Sinezia, C.; Sisnande, T.; Icart, L. P.; Lima, L. M. T.

Aim: The aims of this study were to design and characterize polymeric microparticles for oral delivery of pramlintide, a triple proline human amylin analogue clinically proved efficient in diabetes therapy. Methods: The microparticles were prepared with gastric-resistant polymer Eudragit S100 by double-emulsion and solvent evaporation technique. The study responses were repeatability, encapsulation efficiency, yield, morphology, particle size, response to acidic and alkaline milieu and pharmacokinetics. Results: We obtained spherical microcapsules, with particle size of 66 micrometer + 11, with 83.2 % + 2.7 efficiency for pramlintide entrapment and 67.6 % + 2.1 yield. Intra-venous pramlintide free in solution showed a plasmatic half-life of 6.8 min in mice. In contrast, oral delivery of acid-resistant pramlintide-loaded microparticles in mice showed a protracted release for 120 min compared to 30 min obtained for pramlintide in solution. Conclusions: Oral route is an alternative for therapeutic development of pramlintide formulations.