Lopes Marlene, Aniceto Denise, Abrantes Margarida, Simões Susana, Branco Fábio, Vitória Isabel, Botelho M Filomena, Seiça Raquel, Veiga Francisco, Ribeiro António
Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal; CNC-Center for Neuroscience and Cell Biology, 3004-504 Coimbra, Portugal.
Faculty of Pharmacy, University of Coimbra, 3000-548 Coimbra, Portugal; CNC-Center for Neuroscience and Cell Biology, 3004-504 Coimbra, Portugal; Biophysics Institute, Faculty of Medicine, University of Coimbra, Portugal; CIMAGO, FMUC-Faculty of Medicine, University of Coimbra, Portugal; CNC.IBILI, University of Coimbra, 3000-548 Coimbra, Portugal.
Eur J Pharm Biopharm. 2017 Apr;113:88-96. doi: 10.1016/j.ejpb.2016.11.037. Epub 2016 Dec 19.
This study aimed to assess the biodistribution of antihyperglycemic insulin-loaded alginate/dextran sulfate-based nanoparticles dual coated with chitosan and technetium-99m-albumin (Tc-BSA) after oral administration. The oral administration of 50IU/kg insulin-loaded nanoparticles to type 1 diabetic rats showed prolonged antihyperglycemic effects up to 12h and relative pharmacological availability of 5.04% comparing to the subcutaneous administration. The oral antihyperglycemic effect was further compared between type 1 and type 2 diabetic models by the intraperitoneal glucose tolerance test, revealing that the effect lasted longer in the type 1 diabetic model. Tc-BSA revealed to be a good nanoparticles' tracer since there was no systemic absorption and Tc-BSA-nanoparticles were capable of increasing their residence time in the intestinal epithelium of balb-c mice when compared with Tc-BSA biodistribution. Thus, this biopolymeric-based delivery nanoparticulate system is a promising tool for the therapy of type 1 and type 2 diabetic individuals and prevention of T1D.
本研究旨在评估口服给药后，用壳聚糖和锝-99m-白蛋白（Tc-BSA）双重包被的、负载抗高血糖胰岛素的藻酸盐/硫酸葡聚糖基纳米颗粒的生物分布。对1型糖尿病大鼠口服50IU/kg负载胰岛素的纳米颗粒，显示出长达12小时的延长抗高血糖作用，与皮下给药相比，相对药理利用率为5.04%。通过腹腔葡萄糖耐量试验进一步比较了1型和2型糖尿病模型的口服抗高血糖作用，结果显示该作用在1型糖尿病模型中持续时间更长。Tc-BSA被证明是一种良好的纳米颗粒示踪剂，因为没有全身吸收，并且与Tc-BSA生物分布相比，Tc-BSA纳米颗粒能够增加其在balb-c小鼠肠上皮中的停留时间。因此，这种基于生物聚合物的递送纳米颗粒系统是治疗1型和2型糖尿病个体以及预防1型糖尿病的有前途的工具。
