DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Melaleuca leucadendron (L.) L. flower extract exhibits antioxidant and photoprotective activities in human keratinocytes exposed to ultraviolet B radiation.(2020) Silva, Luan Silvestro Bianchini; Perasoli, Fernanda Barçante; Carvalho, Karen Vitor; Vieira, Karla Murata; Lopes, Miriam Teresa Paz; Souza, Gustavo Henrique Bianco de; Santos, Orlando David Henrique dos; Freitas, Katia MichelleRecently, there has been a demand for the replacement of chemical sunscreens with natural compounds that could prevent or restore UV-induced skin damage. Here, we investigated the photoprotective influence of the Melaleuca leucadendron ethanolic flower extract (EEMec) on factors involved in cellular and molecular UVBinduced oxidative stress in human skin keratinocytes (HaCaT). The phytochemical constituents, antioxidant potential by DPPH assay, content of total phenolic and flavonoid compounds in EEMec were evaluated. HaCaT cells were treated with EEMec followed by irradiation with UVB. CAT activity; GSH and ROS levels; and SOD1, GPx, CAT and COX-2 expression assays were employed to verify the oxidative stress, as well as EEMec effect on transmembrane transport, and pro-inflammatory and pro-apoptotic protein expression. EEMec reverted the viability loss of HaCaT cells after irradiation with UVB, exhibited significant antioxidant capacity and free radical scavenging activity in vitro, inhibited COX-2 expression and ensure protection of DNA-damage. EEMec shown a great photoprotective property to prevent keratinocytes damage induced by UV radiation and, thus a candidate potential to application as an adjuvant in sunscreen formulations as a strategy to reduce risk of sunburn and prevent skin diseases associated with UV-induced inflammation and cancer.Item Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid : development, characterization, and antimalarial activity.(2020) Silva, Marina Goulart da; Cardoso, Jéssica Ferreira; Perasoli, Fernanda Barçante; Branquinho, Renata Tupinambá; Mourão, Renata Silva; Tavares, Harley da Silva; Xocaira, Maria Luiza Costa Trench; Guimarães, Daniel Silqueira Martins; Viana, Gustavo Henrique Ribeiro; Varotti, Fernando de Pilla; Silva, Gisele Rodrigues daMalaria treatment is based on a reduced number of antimalarial drugs, and drug resistance has emerged, leading to the search for new antimalarial drugs incorporated into pharmaceutical formulations. In this study, 10-(4,5- dihydrothiazol-2-yl)thio)decan-1-ol) (thiazoline), a synthetic analog of 3-alkylpiridine marine alkaloid, and a potent antimalarial substance, was incorporated into O/W nanoemulsion. This formulation was prepared by a 23 factorial design. It was characterized by globule diameter, polydispersity index, zeta potential, encapsulation efficiency, in vitro thiazoline release at pH 2 and 6.86, and accelerated stability. In vitro and in vivo antimalarial activity was determined against P. falciparum and P. berghei, respectively. Thiazoline nanoemulsion showed 248.8 nm of globule diameter, 0.236 of polydispersity index, -38.5 mV of zeta potential, 96.92% encapsulation efficiency, and it was stable for 6 months. Thiazoline release profiles differed in acidic and neutral media, but in both cases, the nanoemulsion controlled and prolonged the thiazoline delivery. Thiazoline nanoemulsion exerted in vitro antimalarial activity against the parasite (IC50 = 1.32 µM), and it significantly reduced the in vivo parasitemia for 8 days without increasing the survival time of animals. Therefore, the thiazoline nanoemulsion represents a strategy to treat malaria combining an antimalarial candidate and a new nanocarrier.Item Desenvolvimento de nanoemulsão fotoprotetora de Passiflora edulis.(2019) Almeida, Juliana Cristina dos Santos; Ribeiro, Thascilaine de Souza; Silva, Luan Silvestro Bianchini; Perasoli, Fernanda Barçante; Figueiredo, Bruna Inez Carvalho de; Carvalho, Karen Vitor; Dôres, Rosana Gonçalves Rodrigues das; Souza, Gustavo Henrique Bianco de; Santos, Orlando David Henrique dosO surgimento de inúmeras doenças, como o câncer de pele e o fotoenvelhecimento estão relacionados com a radiação solar em excesso, constituindo um considerável problema de saúde pública. O desenvolvimento fotoprotetores têm sido estimulado com o intuito de proteger a pele dos efeitos nocivos da radiação ultravioleta (UV). O objetivo do presente trabalho foi avaliar o potencial fotoprotetor (FPS) do extrato etanólico bruto (EB) de Passiflora edulis; a associação com a nanoemulsão e a atividade fotoprotetora; além de caracterizar as nanoemulsões quanto ao diâmetro médio, índice de polidispersão (IP) e potencial zeta. Foram desenvolvidas três nanoemulsões tópicas para incorporação do extrato a 0,5%. As nanoemulsões foram avaliadas visualmente quanto à aparência macroscópica 24 horas após o preparo, observando a presença ou não de sinais de instabilidade, como precipitação e separação de fases. Na formulação A, B e C, o extrato bruto foi solubilizado em Croduret, PEG e DMSO, respectivamente. O FPS foi determinado pelo método espectrofotométrico. Visualmente, a formulação A incorporou 100% do EB adicionado e apresentou-se estável após 24 horas. Entretanto, as formulações B e C não incorporaram todo o EB adicionado, ocasionando em separação das nanoemulsões em duas fases. O FPS foi determinado para o extrato etanólico bruto e para a formulação A. Para o extrato etanólico, o valor de FPS encontrado foi igual 11 e para a formulação A antes e após a incorporação do EB, FPS 4 e FPS 20, respectivamente. O diâmetro médio da formulação A sem e com extrato foi de 70,24 ± 0,12 nm e 72,10 ± 0,39 nm, respectivamente, indicando que não houve mudança significativa do diâmetro médio da nanoemulsão após a incorporação do EB. O IP da formulação A antes e após a adição de EB foi inferior a 0,3, caracterizando as mesmas como monodispersas. Os resultados apresentados mostraram que a associação do EB à formulação A resultou no aumento da sua atividade fotoprotetora.Item Amphotericin B-loaded Eudragit RL100 nanoparticles coated with hyaluronic acid for the treatment of vulvovaginal candidiasis.(2020) Melo, Carolina Mirtes; Cardoso, Jéssica Ferreira; Perasoli, Fernanda Barçante; Oliveira Neto, Ari Soares de; Pinto, Luccas Moreira; Marques, Maria Betânia de Freitas; Mussel, Wagner da Nova; Magalhães, Juliana Teixeira de; Moura, Sandra Aparecida Lima de; Araújo, Marcelo Gonzaga de Freitas; Silva, Gisele Rodrigues daThe treatment of vulvovaginal candidiasis (VVC) is based on oral and vaginal formulations which show limited effectiveness. In this study, amphotericin B-loaded Eudragit RL100 nanoparticles coated with hyaluronic acid (AMP EUD nanoparticles/HA) were developed to overcome the drawbacks of the conventional formulations. AMP EUD nanoparticles/HA were synthesized by nanoprecipitation, formulated by statistical experimental design, and characterized. AMP release from EUD nanoparticles/HA and its antifungal activity in a murine model of VVC were evaluated. Nanoparticles showed 147.6 ± 16.7 nm of diameter, 0.301 ± 0.09 of polydispersity index, - 29.9 ± 3.76 mV of zeta potential, and 87.27 % of encapsulation efficiency. They released about 81 % of AMP in 96 h; and provided the elimination of 100 % of the vaginal fungal burden in 24 h. It was suggested that the AMP EUD nanoparticles/HA penetrated into the vaginal epithelium via CD44 receptors. These AMP EUD nanoparticles/HA represent a non-conventional vaginal formulation to improve the treatment of VVC.Item Implants composed of digoxin and poly(ε-caprolactone) : development, characterization, anti-proliferative and anti-angiogenic activities.(2017) Rodrigues, Felipe Fernandes; Braz, Wilson Rodrigues; Perasoli, Fernanda Barçante; Ferreira, Letícia Gonçalves Resende; Barbosa, Leandro Augusto de Oliveira; Silva, Gisele Rodrigues daDrug delivery systems could be applied to locally treat cervical cancer, thus preventing the drawbacks of conventional therapy. In this study, anti-proliferative and anti-angiogenic effects of digoxin incorporated into poly(ε-caprolactone) implants were evaluated, aiming at the local treatment of cervical cancer. Implants were characterized, and the in vitro release profile of digoxin was demonstrated. Anti-proliferative and anti-angiogenic activities of digoxin were investigated by using chorioallantoic membrane and human cervix carcinoma (HeLa) cells, respectively. The chemical structure of digoxin and the semi-crystalline nature of poly(ε-caprolactone) were preserved after designing implants. The hydrophobicity of drug and polymer as well as the semi-crystalline structure provided a controlled diffusion of digoxin from implants. Digoxin released from implantable devices exhibited anti-proliferative activity against HeLa cells. The anti-angiogenic effect was also shown. Finally, implants composed of digoxin and poly(ε-caprolactone) could be applied as a therapeutic alternative to treat the early stage of cervical cancer, once they were able to locally control the release of this anti-angiogenic and anti-proliferative drug, minimizing its systemic side effects and toxicity.