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1.
J Pharm Sci ; 111(2): 417-431, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34461114

RESUMO

This work aimed to develop a new efficient approach for safe treatment of psoriasis. To achieve that, resveratrol-loaded spanlastics(F1-F12) were prepared and evaluated by complete in vitro characterization. The two optimal formulations (F10 and F11) had their particle size in the nano range with high entrapment efficiency and sustainable drug release. These two formulae were incorporated in carbopol 934 gel formulations (G1-G8) with different concentrations of drug and carbopol 934 polymer. G1 and G5 (1% w/w Carbopol 934 gel and 0.1% resveratrol) showed 40.13% ± 2.017% and 73.76% ± 2.46%,8 hours drug release, respectively. Their pH was accepted and non-irritant. At a shear stress of 500 s-1, G1 and G5 showed a reasonable viscosity of 1048.5 ± 2.12 cps and 954 ± 2.15 cps, respectively. In the in vivo psoriasis study, mice treated by G5 gel showed significant improvement of erythema and scaling compared to positive control group and they maintained healthy skin as shown in histopathological observations. Moreover, this group showed the least changes in mRNA expression of inflammatory cytokines. Concisely, our results suggest that selected carbopol gel of resveratrol-loaded spanlastics could maximize resveratrol topical anti-psoriatic effect.


Assuntos
Psoríase , Absorção Cutânea , Animais , Liberação Controlada de Fármacos , Imiquimode , Camundongos , Psoríase/induzido quimicamente , Psoríase/tratamento farmacológico , Psoríase/patologia , Resveratrol/uso terapêutico
2.
Int J Biol Macromol ; 146: 119-131, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31904460

RESUMO

Breast cancer endocrine resistance prevents unleashing full capabilities of Tamoxifen (TMX), besides TMX off-target side effects on healthy tissue. In this study, we engineered TMX nanocomposite via co-loading it on alginate-based silver nanoparticles and embedding within folic acid-polyethylene glycol surface conjugate. The coating process was done by w/o/w double emulsion method. To confirm the silver nanoparticles formation, UV spectroscopy, XRD and TEM analysis were carried out. TEM results confirmed the core-shell structure of folate targeted nanocomposite with approximate average diameter of 66 nm, the nanocomposite structures were characterized by FTIR, TGA and SEM. By comparing with the non-targeted formula, folate decorated formula had 12-folds lowered IC50 value and 12.5-14-fold higher cancer cells toxic selectivity index. Also, after 4 h treatment, both fluorescence microscopic and flow cytometric analysis indicated higher intracellular accumulation of folic acid conjugated formula on MCF-7 cancer cells than the non-targeted one with 3.44-folds. The breast cancer cytotoxic effects of this metal-endocrine nanocomposite formula could be explained by the induction of reactive oxygen species (ROS), down regulation of survival oncogenic genes (BCL-2 and Survivin) and the accumulation of MCF-7 cells in G2/M phase. All these data confirm the efficiency and efficacy of the formulated nanocomposite as future treatment for breast cancer.


Assuntos
Neoplasias da Mama/tratamento farmacológico , Portadores de Fármacos , NF-kappa B/metabolismo , Nanocompostos , Proteínas de Neoplasias/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Tamoxifeno , Alginatos/química , Alginatos/farmacocinética , Alginatos/farmacologia , Neoplasias da Mama/metabolismo , Neoplasias da Mama/patologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Feminino , Humanos , Células MCF-7 , Nanocompostos/química , Nanocompostos/uso terapêutico , Prata/química , Prata/farmacocinética , Prata/farmacologia , Tamoxifeno/química , Tamoxifeno/farmacocinética , Tamoxifeno/farmacologia
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