PEG-PLGA from PolySciTech used in development of oral peptide delivery system for anti-inflammatory applications

 

Typically, peptides (shorter versions of proteins) can not be readily delivered as an oral formulation such as tablet or solution because most peptides are destroyed in the stomach and have poor transportation across the intestinal lining. This is unfortunate as peptide-based drugs are quite effective against a range of disease states and opening up more routes of administration can improve their application range. Recently, researchers at The University of Queensland (Australia) utilized mPEG-PLGA (cat# AK026) from PolySciTech division of Akina (www.polyscitech.com) to develop nanoparticles for oral delivery of anti-inflammatory peptides. This research holds promise to improve therapeutic routes for peptide delivery. Read more: Xu, Weizhi, Vinod Kumar, Cedric S. Cui, Xaria X. Li, Andrew K. Whittaker, Zhi Ping Xu, Maree T. Smith, Trent M. Woodruff, and Felicity Y. Han. "Success in navigating hurdles to oral delivery of a bioactive peptide complement antagonist through use of nanoparticles to increase bioavailability and in vivo efficacy." Advanced Therapeutics (2022): 2200109. https://onlinelibrary.wiley.com/doi/abs/10.1002/adtp.202200109

“Abstract: Substantial preclinical data have validated cyclic hexapeptide, complement C5a receptor 1 antagonists (C5aRAs) that target immune cells as novel treatments for a range of inflammatory diseases which currently have limited effective treatment options. However, like most small-molecule peptides, their poor oral bioavailability and short circulation half-life are major hurdles that have limited their clinical translation. Here, a single emulsion technique was employed to produce poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) with exceptionally high peptide C5aRA (PMX205) loading efficiency (over 50%). Strikingly, the PMX205-NPs not only facilitated prolonged release of the encapsulated PMX205 but also dramatically increased its oral bioavailability (from ∼25% to ∼50%), and therapeutic potential (∼ 95% inhibition of C5a induced neutrophilia in mice and maintenance of neuroprotective barrier integrity). The enhanced in vivo pharmacological activity of PMX205 in the form of NPs opens an exciting opportunity for the clinical application of peptide C5aRAs and possibly other therapeutic peptides. Keywords: C5aR1 antagonists (C5aRAs); bioactive peptide; nanoparticles (NPs); poly(lactic-coglycolic) acid (PLGA); oral bioavailability; pharmacokinetics and blood-brain barrier.”