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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Polyethyleneimine-modified pectin beads for colon-specific drug delivery: In vitro and in vivo implications
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Polyethyleneimine-modified pectin beads for colon-specific drug delivery: In vitro and in vivo implications

机译:聚乙烯亚胺修饰的果胶珠用于结肠特异性药物递送:体内和体外的意义

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摘要

Calcium-pectinate (Ca-pectinate) beads have shown immense potential as colon-specific drug carrier. However, Ca-pectinate itself is unable to prevent its swelling/degradation in the upper gastro-intestinal (Gl) conditions. Hence, polyethyleneimine (PEI) was added in the cross-linking solution to strengthen the Ca-pectinate network. Resveratrol was used as a model drug due to its promising therapeutic activity towards several colonic diseases. Beads were prepared by varying cross-linking solution pH and other formulation variables. The effects of these formulation variables were investigated on the bead's characteristics. Furthermore, surface morphology, drug-polymer interaction, stability, and in vivo pharmacokinetic study of the optimized formulation were performed. The optimized PEI-modified beads prevented drug release in the upper Gi conditions, while released the drug in simulated colonic fluid. Furthermore, in vivo pharmacokinetics studies in rats demonstrated delayed appearance of drug in blood after oral administration. The optimized Ca-pectinate beads demonstrated both in vitro and in vivo colon-specific drug release.
机译:果胶钙(Ca-果胶酸)珠已显示出作为结肠特异性药物载体的巨大潜力。但是,果胶酸钙本身不能防止其在上消化道(G1)条件下的溶胀/降解。因此,在交联溶液中添加聚乙烯亚胺(PEI)以增强Ca-果胶酸盐网络。白藜芦醇由于其对几种结肠疾病的有希望的治疗活性而被用作模型药物。通过改变交联溶液的pH值和其他配方变量来制备微珠。研究了这些配方变量对微珠特性的影响。此外,进行了优化制剂的表面形态,药物-聚合物相互作用,稳定性和体内药代动力学研究。经过优化的PEI修饰的磁珠可在较高的Gi条件下阻止药物释放,而在模拟结肠液中释放药物。此外,对大鼠的体内药代动力学研究表明,口服给药后血液中药物出现延迟。优化的果胶酸钙果胶珠在体外和体内均表现出结肠特异性药物释放。

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