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Magalhäes, Nereide Stela Santos
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Id: biblio-973857
Autor: Ferreira, Kaline Sandrelli Amorim; Santos, Bruna Marília Alves dos; Lucena, Nelise de Paiva; Ferraz, Milena Sales; Carvalho, Rafaela de Siqueira Ferraz; Duarte Júnior, Anivaldo Pereira; Magalhães, Nereide Stela Santos; Lira, Rodrigo Pessoa Cavalcanti.
Título: Ocular delivery of moxifloxacin-loaded liposomes / Perfil de liberação ocular de lipossomas contendo moxifloxacino
Fonte: Arq. bras. oftalmol;81(6):510-513, Nov.-Dec. 2018. graf.
Idioma: en.
Resumo: ABSTRACT Purpose: To determine the release profile of moxifloxacin encapsulated in liposomes in the aqueous humor as a controlled release system for intracameral application. Methods: Liposomes containing moxifloxacin were obtained using the lipid film hydration method and were characterized by particle size and encapsulation efficiency. Female rabbits were used for the in vivo profile release study. Liposomes containing moxifloxacin was injected into the anterior chamber of the right eye of each animal. The rabbits were divided into five groups, and a sample of aqueous humor was collected 2, 4, 8, 24, and 48 h after administration of liposomes containing moxifloxacin administration. Moxifloxacin concentrations in the aqueous humor were analyzed using high-performance liquid chromatography. Results: The average size of the liposomes containing moxifloxacin was 60.5 ± 0.72 nm with a particle size distribution of 0.307. The encapsulation efficiency of moxifloxacin in liposomes was 92.24 ± 0.24%. The results of an in vivo release study of liposomes containing moxifloxacin, showed that the maximum moxifloxacin concentration was achieved within the first 2 h after administration (5.27 ± 1.09 mg/mL) and was followed by a decrease in intracameral concentration (0.35 ± 0.05 mg/mL) until the 24 h mark. Conclusions: The in vivo experiments resulted in liposomes containing moxifloxacin that were homogenous in size and exhibited high drug encapsulation efficiency. The results indicate that liposomes containing moxifloxacin offers a satisfactory aqueous humor release profile after intracameral application.

RESUMO Objetivo: Determinar o perfil de liberação, no humor aquoso, de moxifloxacino encapsulado em lipossomas como um sistema de liberação controlada para aplicação intracameral. Métodos: Lipossomas contendo moxifloxacino foram obtidos através do método de hidratação do filme lipídico e caracterizados por tamanho da partícula e eficiência de encapsulação. Utilizaram-se coelhos fêmeas foram para o estudo do perfil de liberação in vivo. Lipossomas contendo moxifloxacino foram injetados na câmara anterior do olho direito de cada animal. Os coelhos foram divididos em cinco grupos, e uma amostra de humor aquoso foi coletada 2, 4, 8, 24 e 48 h após a administração de lipossomas contendo moxifloxacino. As concentrações de moxifloxacino no humor aquoso foram analisadas usando cromatografia líquida de alta eficiência. Resultados: O tamanho médio dos lipossomas contendo moxifloxacino foi de 60,5 ± 0,72 nm com uma distribuição de tamanho de partícula de 0,307. A eficiência de encapsulação de moxifloxacino nos lipossomas foi de 92,24 ± 0,24. Os resultados de um estudo de liberação in vivo de lipossomas contendo moxifloxacino, mostraram que a concentração máxima de moxifloxacino foi atingida dentro das primeiras 2 h após sua administração (5,27 ± 1,09 mg/mL) e foi seguida de um decréscimo na concentração intracameral (0,35 ± 0,05 mg/mL) até a marca de 24 h. Conclusão: Os experimentos in vivo resultaram em lipossomas contendo moxifloxacino que eram homogêneos em tamanho e exibiam alta eficiência de encapsulação do fármaco. Os resultados indicam que lipossomas contendo moxifloxacino oferecem um perfil de liberação de humor aquoso satisfatório após a aplicação intracameral.
Descritores: Humor Aquoso
Sistemas de Liberação de Medicamentos/métodos
Moxifloxacina/administração & dosagem
Antibacterianos/administração & dosagem
-Disponibilidade Biológica
Cromatografia Líquida de Alta Pressão
Modelos Animais
Injeções Intraoculares
Moxifloxacina/análise
Moxifloxacina/farmacocinética
Lipossomos
Antibacterianos/análise
Antibacterianos/farmacocinética
Limites: Animais
Feminino
Ratos
Responsável: BR1.1 - BIREME


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Id: lil-619656
Autor: Reimão, Juliana Quero.
Título: Estudo da atividade Anti-Leishmania e Anti-Trypanosoma Cruzi de bloqueadores de canal de cálcio, furazolidona e buparvaquona: reposicionamento, associações de fármacos e formulações lipossomais / Study of the antileishmanial and Anti-Trypanosoma cruzi activity of calcium channel blockers, furazolidone and buparvaquone: drug repurposing, drug combinations and liposomal formulations.
Fonte: São Paulo; s.n; 2012. [248] p. ilus, tab, graf.
Idioma: pt.
Tese: Apresentada a São Paulo(Estado) Secretaria da Saúde. Coordenadoria de Controle de Doenças. Programa de Pós Graduação em Ciências para obtenção do grau de Doutor.
Resumo: A pesquisa de medicamentos mais eficazes e que atendam aos padrões atuais de segurança é considerada uma prioridade para o tratamento da leishmaniose e doenças de Chagas. Os principais objetivos do presente trabalho foram: avaliar a atividade anti-Leishmania in vitro e in vivo de bloqueadores de canal de cálcio (BCC) e dos fármacos buparvaquona e furazolidona; realizar combinações de BCC com os principais fármacos usados na clínica da leishmaniose visceral (LV); desenvolver formulações lipossomais de buparvaquona, furazolidona e nimodipino e desenvolver um protocolo de PCR em tempo real (qPCR) visando quantificar a carga parasitária de hamsteres infectados com L. (L.) infantum chagasi após tratamento experimental. Buparvaquona, furazolidona e doze dos treze BBC testados (anlodipino, azelnidipino, bepridil, cilnidipino, fendilina, lercanidipino, lidoflazina, mibefradil nicardipino, nifedipino, nimodipino e nitrendipino) apresentaram atividade in vitro contra diferentes espécie de Leishmania e contra Trypanosoma cruzi, com moderada a baixa citotoxicidade contra células de mamíferos. O estudo de QSAR das 1,4-diidropiridinas permitiu a predição de dois análogos com possível atividade antiprotozoária. Anlodipino, bepridil, fendilina e nimodipino não apresentaram redução na carga parasitária de hamteres infectados com...
Descritores: Modelos Animais
Combinação de Medicamentos
Doença de Chagas
Leishmaniose
Lipossomos
Reação em Cadeia da Polimerase em Tempo Real
Limites: Animais
Responsável: BR91.2 - Centro de Documentação
BR91.2; W4, R363es, 2012


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Id: lil-507806
Autor: Tempone, André Gustavo; Andrade Jr, Heitor Franco.
Título: Nanoformualations of pentavalent abtimony entrapped in phosphatidyserine-liposomes demonstrate highest efficacy aginst experimental visceral leishmaniasis
Fonte: Rev. Inst. Adolfo Lutz;67(2):131-136, maio-ago. 2008. ilus.
Idioma: en.
Resumo: Leishmaniasis is an endemic and tropical disease that afflicts mainly the developing . The limited and highly toxic therapeutic arsenal for leishmaniasis..
Descritores: Antimônio
Leishmania
Lipossomos
Responsável: BR91.2 - Centro de Documentação


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Id: biblio-969463
Autor: Ramirez, ana(edt); Ruiz, Adrian(edt); Melo, Virginia(edt); Garcia, Maritza(edt).
Título: Alternativa con gel de Papaver somniferum (amapola) y Cannabis sativa (marihuana), como tratamiento de artritis reumatoide / Alternative gel Papaver somniferum (poppy) and Cannabis sativa (marihuana), as treatment of rheumatoid arthritis
Fonte: Rev. enferm. neurol;9(1), ene-jun. 2010.
Idioma: es.
Resumo: En la elaboración del presente producto farmacéutico (una formulación galénica entre el gel y la emulsión fluida), se utilizaron dos principios activos naturales considerados psicotrópicos o narcóticos: extracto alcohólico de amapola (Papaver somniferum) y extracto alcohólico de marihuana (Cannabis sativa); éstos tienen actividad biológica conocida dentro del organismo. Son excelentes analgésicos para pacientes con cáncer terminal pero también tienen propiedades antieméticas, estimulantes del apetito, relajantes oculares, bronquíticos, ansiolíticos. Se conoce que para tener una liberación prolongada de un principio activo es muy útil el uso de liposomas; por esta razón se utilizaron liposomas de extracto alcohólico de amapola, considerando que esta planta tiene mejores propiedades analgésicas que la marihuana, por lo cual el extracto de esta última integra un 40% de la formulación.
Descritores: Papaver
Lipossomos
Limites: Humanos
Tipo de Publ: Artigo Clássico
Responsável: MX380.1 - Coordianción de Investigación en Enfermería


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Id: biblio-973489
Autor: Zhao, Qiao-Hong; Zhang, Xi-Shan; Wu, Kun; Zhang, Jie; Xia, Tian-Fang; Chen, Jian; Qin, Zhen-Shen; Pang, Li-Qun.
Título: Preparation of Zoledronate liposome and its impact on apoptosis of Kupffer cells in rat liver
Fonte: Acta cir. bras;33(12):1052-1060, Dec. 2018. graf.
Idioma: en.
Projeto: Huai'an Science and Technology Bureau International Cooperation Project.
Resumo: Abstract Purpose: To establish a method for the preparation of zoledronate liposome and to observe its effect on inducing the apoptosis of rat liver Kupffer cells. Methods: Zoledronate was encapsulated in liposomes, and then the entrapment rate was detected on a spectrophotometer. The prepared Zoledronate liposome (0.01 mg/mL) was injected into the tail vein of SD rats. Three days later, the number of Kupffer cells (CD68 positive) in rat liver tissue was detected by immunohistochemistry. Flow cytometry was used to detect the apoptosis rate of the isolated liver Kupffer cell cultured in vitro. Results: The entrapment rate of Zoledronate was 43.4±7.8%. Immunohistochemistry revealed that the number of Kupffer cells was 19.3±2.1 in PBS group and 5.5±1.7 in Zoledronate liposome group, with a significant difference (P<0.05). The apoptosis rate of Kupffer cells was 4.1±0.8% in PBS group, while it was 9±2.2% and 23.3±5.9% in Zoledronate liposomes groups with different concentrations of Zoledronate liposome (P<0.05). Conclusions: Zoledronate liposomes can effectively induce the apoptosis of Kupffer cells in vivo and in vitro, and the apoptosis rate is related to the concentration of Zoledronate liposome. To establish a rat liver Kupffer cell apoptosis model can provide a new means for further study on Kupffer cell function.
Descritores: Apoptose/efeitos dos fármacos
Ácido Zoledrônico/farmacologia
Macrófagos do Fígado/efeitos dos fármacos
Fígado/citologia
-Imuno-Histoquímica
Distribuição Aleatória
Contagem de Células
Reprodutibilidade dos Testes
Resultado do Tratamento
Ratos Sprague-Dawley
Composição de Medicamentos/métodos
Citometria de Fluxo
Ácido Zoledrônico/administração & dosagem
Ácido Zoledrônico/síntese química
Lipossomos/síntese química
Limites: Animais
Masculino
Responsável: BR1.1 - BIREME


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Id: biblio-887013
Autor: AlGhamdi, Khalid M; Kumar, Ashok; Ashour, Abdelkader E; AL-Rikabi, Ammar C; AlOmrani, Abdullah Hasan; Ahamed, Shaik Shaffi.
Título: Vascular sclerosing effects of bleomycin on cutaneous veins: a pharmacopathologic study on experimental animals
Fonte: An. bras. dermatol;92(4):484-491, July-Aug. 2017. tab, graf.
Idioma: en.
Projeto: King Abdulaziz City for Science and Technology.
Resumo: Abstract: Background: Varicose veins and the complications of venous disease are common disorders in humans. Objective: To study the effects of bleomycin as a potential new sclerosing agent and its adverse events in treating varicose veins. Methods: Bleomycin-loaded liposomes 0.1ml was injected in the dorsal ear veins of white New Zealand rabbits. Sodium tetradecyl sulfate was used as a positive control. Normal saline was used as negative control. The blood vessels of the treated ears were photographed before and at one hour and two, eight and 45 days after treatment. Biopsies from the treated areas were obtained for histological examination. Blood samples were collected to determine any possible toxicity. Results: Bleomycin by itself was ineffective; therefore, liposomes were used as a vector to deliver bleomycin to the vein lumen. Subsequently, bleomycin started showing its sclerosing effects. Toxicity monitoring showed no apparent hematologic, pulmonary, hepatic or renal toxicities. This study revealed that bleomycin induced vasculitis, which led to vascular occlusion, which was observed on day 1 and day 8. No bleomycin-related injury was noted by histopathological examination of lung sections. The calculation of the lung/body weight coefficient indicated that edema was present in the experimental groups compared with the negative and positive controls. Study limitations: Relatively small number of experimental animals used. Conclusions: This study showed that bleomycin-loaded liposomes were able to induce vasculitis and vascular occlusion without any toxicity or complications. It might be useful, hence, to treat patients suffering from Varicose veins and other ectatic vascular diseases with this agent.
Descritores: Soluções Esclerosantes/farmacologia
Tetradecilsulfato de Sódio/administração & dosagem
Varizes/terapia
Bleomicina/farmacologia
Escleroterapia/métodos
Antibióticos Antineoplásicos/administração & dosagem
-Soluções Esclerosantes/administração & dosagem
Soluções Esclerosantes/efeitos adversos
Vasculite/induzido quimicamente
Vasculite/tratamento farmacológico
Veias/efeitos dos fármacos
Bleomicina/administração & dosagem
Modelos Animais de Doenças
Avaliação Pré-Clínica de Medicamentos
Injeções Intravenosas
Lipossomos
Limites: Animais
Coelhos
Responsável: BR1.1 - BIREME


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Id: biblio-1039075
Autor: Jarrar, Qais Bashir; Hakim, Muhammad Nazrul; Cheema, Manraj Singh; Zakaria, Zainul Amiruddin.
Título: In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes
Fonte: Braz. J. Pharm. Sci. (Online);55:e17870, 2019. tab, graf.
Idioma: en.
Resumo: Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes were determined. In addition, the maximum tolerated dose (MTD) was determined in rats via the oral and intraperitoneal routes of administration. Also, the anti-inflammatory efficacy of these liposomes was evaluated using carrageenan-induced paw edema model in rats. MFA-DDC based liposomes demonstrated a drug entrapment efficacy of 93.6%, particles size of 170.9 nm, and polydispersity index of 0.24 which were not statistically affected when stored in room and refrigerated temperatures for at least 4 weeks. The MTD of the intraperitoneally administrated MFA-loaded liposomes was 20 mg MFA/kg, whereas for those of oral administrations, it was up to 80 mg MFA/kg. Intraperitoneal dose (80 mg MFA/kg) of MFA-DDC liposomes induced extrapyramidal symptoms associated with significant elevation in serum potassium and muscle enzymes. Moreover, significant inhibition of paw edema was demonstrated by the oral and intraperitoneal routes. These findings suggest that MFA-DDC based liposomes are an effective formulation of MFA and recommend the use of bioequivalence assessments with commercial formulations.
Descritores: Ácido Mefenâmico/análise
Ditiocarb/análise
Lipossomos/agonistas
-Técnicas In Vitro
Carragenina
Limites: Animais
Feminino
Ratos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-1039079
Autor: He, Suna; Wang, Bowen; Zhang, Runfang; Zhou, Huanhuan; Yang, Qian.
Título: Preparation and evaluation of 2-methoxyestradiol-loaded pH-sensitive liposomes
Fonte: Braz. J. Pharm. Sci. (Online);55:e18204, 2019. tab, graf.
Idioma: en.
Resumo: The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. 2-ME-loaded pH-sensitive liposomes (2-ME-PSLs) was prepared containing the lipids, Lipoid E-80 (E-80), cholesteryl hemisuccinate (CHEMS), and cholesterol (CHOL) via thin-film ultrasonic dispersion. First, preparation conditions of 2-ME-PSLs were optimized by orthogonal test. Then 2-ME-PSL was characterized, and the release behavior and stability of 2-ME-PSL in vitro were evaluated. The optimal preparation conditions for 2-ME-PSLs were as follows: 2-ME : E-80+CHEMS 1:15; CHOL : E-80+CHEMS 1:5; ultrasonication time 20 minutes. The mean particle size, PDI, zeta potential, and entrapment efficiency (EE) of 2-ME-PSLs were 116 ± 9 nm, 0.161 ± 0.025, −22.4 ± 1.7 mV, and 98.6 ± 0.5%, respectively. As viewed under a transmission electron microscope, 2-ME-PSLs were well dispersed and almost spherical. They exhibited significant pH-sensitive properties and were fairly stable when diluted with a physiological solution. In conclusion, 2-ME-PSLs were successfully prepared and possessed a favorable pH sensitivity and good dissolution stability with a normal solution
Descritores: Técnicas In Vitro/instrumentação
/farmacocinética
AMERICAN HOSPITAL ASSOCIATION9TEMEFOS/farmacocinética
Lipossomos/análise
-Ensaios de Seleção de Medicamentos Antitumorais/classificação
Concentração de Íons de Hidrogênio/efeitos dos fármacos
Responsável: BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas


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Id: biblio-951944
Autor: Cavalcanti, Isabella Macário Ferro; Menezes, Talita Gomes Calaça; Campos, Luís André de Almeida; Ferraz, Milena Sales; Maciel, Maria Amélia Vieira; Caetano, Maria Nelly Psiotano; Santos-Magalhães, Nereide Stela.
Título: Interaction study between vancomycin and liposomes containing natural compounds against methicillin-resistant Staphylococcus aureus clinical isolates
Fonte: Braz. J. Pharm. Sci. (Online);54(2):e00203, 2018. tab, graf.
Idioma: en.
Projeto: Brazilian National Research Council.
Resumo: ABSTRACT The treatment of infections caused by resistant microorganisms is limited, and vancomycin (VAN) treatment failures for methicillin-resistant Staphylococcus aureus (MRSA) bacteremia are not uncommon, even when MRSA clinical isolates are susceptible to VAN. Thus, this study proposed the association of VAN with usnic acid and ß-lapachone encapsulated into liposomes as a novel therapeutic option for infections caused by MRSA. Liposomes containing ß-lap (ß-lap-lipo) or usnic acid (UA-lipo) were prepared by the thin lipid film hydration method followed by sonication. Antimicrobial activity against MRSA clinical isolates was investigated by the microdilution method according to the Clinical and Laboratory Standards Institute (CLSI). The interaction studies were carried out using the checkerboard method and epsilometer test (Etest). The interaction between VAN and ß-lap or ß-lap-lipo was synergistic (FICI = 0.453 and FICI = 0.358, respectively). An additive interaction between VAN and UA (FICI = 0.515) was found. UA-lipo resulted in synergism with VAN (FICI = 0.276). The Etest reproduced the results obtained by the checkerboard method for approximately 82% of the analysis. Thus, the present study demonstrated that VAN in combination with UA-lipo, ß-lap or ß-lap-lipo synergistically enhanced antibacterial activity against MRSA
Descritores: Vancomicina/efeitos adversos
Staphylococcus aureus Resistente à Meticilina/classificação
Meticilina/efeitos adversos
-Controle de Infecções
Lipossomos
Responsável: BR1.1 - BIREME


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Id: biblio-839472
Autor: Mehanna, Mohammed Maher; El-Kader, Nouran Abd; Samaha, Magda Wadih.
Título: Liposomes as potential carriers for ketorolac ophthalmic delivery: formulation and stability issues / Liposomes as potential carriers for ketorolac ophthalmic delivery: formulation and stability issues
Fonte: Braz. J. Pharm. Sci. (Online);53(2):e16127, 2017. tab, graf.
Idioma: pt.
Resumo: ABSTRACT Drug delivery to treat ocular disorders locally is a challenging endeavor. Traditional ocular dosage form - eye drops - exhibits poor availability, consequently inefficient therapeutic response. The objective of the study was to formulate and characterize a ketorolac tromethamine ocular system with a prolonged release pattern based on liposomes as a vesicular carrier and to design once daily liquid preparation realizing the thermal in situ gelation principle. Liposomes were prepared by film hydration method. The influence of cholesterol concentration, pH and volume of hydration medium, and type and concentration of charging imparting agents were studied. Liposomes were characterized via, morphological examination, vesicular size, and encapsulation efficiency, and in vitro release performance, moreover its stability was assessed. The results obtained highlighted that liposomes showed a closed vesicular multi-lamellar structure. Ketorolac was successfully encapsulated within the liposomal structure in a cholesterol and charge inducing agent concentration-dependent behaviour. The dispersion of liposomes within thermosensitive Poloxamer in situ gel was able to retard the release of the drug by diffusion providing a controlled prolonged delivery. The liposomal formulations were physically stable for six months. Ketorolac tromethamine in situ liposomal gel representing an efficient alternative in terms of ocular retention and patient compliance when compared with conventional eye drops.
Descritores: Cetorolaco de Trometamina/farmacocinética
Reatividade-Estabilidade
Composição de Medicamentos/classificação
Lipossomos/antagonistas & inibidores
-Trometamina/antagonistas & inibidores
Anormalidades do Olho/complicações
Dermatopatias Vesiculobolhosas
Administração Oftálmica
Responsável: BR1.1 - BIREME



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