PLGA-PEG-Mal and PLGA-PEG-methyl from PolySciTech used in development of oral exanatide-nanoparticle based diabetes treatment

Medicinal technology developments have several goals, depending on the application. In some cases, the goal is to develop a completely new therapy which did not exist before. In other cases, it is to take an existing therapy and reformulate it to improve either efficacy or convenience. Oral formulations are well known to be more convenient for both patient and practitioner as, unlike parental injections, they can be easily self-administered by a patient, are not painful, and do not require handling/safe-disposal of blood-exposed syringes which could potential spread bloodborne pathogens. Diabetes, notably, requires a great deal of injection-based therapy as part of its treatment. One type of this therapy is Exanatide, a glucagen-like peptide 1 receptor which acts to treat type 2 diabetes. Currently Exanatide is only available as an injectable formulation (Bydureon) as oral uptake is very poor. Recently, researchers at Binzhou Medical University, Yantai University, Luye Pharmaceutical Co, and Peking University (China) use PLGA-PEG-Mal (PolyVivo AI020) and mPEG-PLGA (AK037, AK102) from PolySciTech (www.polyscitech.com) to develop Fc decorated nanoparticles capable of crossing the intestinal mucosa for more effective delivery. This research holds promise to provide for a more convenient and effective therapy for diabetes. Read more: Shi, Yanan, Xinfeng Sun, Liping Zhang, Kaoxiang Sun, Keke Li, Youxin Li, and Qiang Zhang. "Fc-modified exenatide-loaded nanoparticles for oral delivery to improve hypoglycemic effects in mice." Scientific Reports 8, no. 1 (2018): 726. https://www.nature.com/articles/s41598-018-19170-y

“Abstract: To improve the oral efficiency of exenatide, we prepared polyethylene glycol-poly(lactic-co-glycolic acid) (PEG-PLGA) NPs modified with Fc (NPs-Fc) for exenatide oral delivery. Exenatide was encapsulated into the NPs by the w/o/w emulsion-solvent evaporation method. The particle size of the NPs-Fc was approximately 30 nm larger than that of the unmodified NPs with polydispersity indices in a narrow range (PDIs; PDI < 0.3) as detected by DLS, and the highest encapsulation efficiency of exenatide in the NPs was greater than 80%. Fc-conjugated NPs permeated Caco-2 cells faster and to a greater extent compared to unmodified NPs, as verified by CLSM and flow cytometry. Hypoglycemic effect studies demonstrated that oral administration of exenatide-loaded PEG-PLGA NPs modified by an Fc group extended the hypoglycemic effects compared with s.c. injection of the exenatide solution. Fluorescence-labeled NPs were used to investigate the effects of Fc targeting, and the results demonstrated that the NPs-Fc stayed in the gastrointestinal tract for a longer time in comparison with the unmodified NPs, as shown by the whole-body fluorescence images and fluorescence images of the dissected organs detected by in vivo imaging in live mice. Therefore, Fc-targeted nano-delivery systems show great promise for oral peptide/protein drug delivery.”