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1.
Arch Razi Inst ; 78(3): 1023-1028, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-38028832

RESUMO

Rasagiline is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B) that is effective in the treatment of Parkinson's disease (PD). It had antioxidant and anti-apoptotic activity in experimental models. Moreover, it has low permeability and its oral bioavailability is weak and highly variable due to extensive first-pass hepatic metabolism (35%). This study aimed to formulate rasagiline mesylate (RM) as a lipid-polymer hybrid nanoparticle in order to enhance its permeation and increase its chance to be absorbed by lymphatic circulation to avoid metabolism and control its release. Successful formulation (PCL-2) was reached by the nanoprecipitation method using polycaprolactone with RM in the organic phase and lecithin in the aqueous phase DSPE-PEG. The lipid:polymer ratio of 24% and DSPE: lecithin of 50% resulted in stable nanoparticles having a particle size of 132±4.58 nm, polydispersity index of 0.273±0.02, zeta potential of -25.6±3.3, entrapment efficiency of 46±3.9%, and drug loading of 51.93±6.5. Results showed that the diffusion was more effective on the release profile than the degradation and resulted in a Fickian diffusion mechanism.


Assuntos
Inibidores da Monoaminoxidase , Fármacos Neuroprotetores , Animais , Inibidores da Monoaminoxidase/farmacologia , Inibidores da Monoaminoxidase/uso terapêutico , Lecitinas , Fármacos Neuroprotetores/farmacologia , Mesilatos
2.
Ann Burns Fire Disasters ; 23(4): 199-205, 2010 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-21991225

RESUMO

Background. Thermal injury causes the destruction of the physical skin barrier that normally protects the body from invasion by micro-organisms and induces an immunocompromised state that predisposes burn patients to infection, sepsis, and multiple organ failure. Reactive oxygen species contribute to burn-mediated immune suppression, and as the use of antioxidants has a positive effect on immune function, this may reduce the incidence of wound infection and related complications in burn patients. Patients and methods. One hundred and eighty burn patients of either sex and different ages, suffering from burns of varying percentage, were involved in the study. They were allocated to six groups: A, B, C, D, E, and F, each of 30 patients. Groups B, C, D, E, and F were treated with antioxidants (vitamins E and C, zinc sulphate, allopurinol, melatonin, and N-acetylcysteine, respectively) while group A was treated without antioxidants, according to our hospital policy. Thirty healthy subjects (group G) were also involved in the study as a control group for comparison. In each group, serum malondialdehyde and serum glutathione levels, microbiological values, healing time, and the mortality rate were measured using standard methods. Results. Administering antioxidants to burn patients produced significant improvements in the parameters studied compared with burn patients not given antioxidants. Conclusion. The study clearly showed the beneficial effect of antioxidants in the treatment of burn patients, as evidenced by the reduced incidence of wound infection and the shortening of healing time, in addition to the lower mortality rate. It is therefore recommended to add antioxidants to the treatment list of burn patients.

3.
Ann Burns Fire Disasters ; 22(1): 6-11, 2009 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-21991144

RESUMO

Background. Burns cause a systemic inflammatory response, endothelial dysfunction, and increased microvascular permeability which results in oedema being formed; these effects are probably the result of a complex interplay between the direct effects of heat on the microcirculation and the action of chemical mediators, including reactive oxygen species. The use of antioxidants can reduce these changes, which are considered a promised step in burns management. Patients and methods. Forty-eight burn patients of either sex and with varying burns percentages were involved in the study. They were each allocated to one of four groups: A, B, C, and D, each group composed of 12 patients. Groups B, C, and D were treated with antioxidants: allopurinol, melatonin, and N-acetylcysteine respectively, while group A was treated according to normal hospital policy, without antioxidants; 12 healthy subjects (group E) served as a control group for comparison. In each group, serum malondialdehyde and serum glutathione levels were measured and liver and kidney function tests were performed, as well as microalbuminuria tests, using standard methods. Results. The administration of antioxidants to burns patients produced significant improvements in the parameters studied compared to group A parameters (no antioxidant given). Conclusion. This study clearly demonstrates the role of reactive oxygen species in endothelial dysfunction occurring in burn patients and the beneficial effect of antioxidants in reducing it, as shown by the reduced microalbuminuria and reduced resuscitation fluid in antioxidant-treated burn patients; the study also supports newly emerging evidence regarding the use of microalbuminuria as an indicator for endothelial dysfunction in burn patients.

4.
Ann Burns Fire Disasters ; 21(4): 186-91, 2008 Dec 31.
Artigo em Inglês | MEDLINE | ID: mdl-21991135

RESUMO

Burns are a major health problem worldwide, with high mortality and morbidity in addition to causing changes in the quality of life of burn patients. Utilizing antioxidant therapeutic strategies depending on new mechanisms involved in the pathogenesis of burns-related "oxidative stress" may be considered a promising step in burns management. This study involved 180 burn patients of varying age and either sex and with varying burns percentages. The patients were subdivided into six groups (A, B, C, D, E, and F); each group thus included 30 patients. Patients in groups B, C, D, E, and F were treated with antioxidants (vitamin E with vitamin C, zinc sulphate, allopurinol, melatonin, and N-acetylcysteine respectively) while group A was treated according to hospital policy, without any antioxidant; also, healthy subjects (group G) were involved in the study as a control group for comparison.In each group we examined serum malondialdehyde and serum glutathione levels, serum zinc and copper levels, liver function, renal function, mortality rate, and healing time, using standard methods. It was found that the administration of antioxidants to burn patients produced significant improvement in the parameters studied compared with group A (no antioxidant given). This study clearly shows the importance of the therapeutic targeting of oxidative stress in the treatment of burns. It is important to consider antioxidant a most effective weapon that must be added to the arsenal available in the combating of burn complications.

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