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1.
Bioorg Med Chem Lett ; 22(9): 3213-8, 2012 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-22460032

RESUMO

Recently, we demonstrated the safety use of calendula oil/chitosan microcapsules as a carrier for both oral and topical deliveries. We also reported the improved biological activity towards skin cells and Staphylococcus aureus of phyllanthin containing chitosan microcapsules. However, the possibility of both oral and topical applications was still necessary to be further studied. Here we investigated that both oral and topical applications of chitosan-based microcapsules were tested using hydrocortisone succinic acid (HSA) and 5-fluorouracil (5-FU), respectively. The drug loading efficiency, particle size, surface morphology and chemical compositions of both drug loaded microcapsules were confirmed by UV-vis spectrophotometer, particle size analyzer, scanning electron microscope and Fourier transform infrared spectroscopy. The in vitro release studies revealed that both HSA and 5-FU could be released form chitosan microcapsules. The mean adrenocorticotropic hormone concentration in HSA loaded microcapsule mice plasma was detected to be lower than that of water control. One hundred micrograms per milliliter of 5-FU containing microcapsules exhibited a stronger growth inhibition towards skin keratinocytes than that of free 5-FU. In vitro drug delivery model demonstrated the delivery of 5-FU from microcapsule treated textiles into nude mice skin. Further uses of the drug loaded microcapsules may provide an efficiency deliverable tool for both oral and topical applications.


Assuntos
Cápsulas/química , Sistemas de Liberação de Medicamentos/métodos , Administração Oral , Administração Tópica , Animais , Quitosana , Fluoruracila , Hidrocortisona , Queratinócitos/citologia , Camundongos , Pele/citologia , Pele/efeitos dos fármacos , Staphylococcus aureus , Ácido Succínico
2.
Bioorg Med Chem Lett ; 20(14): 4147-51, 2010 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-20538460

RESUMO

The use of chitosan as the wall of microcapsule designed for delivery of encapsulated celecoxib is reported. Microcapsules were characterised with respect to size and encapsulation efficiency of celecoxib. In vivo animals demonstrated that both free celecoxib administration and chitosan/celecoxib microcapsules administration lead to a significant inhibition of cyclooxygenase-2 protein expression in the hepatocytes when compared with vehicle control mice. Interestingly, microcapsule containing celecoxib showed a better inhibition of cyclooxygenase-2 protein expression when compared with a simple oral administration of free celecoxib. Gas-chromatography-mass-spectrometry analysis showed that in mice treated with free celecoxib or chitosan/celecoxib microcapsules, their plasma concentration of celecoxib was similar. Microcapsules-based biomaterials as oral drug delivery vehicles may help to improve the absorption efficiency of therapeutic drugs.


Assuntos
Quitosana/síntese química , Quitosana/farmacologia , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/farmacologia , Pirazóis/síntese química , Pirazóis/farmacologia , Sulfonamidas/síntese química , Sulfonamidas/farmacologia , Celecoxib , Cromatografia Gasosa-Espectrometria de Massas , Microscopia Eletrônica de Varredura , Microesferas
4.
Carbohydr Polym ; 89(3): 795-801, 2012 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-24750864

RESUMO

In this paper, a simple and versatile coacervation technique has been developed by using an ultrasound-assisted oil/water emulsion method for the preparation of antifungal agent-loaded microcapsules. Two types of chitosan microcapsules are successfully prepared. The mean particle size of the chitosan/miconazole nitrate microcapsules is 2.6 µm and that of the chitosan/clotrimazole microcapsules is 4.1 µm. The encapsulation efficiency of the chitosan/miconazole nitrate microcapsules (77.58-96.81%) is relatively higher than that of the chitosan/clotrimazole microcapsules (56.66-93.82%). The in vitro drug release performance of the microcapsules shows that the chitosan/miconazole nitrate microcapsules release about 49.5% of the drug while chitosan/clotrimazole microcapsules release more than 66.1% of the drug after 12h under a pressure of 5 kg at pH 5.5, which is similar to the pH of human skin. The prepared drug-loaded microcapsules could be applied onto bandages or socks, and will continuously release antifungal drugs in a controlled manner under pressure.


Assuntos
Antifúngicos/química , Cápsulas , Quitosana/química , Clotrimazol/química , Emulsões , Miconazol/química , Cromatografia Líquida de Alta Pressão , Microscopia Eletrônica de Varredura , Espectroscopia de Infravermelho com Transformada de Fourier
5.
Int J Mol Med ; 24(4): 411-9, 2009 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-19724879

RESUMO

In recent years, textile materials with special applications in the cosmetic field have been developed. A new sector of cosmetic textiles is opened up and several cosmetic textile products are currently available in the market. Microencapsulation technology is an effective technique to control the release properties of active ingredients that prolong the functionality of cosmetic textiles. This study discusses the development of cosmetic textiles and addresses microencapsulation technology with respect to its historical background, significant advantages, microencapsulation methods and recent applications in the textile industry. Gelatin microcapsules containing vitamin C were prepared using emulsion hardening technique. Both the optical microscopy and scanning electron microscopy demonstrated that the newly developed microcapsules were in the form of core-shell spheres with relatively smooth surface. The particle size of microcapsules ranged from 5.0 to 44.1 microm with the average particle size being 24.6 microm. The gelatin microcapsules were proved to be non-cytotoxic based on the research findings of the toxicity studies conducted on human liver and breast cell lines as well as primary bone marrow culture obtained from patient with non-malignant haematological disorder. The gelatin microcapsules were successfully grafted into textile materials for the development of cosmetic textiles.


Assuntos
Ácido Ascórbico/química , Materiais Biocompatíveis/química , Cápsulas/química , Gelatina/química , Materiais Biocompatíveis/toxicidade , Cápsulas/toxicidade , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Modelos Teóricos , Têxteis/toxicidade
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