期刊
AAPS PHARMSCITECH
卷 13, 期 2, 页码 364-372出版社
SPRINGER
DOI: 10.1208/s12249-012-9752-0
关键词
casein; complex coacervation; microcapsules; pectin; release kinetics
资金
- CAPES (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior), Brazil
- CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico), Brazil
Controlled release of drugs is an important strategy to diminish the drug dose and adverse side effects. Aqueous mixtures of polysaccharides and proteins are usually unstable above a certain biopolymer concentration and phase separation occurs either because of repulsive (segregative) or attractive (associative) interactions. Herein, pectin/casein microcapsules were prepared by complex coacervation aiming at prolonged drug release. The morphological characteristics, particle size, distribution, and release kinetics of microcapsules were studied using as a model the hydrophilic drug acetaminophen. It was detected that complexation of pectin/casein particles occurs at pH values lower than 6, resulting in the formation of spherical particles after spray drying. Microcapsules had a mean diameter of 3.138 and 4.929 mu m without drug, and of 4.680 and 5.182 mu m with drug using USP and 8003 pectin, respectively. The in vitro release of acetaminophen from microcapsules was slow and the drug release mechanism was controlled by diffusion following first-order kinetics. There was greater release of acetaminophen in simulated gastric fluid than simulated intestinal fluid conditions. Concluding, the polymeric system present herein seemed to be appropriate for a prolonged release of acetaminophen throughout the gastrointestinal tract. Nevertheless, it is likely that it is a promising pectin/casein complex for lipossoluble drugs, which merits further investigation.
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