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1.
Pharm Dev Technol ; 25(1): 54-67, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31535923

RESUMO

This study aimed to prepare and characterize organogels containing microparticles of ascorbic acid (AA) obtained from propolis by-product. The formulations F1 (5% of microparticles) and F2 (10% of microparticles) were evaluated regarding rheological and textural properties, antioxidant and radical scavenging activity, in vitro release and cellular studies. The organogels showed plastic flow behavior and rheopexy. The textural parameters were within acceptable values for semisolid formulations. The antioxidant capacity of organogels F1 and F2 by the DPPH assay demonstrated IC50 ranging from 1523.59 to 1166.97 µg/mL, respectively. For the FRAP assay, the values found were 842.88 and 956.14 µmol of FSE/g formulation, respectively. Good scavenging activity against nitrogen species was observed. The concentration of 63 µg/mL did not present toxicity on HaCaT and HFF-1 cells. In vitro release profile of AA from organogels showed a slow pattern of drug release, mainly for F2. Therefore, the proposed organogel containing AA microparticles with propolis by-product matrix represents a promising platform for topical drug delivery with antioxidant effect.


Assuntos
Ácido Ascórbico/química , Géis/química , Própole/química , Antioxidantes/química , Química Farmacêutica/métodos , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Viscosidade/efeitos dos fármacos
2.
Food Funct ; 9(8): 4518, 2018 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-30019728

RESUMO

Correction for 'Development of a microparticulate system containing Brazilian propolis by-product and gelatine for ascorbic acid delivery: evaluation of intestinal cell viability and radical scavenging activity' by Lizziane Maria Belloto de Francisco et al., Food Funct., 2018, DOI: 10.1039/c8fo00863a.

3.
Food Funct ; 9(8): 4194-4206, 2018 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-29993073

RESUMO

The use of propolis by-product (PBP) microparticles (MP) as delivery systems can be a promising tool to surpass drawbacks related to low stability of ascorbic acid (AA). The objective of this study was to develop and characterize MP prepared with PBP containing AA. The MP was characterized regarding morphology, particle size, polydispersity index (PDI), association efficiency (AE), drug loading (DL), infrared and Raman spectroscopy as well as antioxidant and radical scavenging activity, in vitro release, and cellular studies. MP was shown to be spherical with some agglomeration. Its particle size was 1654 ± 0.210 nm with a PDI of 0.7. The AE and DL were, respectively, 100.30 ± 2.66% and 13.16 ± 0.59. Spectroscopic studies indicated a possible interaction between the PBP and AA. 2,2-Diphenyl-1-picrylhydrazyl (DPPH˙), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and ferric reducing antioxidant power (FRAP) assays demonstrated that the MP containing AA have an excellent antioxidant capacity as well as a considerable scavenging activity against reactive oxygen and nitrogen species. The in vitro release profile showed a slow pattern of drug release of AA from MP. Viability studies with intestinal cells revealed that MP did not present toxicity in Caco-2 and HT29-MTX. Moreover, AA could permeate Caco-2 monolayers and triple co-culture substantially at the end of 8 h, opposite to the MP. Therefore, the proposed MP formulation represents a promising platform for oral delivery of AA with a local effect on intestines.


Assuntos
Antioxidantes/farmacologia , Ácido Ascórbico/farmacologia , Células Epiteliais/efeitos dos fármacos , Gelatina/química , Mucosa Intestinal/citologia , Própole/química , Antioxidantes/química , Ácido Ascórbico/química , Células CACO-2 , Células HT29 , Humanos , Microscopia Eletrônica de Varredura , Espectrofotometria Infravermelho , Análise Espectral Raman
4.
Pharm Dev Technol ; 23(4): 316-323, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28565928

RESUMO

The use of iron oxide magnetic nanoparticles (IMNP) in medical and pharmaceutical areas dates to the beginning of the 1970s, as carriers. Some other uses to these nanoparticles are in vitro separation, magnetic resonance imaging and drug targeting agent. Many preparations containing IMNP have been described and used in drug delivery, hyperthermia, in vitro separation, tissue repair, cellular therapy, for magnetic separation, magnetic resonance imaging, as spoilers for magnetic resonance spectroscopy, and more recently as sensors for metabolites and other biomolecules. The use of these nanostructures as antibacterial agents has also been reported, which could kill some bacteria species causing no damage to the human host cells. Recently, they have been used as hyperthermia agents to treat infections or cancer, which are more susceptible than the healthy host's cells. Engineering designs, physiochemical characteristics, biomedical applications of IMNP, toxicity and magnetic nanotoxicology have been discussed. However, the application of IMNP as antimicrobials is very important. Thus, this review explores the therapeutic activities of IMNP and their use as antimicrobial agents. These nanoparticles can be efficient for the treatment of microbial infections, probably acting as membrane permeability enhancer, damaging the cell wall or by generating reactive oxygen species.


Assuntos
Antibacterianos/uso terapêutico , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Nanopartículas de Magnetita/uso terapêutico , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Sistemas de Liberação de Medicamentos/métodos , Humanos , Hipertermia Induzida/métodos , Imageamento por Ressonância Magnética/métodos , Nanopartículas de Magnetita/química , Nanomedicina/métodos , Nanotecnologia/métodos , Neoplasias/terapia
5.
Curr Drug Deliv ; 13(7): 1152-1164, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26563943

RESUMO

Metronidazole is an antimicrobial agent utilized for the treatment of protozoa and anaerobic bacteria infections. Many times, it is necessary to modify the metronidazole release, and the development of modified release systems may be suggested. In this study, we are able to investigate the use of the residue normally thrown out from the preparation of propolis extracts (BP) as strategy to modify the metronidazole release. We prepared films containing polymeric adjuvant (gelatin or ethylcellulose) and metronidazole, by solvent casting method. Density, mechanical properties, water vapor permeability (WVP), moisture uptake capacity (MUC), thermogravimetry, differential scanning calorimetry, Fourier transform infrared spectroscopy (FT-IR), and in vitro metronidazole release were investigated. Thickness and density of the preparations indicated that the compounds were homogeneously dispersed throughout. Mechanical properties were influenced by film composition. Films containing gelatin showed higher resistance to stress while those containing ethylcellulose presented greater flexibility. The greater the adjuvant concentrations lower the resistance to rupture and the elasticity, but higher MUC and WVP of formulations. FT-IR tests suggested interactions between BP and the adjuvants. Films were capable to protect the metronidazole and changed its release profile. BP films are of great practical importance constituting a novel strategy to modify the metronidazole release.


Assuntos
Anti-Infecciosos/química , Sistemas de Liberação de Medicamentos , Metronidazol/química , Própole , Celulose/análogos & derivados , Celulose/química , Liberação Controlada de Fármacos , Gelatina/química , Espectroscopia de Infravermelho com Transformada de Fourier , Resistência à Tração , Termogravimetria , Resíduos , Água/química
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