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1.
Int J Pharm ; 638: 122912, 2023 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-37015296

RESUMO

The goal was to scrutinize niosomes as potential carriers for enhanced efficacy of norfloxacin against Toxoplasma gondii RH strain. This was assessed in vitro and in vivo. Standard niosomes of Span 60 and cholesterol were prepared. Gelucire 48/16 or Tween 80 was incorporated as hydrophilic fluidizer. The prepared vesicles were characterized for shape, size, viscosity and norfloxacin release. The in vitro anti-Toxoplasma was assessed by monitoring tachyzoites viability after incubation with niosomes. In vivo efficacy of niosomes encapsulated norfloxacin was evaluated on infected mice. Transmission electron micrographs showed nano-sized spherical vesicles. Norfloxacin release varied with niosomal composition to show faster liberation in presence of fluidizing agent. The half maximum effective concentration of norfloxacin against tachyzoites (EC50) was significantly reduced after niosomal encapsulation compared with simple drug solution with no significant difference between vesicular formulations. Tachyzoite count in the peritoneal fluid of infected mice was reduced by 45.2, 90.8, 88.3 and 84% after treatment with simple drug dispersion, standard niosomes, Gelucire containing and Tween containing vesicles, respectively compared to infected untreated mice. These results correlate with the in vitro data and reflects the efficacy of niosomes. The study introduced surfactant vesicles as a tool for enhanced efficacy of norfloxacin against toxoplasma.


Assuntos
Lipossomos , Tensoativos , Camundongos , Animais , Norfloxacino/farmacologia , Polissorbatos , Composição de Medicamentos , Tamanho da Partícula
2.
Carbohydr Polym ; 232: 115826, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31952620

RESUMO

The study investigated chitosan coated nanostructured lipid carriers (NLCs) for oral delivery of albendazole in treatment of trichinellosis. NLCs comprised precirol and oleic acid with Tween and Span 80. Dicetylphosphate was used as charging agent to allow chitosan coating. Trichinella spiralis infected mice were used and albendazole suspension, coated or uncoated NLCs were orally administered at different stages of infection. NLCs were spherical with size of 188 and 200 nm for coated and uncoated NLC, respectively. Treatment during intestinal phase reduced worm count with NLCs showing better rank. This was reflected further by reduced larvae count and improved histopathological features. Starting treatment in the migrating phase reduced larval count by 62.9, 99.6 and 89.5 % after administration of suspension, coated and uncoated NLCs, respectively. The same rank was recorded for the encysted phase. NLCs enhanced the efficacy of albendazole against Trichinella spiralis compared with suspension with chitosan coated NLCs being superior.


Assuntos
Albendazol/farmacologia , Antiprotozoários/farmacologia , Quitosana/química , Lipídeos/química , Nanoestruturas/química , Trichinella spiralis/efeitos dos fármacos , Administração Oral , Albendazol/administração & dosagem , Albendazol/química , Animais , Antiprotozoários/administração & dosagem , Antiprotozoários/química , Quitosana/administração & dosagem , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Lipídeos/administração & dosagem , Nanoestruturas/administração & dosagem , Testes de Sensibilidade Parasitária , Tamanho da Partícula , Propriedades de Superfície
3.
Pharm Dev Technol ; 24(2): 157-165, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-29441809

RESUMO

The fluidity of vesicular membrane affects vesicular transdermal drug delivery. Essential oils can be located in vesicular membrane imparting flexibility and influencing transdermal delivery. Accordingly, the objective was to investigate the effect of incorporation of essential oils in niosomes on felodipine transdermal delivery. Rigid niosomes comprising Span 60 with cholesterol (2:1, w/w) were used with clove, eucalyptus or lemon oils being incorporated in the vesicles at increasing concentrations. The vesicle size and shape was monitored using scanning electron microscopy. Thermal analysis was used to monitor the thermal behavior. Drug entrapment efficiency, release and skin permeation were monitored. Niosomes were spherical with size ranging from 279 to 345 nm. The drug entrapment ranged from 97.9 to 98.8%. Thermal analysis confirmed the existence of oils within vesicular membrane and highlighted the membrane fluidizing effect. Drug release depended on the oil with clove oil or eucalyptus oil showing a trend of increased drug release compared with plain niosomes. In contrast, lemon oil reduced drug release rate. Skin permeation study reflected the superiority of oil containing niosomes. The results correlated with the fluidizing and penetration enhancing effects of oils. The study introduced essential oils as potential niosomes fluidizing agents for enhanced transdermal drug delivery.


Assuntos
Felodipino/administração & dosagem , Felodipino/química , Lipossomos/química , Óleos Voláteis/química , Administração Cutânea , Animais , Sistemas de Liberação de Medicamentos/métodos , Masculino , Microscopia Eletrônica de Varredura/métodos , Tamanho da Partícula , Coelhos , Pele/metabolismo , Absorção Cutânea
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