PLGA-PEG-Mal from PolySciTech used in development of oral insulin delivery system

 

Diabetes is a common and debilitating disease caused by inappropriate concentration of glucose in the blood stream. It is often treated using insulin however insulin must typically be injected which is painful and unpleasant leading to poor patient compliance. Recently, researchers at University of Porto (Portugal) and Oslo University (Norway) used PLGA-PEG-Mal (AI110) from PolySciTech (www.polyscitech.com) to create labeled nanoparticles. These particles were loaded with insulin and tested in animal model for absorption. This research holds promise for improved therapies against diabetes in the future. Read more: Azevedo, Cláudia, Jeannette Nilsen, Algirdas Grevys, Rute Nunes, Jan Terje Andersen, and Bruno Sarmento. "Engineered albumin-functionalized nanoparticles for improved FcRn binding enhance oral delivery of insulin." Journal of Controlled Release (2020). https://www.sciencedirect.com/science/article/pii/S0168365920304363

“Abstract: Oral delivery of biopharmaceuticals, as insulin, is hampered by rapid degradation and inefficient absorption in the gastrointestinal tract (GIT). To solve this, a new class of biodegradable poly(lactic-co-glycolic)-poly(ethylene glycol) (PLGA-PEG) mucodiffusive nanoparticles (NPs) was designed. Specifically, these were decorated with site-specific conjugated human albumin, engineered for improved pH dependent binding to the neonatal Fc receptor (FcRn), which naturally mediates transport of albumin across the intestinal epithelium. The designed NPs of monodisperse 150 nm in size were 10% loaded with insulin and their surface was successfully functionalized with human albumin. Importantly, the engineered albumin-functionalized NPs bound human FcRn favorably in a pH dependent manner and showed enhanced transport across polarized cell layers. When orally administered to human FcRn expressing mice induced with diabetes, a reduction of glycemia was measured as a function of receptor targeting, with up to around 40% reduction after 1 h post-delivery. Thus, biodegradable PLGA-PEG NPs decorated with human albumin for improved FcRn-dependent transport offer a novel attractive strategy for delivery of encapsulated biopharmaceuticals across intestinal barriers. Keywords: Engineered albumin variants FcRn binding Glycemic decrease Intestinal permeability PLGA-PEG nanoparticles Type 1 diabetes mellitus”