Tuesday, May 29, 2018

PLGA-PEG-Mal from PolySciTech used as part of oral exenatide formulation development for diabetes treatment



Convenience is one of the often overlooked aspects of medical technology, however it is critical as convenience encourages patient compliance with medicinal regimens. Naturally, patients prefer oral formulations over injected formulations. Some medicines, however, have very poor absorption from the GI tract, which limits their ability to be administered by this route. Exenatide, a drug which treats diabetes, is one example of a poorly absorbed medicine. Recently, researchers at Binzhou Medical University, Yantai University, and Luye Pharmaceutical Co. (China) used PLGA-PEG-Maleimide (PolyVivo AI020) and mPEG-PLGA (PolyVivo AK037) from PolySciTech (www.polyscitech.com) to generate nanoparticles to cross the intestinal barrier to improve the oral bioavailability of exanatide. This research holds promise to offer an oral therapy for diabetes. Read more: Zhang, Liping, Yanan Shi, Yina Song, Xinfeng Sun, Xuemei Zhang, Kaoxiang Sun, and Youxin Li. "The use of low molecular weight protamine to enhance oral absorption of exenatide." International Journal of Pharmaceutics (2018). https://www.sciencedirect.com/science/article/pii/S0378517318303648

“Abstract: Although oral delivery of exenatide has significant advantages, its poor permeability through intestinal epithelial membranes and rapid digestion by pepsin and ereptase in the gastrointestinal tract make effective oral delivery of exenatide a formidable challenge. In this study, we constructed a zinc ion (Zn2+) and exenatide complex functionalized nanoparticle (NP) oral delivery system to overcome the above-mentioned issue. Polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) was used as a drug carrier to escape enzymatic degradation in the gastrointestinal tract, and low molecular weight protamine (LMWP) was used as a functional group to increase penetration of NPs into the intestinal epithelium. The functionalized NPs exhibited significantly improved penetration across the intestinal epithelium, as shown by cell uptake and transmembrane transport experiments. Moreover, a significant hypoglycemic effect was observed in diabetic rats. The relative bioavailability of the orally administered functionalized NPs vs. subcutaneous injection was 7.44%, 29-fold that of the exenatide-Zn2+ solution group. These findings indicate that our modification could effectively improve exenatide treatment. Keywords: Low molecular weight protamine PEG-PLGA Functionalized nanoparticle Exenatide-Zn2+ Oral delivery”

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