Oral Bioavailability of Insulin Contained in Polysaccharide Nanoparticles

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• 作者：Bruno Sarmento ; Antó ; nio Ribeiro ; Francisco Veiga ; Domingos Ferreira ; Ronald Neufeld
• 刊名：Biomacromolecules
• 出版年：2007
• 出版时间：October 2007
• 年：2007
• 卷：8
• 期：10
• 页码：3054 - 3060
• 全文大小：362K
• 年卷期：v.8,no.10(October 2007)
• ISSN：1526-4602

文摘

The pharmacological activity of insulin-loaded dextran sulfate/chitosan nanoparticles was evaluated followingoral dosage in diabetic rats. Nanoparticles were mucoadhesive and negatively charged with a mean size of 500nm, suitable for uptake within the gastrointestinal tract. Insulin association efficiency was over 70% and wasreleased in a pH-dependent manner under simulated gastrointestinal conditions. Orally delivered nanoparticleslowered basal serum glucose levels in diabetic rats around 35% with 50 and 100 IU/kg doses sustaininghypoglycemia over 24 h. Pharmacological availability was 5.6 and 3.4% for the 50 and 100 IU/kg doses,respectively, a significant increase over 1.6%, determined for oral insulin alone in solution. Confocal microscopicexaminations of FITC-labeled insulin nanoparticles showed adhesion to rat intestinal epithelium, and internalizationof insulin within the intestinal mucosa. Encapsulation of insulin into dextran sulfate/chitosan nanoparticles wasa key factor in the improvement of the bioavailability of its oral delivery over insulin solution.