote the carrying and protection of the drug and its gradual release in the body. Thus, sodium alginate, being a water-soluble polysaccharide, was used to produce spheres of the copper(II), 1,10-phenanthroline, and L-isoleucine complex, enhancing the application of a future drug based on the material. (Baek K, Woo MR, Choi YS, Kang MJ, Kim JO, Choi HG, et al. Engineering sodium alginate microparticles with different crystallinities for niclosamide repositioning and solubilization to improve solubility and oral bioavailability in rats. International Journal of Biological Macromolecules. 2024;283:137471.)

[005] Based on this premise, the present invention relates to the production of spheres of the copper(II), 1,10-phenanthroline and L-isoleucine complex encapsulated in sodium alginate with antioxidant properties. Brief description of the drawings

[006] Based on the applied methodology, spheres of the copper(II), 1,10-phenanthroline and L-isoleucine complex encapsulated in sodium alginate with antioxidant properties were obtained in concentrations of 10%, 15% and 25% (w / w), depending on Petition 870250013330, dated 02 / 18 / 2025, page 8 / 18 3 / 7 of these concentrations showed the best results in both the synthesis and characterization tests.

[007] Figure 1 shows spheres of the copper(II) complex, 1,10-phenanthroline, L-isoleucine encapsulated in sodium alginate at concentrations a) 10% [Cu(II)-(1,10-phen)-(L-ile)]10%; b) 15% [Cu(II)-(1,10-phen)-(L-ile)]15% and c) 25% [Cu(II)-(1,10-phen)-(L-ile)]25%, which demonstrates the difference in the color of the spheres as a function of the crystal concentration, with a standard average size of 1 mm in diameter.

[008] Figure 2 shows the X-ray diffraction of spheres of the copper(II) complex, 1,10-phenanthroline and L-isoleucine encapsulated in sodium alginate at concentrations a) [Cu(II)(1,10-phen)-(L-ile)]10%; b) [Cu(II)-(1,10-phen)-(L-ile)]15%; and c) 25% [Cu(II)-(1,10-phen)-(L-ile)]25%. The diffractograms confirm the presence of the crystal in the matrix of the spheres, with the intensity of the crystalline peaks increasing proportionally to the increase in crystal concentration.

[009] Figure 3 presents the results obtained from the differential scanning calorimetry (DSC) curve of the spheres [Cu(II)-(1,10-phen)-(L-ile)]10%, [Cu(II)-(1,10-phen)-(L-ile)]15%, [Cu(II)-(1,10-phen)-(L-ile)]25%. The DSC curves for all crystal concentrations used confirm the presence of the complex in the polymer matrix with an endothermic dehydration event related to free and coordinate water existing in the material and other organic compounds in a range varying between 300 K and 750 K. The enthalpy involved in the process varies according to Petition 870250013330, dated 02 / 18 / 2025, page 9 / 18 4 / 7 with the concentration of copper(II) crystal, 1,10-phenanthroline and L-isoleucine. At 10%, ΔH = 91.45 kJ / mol, increasing to 383.41 kJ / mol with 15% and 395.41 kJ / mol with 25%. Therefore, due to the existing events and the amount of energy involved in the loss and dehydration process, the higher the concentration of the complex, the greater its potential for use as an antioxidant agent.

[010] Figure 4 shows the DPPH radical inhibition pattern of the copper(II), 1,10-phenanthroline, and L-isoleucine crystal encapsulated in sodium alginate and provides a comparison with the standard flavonoid rutin. The results indicate that the crystal has the potential to inhibit the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical with reduction capacities ranging from 15% to 40%, proportionally to the increase in the concentration of the study material. Compared to rutin, a flavonoid with antioxidant and anti-inflammatory properties found in foods such as grapes, apples, blackberries, and various citrus fruits, the copper(II), 1,10-phenanthroline, and L-isoleucine complex has the potential to replace this dietary supplement as an antioxidant agent, given that its method of obtaining it and reduced manufacturing cost would lower prices and popularize a possible drug based on the crystal.Furthermore, the spheres obtained can be applied to specific regions of the human body, reducing a number of problems caused by oxidative stress. Description of the invention

[011] The invention relates to spheres obtained from the solubility of sodium alginate with copper(II) crystals, Petition 870250013330, dated 02 / 18 / 2025, page 10 / 18 5 / 7 1,10-phenanthroline and L-isoleucine, in concentrations of 10%, 15% and 25%.

[012] Crystal synthesis: The crystal is synthesized by the slow solvent evaporation technique through the following steps: a) A solution of 1,10-phenanthroline (1 mmol) in 30 mL of water / methanol (50% / 50%) was prepared and subsequently added to an aqueous solution of 10 mL of copper(II) nitrate (1 mmol); b) Next, L-isoleucine (1 mmol) and sodium bicarbonate (1 mmol) were added to the solution from step a), and the mixture was stirred magnetically at 70°C for 3 hours; c) The solution formed in step b) is sealed with plastic film with small holes and left in an oven at a constant temperature of 35 °C, with the crystals obtained after 10 days.

[013] Sphere preparation: the polymeric spheres are obtained by incorporating copper(II) crystal, 1,10phenanthroline and L-isoleucine, at concentrations of 10%, 15% and 25% (w / w), into solutions containing 90%, 85% and 75% sodium alginate, respectively, and stirring for 24 hours. At the end of this period, the resulting solutions are added dropwise to calcium chloride solutions (1%) to form the spheres. Petition 870250013330, dated 02 / 18 / 2025, page 11 / 18 6 / 7

[014] Another aspect of the present invention is that the spheres are characterized by the following formulations: - Formulation 1: 90% sodium alginate solution in deionized water; 10% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2); - Formulation 2: Formulation 1: 85% sodium alginate solution in deionized water; 15% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2); - Formulation 3: 75% sodium alginate solution in deionized water; 25% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2). Examples of how the invention can be implemented

[015] Figure 1 shows the spheres formed from the solubility of the copper(II) complex, 1,10-phenanthroline and lysoleucine and sodium alginate. From the concentrations used of the crystal, it is possible to observe a variation in the intensity of the spheres' color, which is proof of the incorporation of the crystal into the polymeric matrix. The standard average size of 1.0 mm in diameter obtained in the encapsulation favors its use as a drug, since they are suitable for absorption by the body.

[016] Figure 2 shows the X-ray diffraction of the spheres obtained, which confirms the presence of the crystal. Petition 870250013330, dated 02 / 18 / 2025, page 12 / 18 7 / 7 copper(II), 1,10-phenanthroline and L-isoleucine, since the polymer matrix contains crystalline peaks corresponding to the ternary complex.

[017] The DSC curves shown in Figure 3 present the enthalpy values ​​involved in the dehydration process of the spheres in a temperature range that varies from 300K to 750K°, with the endothermic events proving the existence of organic compounds in the polymeric matrix.

[018] Figure 4 shows the DPPH radical inhibition potential of copper (II) crystal, 1,10-phenanthroline and L-isoleucine and provides a comparison with the standard flavonoid rutin. It can be observed that the material inhibits this radical in a manner proportional to the concentration used. Petition 870250013330, dated 02 / 18 / 2025, page 13 / 18

Claims

1 / 1 CLAIMS 1. SPHERES WITH ANTIOXIDANT PROPERTIES, characterized by comprising a solution of sodium alginate and copper(II) crystal, 1,10-phenanthroline and L-isoleucine in powder form, in concentrations of 10%, 15% and 25%, specifically defined by the following formulations: - Formulation 1: 90% sodium alginate solution in deionized water; 10% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2); - Formulation 2: Formulation 1: 85% sodium alginate solution in deionized water; 15% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2); - Formulation 3: 75% sodium alginate solution in deionized water; 25% copper(II) crystal, 1,10-phenanthroline and L-isoleucine and 1% calcium chloride (CaCl2).

2. SPHERES WITH ANTIOXIDANT PROPERTIES, according to claim 1, characterized by the average size of the spheres being 1.0 mm in diameter. Petition 870250013330, dated 02 / 18 / 2025, page 14 / 18

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