Programa de Pós-Graduação em Ciências Farmacêuticas
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Master Thesis Nanoemulsões contendo fitol como alternativa farmacológica para o tratamento da leishimaniose cutânea(Universidade Federal do Rio Grande do Norte, 2022-12-12) Freire, Victoria Louise Pinto; Silva Júnior, Arnóbio Antonio da; Silva, Marcelo de Sousa da; https://orcid.org/0000-0002-7516-1787; http://lattes.cnpq.br/2593509584288129; http://lattes.cnpq.br/8701522182756219; Andrade Neto, Valter Ferreira de; Oliveira, Douglas Dourado; Nascimento, Ednaldo Gomes doLeishmaniasis is considered one of the main neglected diseases in the world, with large numbers of cases annually, it is caused by protozoa of the genus Leishmania spp. and affects mainly populations in poorer countries. The treatment of the disease is very limited, toxic to the patient, high cost and the parasite is resistant to chemotherapy. In this way, trying to solve problems such as the side effects of drugs already in use, reducing drug resistance and improving existing treatments, pharmaceutical nanotechnology appears with drug delivery systems on a nanometric scale, as is the case of nanoemulsions (NE). At the same time, alternative leishmanicidal active principles have been sought to treat the disease, such as phytol, which is a component of chlorophyll from the diterpene class, which is found abundantly in nature and has a wide range of proven biological activities. Thus, the present study aims to develop NE containing biocompatible phytol by the phase inversion emulsification technique, to evaluate the effect of the composition on the physical-chemical parameters of the nanoemulsions, to observe the long-term and accelerated stability of the systems obtained with and without the active one, also observe the cytocompatible profile in 3T3 cells, the hemolytic potential in erythrocytes and the in vitro capacity of these antileishmanial systems. Thus, it was observed that the EN developed were stable for up to 30 days and under high stress conditions with centrifugations at high rotations showing adequate macroscopic and physical-chemical parameters. A cytocompatible profile was also observed at up to 70% in the concentrations tested with the cell line tested and in the hemolysis assay only showed hemolysis in the initial concentrations, suggesting safety for administering the system in an in vivo study. It was also observed that the developed EN had a good and timedependent activity. Therefore, the NE produced proved to be a promising drug for the treatment of cutaneous leishmaniasis, proving to be safe and effective.Master Thesis Efeito ansiolítico da nanoemulsão de óleo de girassol contendo fitol em ratas wistar expostas ao labirinto em cruz elevado(Universidade Federal do Rio Grande do Norte, 2024-12-19) Almeida, Hélida Maravilha Dantas e Sousa; Silva Júnior, Arnóbio Antonio da; Silva, Alianda Maira Cornelio da; https://orcid.org/0000-0002-7516-1787; http://lattes.cnpq.br/2593509584288129; https://orcid.org/0000-0001-9749-784X; http://lattes.cnpq.br/6950044006557333; Souza, Daniela Baptista de; Pedrosa, Matheus de Freitas FernandesPhytol, a diterpene with notable effects on the central nervous system, has demonstrated anxiolytic properties in Swiss mice subjected to the elevated plus maze. Despite these findings, limited research has explored the impact of phytol nanoemulsions in animal models of anxiety, particularly in females. The present study aims to evaluate the effects of phytol incorporated into a sunflower oil nanoemulsion on rats exposed to the elevated plus maze. The formulation was developed using the phase inversion method, varying phytol concentration within the oil phase. The most stable formulation, containing the highest diterpene concentration, underwent extensive physicochemical characterization, including droplet size, polydispersity index (PDI), zeta potential, and pH over 35 days. Characterization techniques included fourier transform infrared spectroscopy, transmission electron microscopy, and chromatographic analysis. Additionally, the formulation was tested for hemolytic activity and antioxidant capacity using the DPPH assay and evaluated for its biocompatibility and delivery to the brain using a chicken embryo model. In vivo studies were performed in Wistar rats, with the animals divided into treatment groups (vehicle; diazepam 2 mg/kg; phytol 25 mg/kg; phytol 75 mg/kg; blank nanoemulsion; phytol nanoemulsion 25 mg/kg; and phytol nanoemulsion 75 mg/kg) administered via intraperitoneal injection. The physicochemical analysis revealed that the highest achievable phytol concentration in the nanoemulsion was 2.5%, with an average droplet size of approximately 160 nm, a PDI of 0.235, and a negative zeta potential of -27 mV, showing stability for over 30 days. Behaviorally, a significant reduction in anxiety-like behaviors was observed, as evidenced by increased entries and time spent in the open arms of the maze for rats treated with both the blank and phytol nanoemulsions at varying concentrations, compared to the vehicle group and the free phytol treatment at 25 mg/kg. These findings suggest that the phytol nanoemulsion formulation exhibits superior anxiolytic efficacy compared to the free phytol, highlighting the potential therapeutic advantage of the nanoemulsion system.Doctoral Thesis Resíduo agroindustrial de Agave sisalana como um inovador insumo cosmético antioxidante: avaliação in vitro e in vivo(Universidade Federal do Rio Grande do Norte, 2022-12-20) Barreto, Stella Maria Andrade Gomes; Ferrari, Márcio; Giordani, Raquel Brandt; http://lattes.cnpq.br/5032750980466610; https://orcid.org/0000-0002-2425-7586; http://lattes.cnpq.br/5782539548696465; https://orcid.org/0000-0001-7830-626X; http://lattes.cnpq.br/2234955265649411; Lima, Adley Antonini Neves de; https://orcid.org/0000-0002-3798-3915; http://lattes.cnpq.br/4061809277935577; Damasceno, Gabriel Azevedo de Brito; Tavares, Josean Fechine; Isaac, Vera Lucia BorgesAgave sisalana (sisal) is a plant extensively cultivated in the northeast region to obtain a hard fiber used to produce string and rope. However, only a small portion of the gross weight of sisal leaves is used, and the rest is discarded as residue. This residue has metabolites with potential antioxidant activity in its chemical constitution. In view of this, the objective of this work was, from the residue of A. sisalana, to obtain and characterize a hydroethanolic and a purified absorption, to evaluate the antioxidant potential in vitro and in vivo and to develop a nanoemulsion for carrier fractions to be applied as a cosmetic product antioxidant. From the residue, a recipe rich in polysaccharides (FRE) were received and, from the FRE, another recipe was through ultrafiltration dialysis (FREP). The qualitative composition was evaluated using liquid chromatography coupled to mass spectrometry (LC-MS). Both fractions were evaluated for their antioxidant activity in vitro, using different spectrophotometric techniques, culture medium and in vivo, using the Caenorhabditis elegans model. Furthermore, an experimental factorial design (2³+3PC) was designed to obtain a nanoemulsified system and its stability evaluated. FRE and FREP are mainly composed of terpenoids and O-glycosylated metabolites. FRE showed greater ability to directly inhibit DPPH and ABTS radicals, while FREP showed greater metal chelating activity (Cu2+ and Fe2+). The two fractions promote a protective effect against oxidative stress in 3T3 cells. In C. elegans models, FRE and FREP promoted intracellular reduction of ROS and increased survival representation. The expression of gst-4:GFP was positive for FRE whereas, for FREP, a reduction in expression was observed. The nanoemulsion consisting of 20% oil phase, 5% surfactants and 75% aqueous phase was considered stable for 90 days at different temperatures. The use of sisal residue as a new antioxidant input for the cosmetic industry can bring environmental benefits and contribute to the socioeconomic development of the region.Master Thesis Desenvolvimento e caracterização de formulações larvicidas contendo derivado do ácido cinâmico para o combate ao Aedes aegypti(Universidade Federal do Rio Grande do Norte, 2020-04-13) Almeida, Addison Ribeiro de; Aragão, Cícero Flávio Soares; Ferreira, Leandro de Santis; Albernaz, Lorena Carneiro; Langassner, Silvana Maria ZucolottoThe main strategy for controlling diseases transmitted by the Aedes aegypti mosquito is the elimination of the vector, mainly in its larval stage. Commercial larvicides and insecticides shows environmental toxicity. In this context, natural products show as alternatives to solve this problem. The aim of this study was to develop and characterize formulations containing pentyl cinnamate and evaluate its larvicidal activity for Aedes aegypti. The pentyl cinnamate was obtained by semisynthesis through the esterification of cinnamic acid. This compound was characterized and its purity determined by NMR 1H e 13C, GC-MS and UHPLCMS/MS. Pentyl cinnamate activity tests were performed on L3 larvae and on adult mosquitoes of A. aegypti, obtaining a larvicidal activity with LC50 of 19.9 μg.mL-1 , and against adult mosquitoes at a dose of 200 μg per bottle test, 80.8 ± 3.8% mortality in 2 h. Nanoemulsions were produced with PHOSAL® 50+ (PHO), LIPOID® S 20 (L20) and LIPOID® S 75-3 (L75) lecithins by homogenization with mechanical agitation and ultra turrax. The nanoemulsions were subjected to spray drying to obtain solid microparticles, which were characterized by FTIR, SEM and thermal analysis by DSC and TG. The nanoemulsions obtained by agitation with turrax showed smaller droplet sizes, being that of PHO: 81.0 ± 1.8 nm; L20: 120.4 ± 4.9 nm and L75 with 150.9 nm. The PHO nanoemulsions proved to be the most stable during 30 days of observation, they were also the ones that showed higher content of pentyl cinnamate whith 66.0 ± 0.5%. The images obtained by SEM showed that the microparticles formed by the different lecithins had a similar aspect between them. In the FTIR spectra, stretching signals characteristic of the pentyl cinnamate and excipients were observed and by DSC and TG techniques it was possible to see an increase in the stability of the compound incorporated in solid microparticles. The preliminary study of toxicity in zebrafish showed evidence of toxicity of pentyl cinnamate in low concentrations, however, future studies must be carried out for the influence of the solvent in this type of model. The nanoemulsions and microparticles produced proved to be suitable for making the use of this ester in water with potential use as a larvicide and adulticide feasible, opening perspectives for studies with other compounds.Master Thesis Utilização do subproduto do beneficiamento do sisal (Agave sisalana Perrine): desenvolvimento de nanoemulsões cosméticas e avaliação da segurança e eficácia(2017-03-31) Barreto, Stella Maria Andrade Gomes; Ferrari, Márcio; Giordani, Raquel Brandt; ; http://lattes.cnpq.br/5032750980466610; ; http://lattes.cnpq.br/5782539548696465; ; http://lattes.cnpq.br/2234955265649411; Rocha, Hugo Alexandre de Oliveira; ; http://lattes.cnpq.br/4651814546820796; Isaac, Vera Lúcia Borges; ; http://lattes.cnpq.br/4842462513285606The processing of the leaves of Agave sisalana provides fiber, with added value for the sisal industry, and the rest of the plant material, known as by-product, is thrown and generates environmental impact. Different applications have been attributed, however, there are no scientific researches that aim to use this product as a cosmetic raw material. The objective of this research was to obtain and characterize polysaccharides-enriched fraction (FrE) from the Agave sisalana by-product of, assess the safety in vitro and in vivo, as well as to evaluate the antioxidant activity in vitro, and then to develop a nanoemulsion with moisturizer effect. From the liquid portion of the by-product obtained the crude extract (EB) and two fractions resulting from extractive process. The EB and the fractions were evaluated for the presence of sugars, proteins and polyphenols. Safety was evaluated by cytotoxicity and phototoxicity in vitro assays using the colorimetric method of Neutral Red. Irritability was evaluated by the primary contact test (patch test). The antioxidant capacity was assessed using the DPPH scavenging tests and molybdenum method. Different systems were obtained by means of pseduodiagrama ternary containing, or not, 0.5% FrE. The selected formulations were submitted to preliminary stability tests and accelerated in different temperatures conditions for a period of 90 days. The moisturizing efficacy was evaluated by water content of the stratum corneum and transepidermal water loss for a period of 5 hours. The samples presented as chemical constituents, sugars, polyphenols and proteins. The FrE showed no phototoxic potential or cytotoxic, and was not irritating to skin of volunteers and can be considered an asset with antioxidant property Nanoemulsion containing 40% oil phase, 50% aqueous phase and 10% surfactants was stable for 90 days.The nanoemulsion was able to significantly increase the water content and maintain skin barrier function after 5 hours from a single application. The fraction obtained from the industrial by-product of Agave sisalana demonstrated a promising profile as raw material for cosmetic skin care with moisturizing and antioxidant capacity, together with the possibility of adding value to industrial waste, reducing the damage caused to the environment by disposing of this material.