PLGA-PEG derivatives from PolySciTech used in development of targeted nanoparticle for treatment of type-1 diabetes

 

Approximately 1.9 million Americans have type 1 diabetes (diabetes.org), a chronic condition in which the pancreas produces little or no insulin. One way to target nanoparticles is to functionalize them with a particular ligand, although typically a peptide or protein any molecule which provides good binding can be used for this. Researchers at Universidade do Porto and Universidade do Minho used PLGA-PEG-COOH (AI171), PLGA-PEG-Mal (AI110), and PLGA-Rhodamine (AV011) from PolySciTech division of Akina, Inc. (www.polyscitech.com) to create nanoparticles surface functionalized with exenatide (GLP1 binding) for delivery of peptide therapy to the pancreatic-based insulin system. This research holds promise for improved treatment of diabetes in the future. Read more: Cristelo, Cecília, Rute Nunes, Soraia Pinto, Joana Moreira Marques, Francisco Miguel Gama, and Bruno Sarmento. "Targeting β Cells with Cathelicidin Nanomedicines Improves Insulin Function and Pancreas Regeneration in Type 1 Diabetic Rats." ACS Pharmacology & Translational Science (2023). https://pubs.acs.org/doi/abs/10.1021/acsptsci.3c00218

“Type 1 diabetes (T1D) is an incurable condition with an increasing incidence worldwide, in which the hallmark is the autoimmune destruction of pancreatic insulin-producing β cells. Cathelicidin-based peptides have been shown to improve β cell function and neogenesis and may thus be relevant while developing T1D therapeutics. In this work, a cathelicidin-derived peptide, LLKKK18, was loaded in poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), surface-functionalized with exenatide toward a GLP-1 receptor, aiming the β cell-targeted delivery of the peptide. The NPs present a mean size of around 100 nm and showed long-term stability, narrow size distribution, and negative ζ-potential (−10 mV). The LLKKK18 association efficiency and loading were 62 and 2.9%, respectively, presenting slow and sustained in vitro release under simulated physiologic fluids. Glucose-stimulated insulin release in the INS-1E cell line was observed in the presence of the peptide. In addition, NPs showed a strong association with β cells from isolated rat islets. After administration to diabetic rats, NPs induced a significant reduction of the hyperglycemic state, an improvement in the pancreatic insulin content, and glucose tolerance. Also remarkable, a considerable increase in the β cell mass in the pancreas was observed. Overall, this novel and versatile nanomedicine showed glucoregulatory ability and can pave the way for the development of a new generation of therapeutic approaches for T1D treatment.”

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