This paper describes the investigation and development of a novel magnetic drug delivery nanosystem (labeled as MO-20) for cancer therapy. The drug employed was oncocalyxone A (onco A), which was isolated from Auxemma oncocalyx, an endemic Brazilian plant. It has a series of pharmacological properties: antioxidant, cytotoxic, analgesic, anti-inflammatory, antitumor and antiplatelet. Onco A was associated with magnetite nanoparticles in order to obtain magnetic properties. The components of MO-20 were characterized by XRD, FTIR, TGA, TEM and Magnetization curves. The MO-20 presented a size of about 30 nm and globular morphology. In addition, drug releasing experiments were performed, where it was observed the presence of the anomalous transport. The results found in this work showed the potential of onco A for future applications of the MO-20 as a new magnetic drug release nanosystem for cancer treatment.
1 January 2023 in Brazilian Archives of Biology and Technology
This article aims to report the preparation and optimized formulation of Ctn[15-34], a designed anti-infective peptide, with poly(lactic acid-co-glycolic acid), PLGA, nanoparticles. Ctn[15-34] is a short peptide derived from crotalicidin, a cathelicidin-related antimicrobial peptide from the venom of the South American rattlesnake (Crotalus durissus terrificus), that has arisen as a promising antifungal and microbicide agent. The PLGA nanoparticles were prepared and loaded with carboxyfluorescein (CF)-Ctn[15-34] using the double emulsion/solvent evaporation method. After a preformulation study, which tested different formulation parameters, Poly (vinyl alcohol) 87-89% hydrolyzed and sonication with Sonifier® were choosen to prepare unloaded PLGA nanoparticles by that method, resulting in smaller particle size and Polydispersity Index (PDI) values and higher zeta potential values of nanoparticles. This better condition was used to prepare CF-Ctn[15-34]-loaded PLGA nanoparticles, resulting in homogeneous and spherical nanoparticles, with an average size of 213.2 ± 2.00 nm, PDI of 0.044 ± 0.04 and zeta potential of -16.03 ± 1.20 mV. An excellent encapsulation efficiency was obtained, corresponding to 93.3 ± 0.10 %. The drug-release profile showed a rapid initial release of the peptide, approximately 27 % in the first 24 hours, followed by a sustained release for at least 16 days. Another relevant aspect in the peptide formulation is that the CF-Ctn[15-34]-loaded nanoparticles potentiated the antifungal effect against the opportunistic pathogenic yeast Cryptococcus neoformans compared with the free, in solution Ctn[15-34], in equivalent volume dosage. A preparation method of CF-Ctn[15-34]-loaded PLGA nanoparticles was established and validated, representing a successful approach to deliver CF-Ctn[15-34] for pharmaceutical applications.
Myracrodruon urundeuva, popularly known as 'aroeira-do-sertão', a large tree, with a tall trunk. Belonging to the Anacardiaceae family, it occurs in the 'caatinga' and dry forests of Brazil, from Ceará to the states of Paraná and Mato Grosso do Sul. The present study aimed to analyse the whitening and antioxidant activities of the aqueous extract of the leaves of Myracrodroun urundeuva (AELMU). Inhibition of the tyrosinase enzyme, as well as its copper chelating capacity and antioxidant effect were evaluated. The AELMU (at 2000 µg/mL) showed excellent inhibitory action (83.76%) on tyrosinase by chelating the copper ion while kojic acid at the same concentration inhibited 97.81%. Moreover, the extract displayed important antioxidant activity (inhibited 76,46% of the 2,2-diphenyl-1-picrylhydrazyl radical - DPPH; 49,59% of thiobarbituric acid reactive substances and 51,07% of the hydroxyl radical). Thus, the extract under study is promising for use in cosmetics, given its multifactorial action.
In this study, the spray drying technique was used to prepare L-ascorbic acid (AA) microparticles encapsulated with galactomannan-an extract from the seeds of the Delonix regia species. The physico-chemical characteristics, antioxidant activity, and encapsulation efficiency of the AA microparticles were evaluated and characterized using thermogravimetric analysis, differential scanning calorimetry, infrared spectroscopy, X-ray diffraction, and scanning electron microscopy. The free-radical scavenging activity of the AA microparticles was determined at different environmental conditions using DPPH (1,1-diphenyl-2-picryl-hydrazyl). X-ray diffraction measurements demonstrated a loss of crystallinity in AA after the encapsulation process, and a DSC scan also showed the loss of the compound's melting peak. Thermogravimetric analysis showed small differences in the thermal stability of galactomannan before and after the incorporation of AA. The mean diameters of the obtained spherical microspheres were in the range of 1.39 ± 0.77 µm. The encapsulation efficiency of AA microparticles in different environmental conditions varied from 95.40 to 97.92, and the antioxidant activity showed values ranging from 0.487 to 0.550 mg mL-1
O objetivo desse estudo foi formular e avaliar comprimidos de liberação controlada. Comprimidos de liberação controlada de teofilina foram preparadas pelo método de compressão direta usando dois polímeros como, o HPMC K 100M (polímero hidrofílico) e a Goma Guar (Polímero natural), isolado ou em mistura (GG:HPMC 3:1) e GG:HPMC 1:3). Os comprimidos foram caracterizados através do peso médio, diâmetro, altura, dureza, friabilidade. Todos os resultados estiveram em conformidade com os limites aceitáveis. O ensaio de intumescimento foi realizado em água destilada durante 4 horas, sendo determinado pela diferença de peso do comprimido seco e intumescido. O ensaio de dissolução foi realizado em água destilada (900 mL, 37 ± 0,5ºC, 50 rpm, aparato II) durante 8 horas. Os resultados demonstraram que a Goma guar isolada não possui capacidade de retardar a liberação da teofilina por 8 horas. Comprimidos matriciais contendo GG:HPMC (3:1) apresentaram um melhor controle de liberação da teofilina.
In the pharmaceutical industry, the fruits of the fava d'anta are used to extract quercetin and rutin, which are the basis for the production of medicines that work to treat varicose veins, hemorrhoids, circulatory system disorders and a variety of other conditions. The aim of this article is to carry out a comprehensive review of the chemical constitution and pharmacology of fava d'anta. This is an integrative review using the following databases: Embase, SciElo, LILACS, CAPES Periodicals and Medline, with the search expression “Dimorphandra gardneriana” OR “Dimorphandra mollis”. Studies were selected without any restrictions on language or time of publication, in order to conduct the most comprehensive search possible. A total of 278 articles were identified, of which 72 were viewed on Embase, 31 on Scielo, 19 on LILACS, 114 on CAPES and 42 on Medline. After reviewing the titles, abstracts and removing duplicates, 13 articles were obtained for full text analysis. The studies analyzed showed various pharmacological activities of the compounds extracted from the D. mollis and D. gardneriana species, including antioxidant, anti-inflammatory, neuroprotective, antiviral and lipid metabolism modulating properties. Thus, the presence of the flavonoids rutin and quercetin reinforces the potential of these species for therapeutic applications.