Oral delivery of the amylin receptor agonist pramlintide
Oral delivery of pramlintide-loaded microparticles resulted in a release duration of 120 minutes, which is significantly longer than the 30 minutes observed with the solution form.
Where it sits
this study against the rest of the pramlintide corpusSummary and findings
This study aimed to design and characterize polymeric microparticles for the oral delivery of pramlintide. The microparticles were evaluated for various parameters including encapsulation efficiency and pharmacokinetics in mice. Results indicated a protracted release of pramlintide from microparticles compared to the solution form.
Abstract
<h4>Aim</h4> 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. <h4>Methods</h4> 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. <h4>Results</h4> We obtained spherical microcapsules, with particle size of 66 μm ± 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. <h4>Conclusions</h4> Oral route is an alternative for therapeutic development of pramlintide formulations. <h4>Graphical abstract</h4>