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1.
J Phys Chem B ; 128(22): 5427-5436, 2024 Jun 06.
Artigo em Inglês | MEDLINE | ID: mdl-38808516

RESUMO

5-Fluorouracil (5-FU) is an antineoplastic agent known for its low bioavailability and limited cellular penetration, often resulting in adverse effects on healthy cells. Thus, finding vehicles that enhance bioavailability, enable controlled release, and mitigate adverse effects is crucial. The study focuses on encapsulating 5-FU within soy lecithin vesicles (SLVs) and assessing its impact on the carrier's properties and functionality. Results show that incorporating 5-FU does not affect SLVs' size or polydispersity, even postlyophilization. Liberation of 5-FU from SLVs requires system disruption rather than spontaneous release, with an encapsulation efficiency of approximately 43% determined using Square Wave Voltammetry. Cytotoxicity assays on colorectal cancer cells reveal SLV-based delivery's significant efficacy, surpassing free drug solution effects with 45% cell viability after 72 h vs 73% viability. The research addresses 5-FU's limited bioavailability by creating a biocompatible nanocarrier for efficient drug delivery, highlighting SLVs as promising for targeted cancer therapy due to sustained antiproliferative effects and improved cellular uptake. The study underscores the importance of tailored drug delivery systems in enhancing therapeutic outcomes and suggests SLV/5-FU formulations as a potential advancement in cancer treatment strategies.


Assuntos
Sobrevivência Celular , Portadores de Fármacos , Fluoruracila , Glycine max , Lecitinas , Fluoruracila/química , Fluoruracila/farmacologia , Lecitinas/química , Humanos , Portadores de Fármacos/química , Sobrevivência Celular/efeitos dos fármacos , Glycine max/química , Liberação Controlada de Fármacos , Técnicas Eletroquímicas , Nanopartículas/química
2.
Colloids Surf B Biointerfaces ; 188: 110759, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31887645

RESUMO

Diabetes is a disease that affects millions of people in the World, constituting a global problem. Patients are administered insulin subcutaneous injections, resulting in high costs and frequent infections in the injection site. A possible solution to this problem may be the use of nanotechnology. Nanotransporters can act as specific release systems able to overcome the current limitations to drug delivery. Liposomes and vesicles can deliver drugs directly and efficiently to the site of action, decreasing toxicity and adverse effects. In previous studies, we demonstrated the biocompatibility and safety of catanionic benzyl n-hexadecyldimethylammonium 1,4 -bis-2-ethylhexylsulfosuccinate (BHD-AOT) vesicles using both in vitro and in vivo tests. Thus, the aims of this work were to evaluate the ability of the BHD-AOT vesicles to encapsulate insulin; to analyze the structural properties and stability of the system, vesicle-Insulin (VIn), at different pH conditions; and to study the ability of VIn to decrease the glycemia in miceby different administration routes. Our results showed that 2 and 5 mg mL-1 of vesicles were able to encapsulate about 55 % and 73 % of insulin, respectively. The system VIn showed a significant increase in size from 120 to 350 nm, changes in the surface zeta potential value, and high stability to different pH conditions. A significant decrease of the glycemia after VIn administration was demonstrated in in vivo assays, including the oral route. Our results reveal that BHD-AOT vesicles may be an appropriate system to encapsulate and protect insulin, and may be a potential system to be administrated in different ways as an alternative strategy to conventional therapy.


Assuntos
Compostos de Amônio/química , Sistemas de Liberação de Medicamentos , Insulina/química , Nanopartículas/química , Succinatos/química , Animais , Glicemia/análise , Glicemia/metabolismo , Cátions/química , Portadores de Fármacos/química , Insulina/administração & dosagem , Insulina/metabolismo , Camundongos , Estrutura Molecular , Tamanho da Partícula , Propriedades de Superfície
3.
Bioelectrochemistry ; 120: 120-126, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29247891

RESUMO

In this contribution an electrochemical study is described for the first time of lipid peroxidation and the role of antioxidant on lipid protection using large unilamellar vesicles (LUVs). In order to simulate the cell membrane, LUVs composed of 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) were used. A vesicle-modified electrode was constructed by immobilizing DOPC LUVs onto carbon paste electrodes (CPEs). Lipid peroxidation was studied electrochemically by incubating the vesicle-modified electrodes with hydroxyl (HO) radicals generated via the Fenton reaction. Oxidative damage induced by HO was verified by using square wave voltammetry (SWV) and was indirectly measured by the increase of electrochemical peak current to [Fe(CN)6]4- which was used as the electrochemical label. Ascorbic acid (AA) was used as the antioxidant model in order to study its efficacy on free radical scavenging. The decrease of the electrochemical signal confirms the protective key role promoted by AA in the prevention of lipid peroxidation in vesicles. Through microscopy, it was possible to observe morphologic modification on vesicle structures after lipid peroxidation in the presence or absence of AA.


Assuntos
Antioxidantes/farmacologia , Ácido Ascórbico/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Fosfatidilcolinas/química , Lipossomas Unilamelares/química , Técnicas Eletroquímicas/métodos , Eletrodos , Peróxido de Hidrogênio/química , Radical Hidroxila/química , Ferro/química
4.
Beilstein J Nanotechnol ; 7: 655-63, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27335755

RESUMO

In this contribution a strategy is shown to covalently immobilize gold nanoparticles (AuNPs) onto vesicle bilayers with the aim of using this nanomaterial as platform for the future design of immunosensors. A novel methodology for the self-assembly of AuNPs onto large unilamellar vesicle structures is described. The vesicles were formed with 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) and 1-undecanethiol (SH). After, the AuNPs photochemically synthesized in pure glycerol were mixed and anchored onto SH-DOPC vesicles. The data provided by voltammetry, spectrometry and microscopy techniques indicated that the AuNPs were successfully covalently anchored onto the vesicle bilayer and decorated vesicles exhibit a spherical shape with a size of 190 ± 10 nm. The developed procedure is easy, rapid and reproducible to start designing a possible immunosensor by using environmentally friendly procedures.

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