John Garner

Mal-PEG-PLGA from PolySciTech used in development of oral-exanatide formulation for improved diabetes treatment.

Blog Post created by John Garner on Apr 9, 2018

2018 Exanatide delivery.jpg

The incidence of type 2 diabetes has expanded rapidly over the past several decades and is characterized by uncontrolled blood-sugar. Exanatide is a peptide based drug which acts to increase the pancreas response for insulin secretion as a means to control blood sugar. Due to the sensitivity of this peptide to degradation, as well as its poor bioavailability, it is currently only available as an injection. Recently, researchers at Yantai University and Binzhou Medical University (China) used Mal-PEG-PLGA (PolyVivo AI020) and PEG-PLGA (AK037) from PolySciTech ( to develop a transferrin-coated exenatide delivery nanoparticle system that could be ingested and had high bioavailablity. This research holds promise for the development of improved oral diabetes treatment options. Read more: Zhang, Liping, Yanan Shi, Yina Song, Dongyu Duan, Xuemei Zhang, Kaoxiang Sun, and Youxin Li. "Tf ligand-receptor-mediated exenatide-Zn2+ complex oral-delivery system for penetration enhancement of exenatide." Journal of Drug Targeting just-accepted (2018): 1-36.

“Abstract: Safe and effective oral delivery of peptide is a challenge. Here, we used exenatide and zinc ions (Zn2+) to form a complex to explore a meaningful oral-targeted drug-delivery system. Polyethylene glycol-poly(lactic acid-co-glycolic acid) (PEG-PLGA) was used to prepare nanoparticles (NPs) to escape the degradation caused by gastrointestinal enzymes. Transferrin (Tf) was used as a targeting group. PEG-PLGA-NPs and Tf-modified exenatide-Zn2+-loaded NPs (Tf-PEG-PLGA-NPs) were uniformly sized spheres according to transmission electron microscopy. The results of pharmacodynamic and pharmacokinetic investigations in vivo were consistent with in vitro studies using Caco-2 cells. Tf enhanced NPs transport in cell-uptake and transmembrane-transport experiments. Our results showed that the relative bioavailability of Tf-exenatide-Zn2+-NPs was higher than that of exenatide-Zn2+-NPs. The relative bioavailability of Tf-exenatide-Zn2+-NPs versus subcutaneous injection of exenatide was 6.45%. This was a preliminary exploration of the oral administration of exenatide, that data from which can be used for future investigations. Keywords: transferrin, exenatide-Zn2+, PEG-PLGA, targeted nanoparticles, oral delivery”


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