Nanoparticle based Parkinson’s disease treatment developed using block PEG-PLGA and maleimide reactive intermediates from PolySciTech

Parkinson’s disease is both fatal and the second most common neurodegenerative disease in the world. One of the difficulties with treating it is formulating medicines so that they can cross from the blood-stream over into the brain tissue. Recently, researchers utilized block mPEG-PLGA (PolyVivo #AK104) and maleimide-PEG-PLGA (PolyVivo # AI109) from PolySciTech (www.polyscitech.com) to create a nanoparticle loaded with rotigotine, a dopamine agonist effective for Parkinson’s therapy. They used the maleimide groups to conjugate lactoferrin on the outside which assisted with uptake across the blood brain barrier. This system showed promise for non-toxic uptake into the brain when administered via intranasal route in mouse model. This research holds promise to provide for improved therapies for Parkinson’s disease.  Read more: Bi, Chenchen, Aiping Wang, Yongchao Chu, Sha Liu, Hongjie Mu, Wanhui Liu, Zimei Wu, Kaoxiang Sun, and Youxin Li. "Intranasal delivery of rotigotine to the brain with lactoferrin-modified PEG-PLGA nanoparticles for Parkinson’s disease treatment." International Journal of Nanomedicine 11 (2016): 6547. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5153272/

“Abstract: Sustainable and safe delivery of brain-targeted drugs is highly important for successful therapy in Parkinson’s disease (PD). This study was designed to formulate biodegradable poly(ethylene glycol)–poly(lactic-co-glycolic acid) (PEG-PLGA) nanoparticles (NPs), which were surface-modified with lactoferrin (Lf), for efficient intranasal delivery of rotigotine to the brain for the treatment of PD. Rotigotine NPs were prepared by nanoprecipitation, and the effect of various independent process variables on the resulting properties of NPs was investigated by a Box–Behnken experimental design. The physicochemical and pharmaceutical properties of the NPs and Lf-NPs were characterized, and the release kinetics suggested that both NPs and Lf-NPs provided continuous, slow release of rotigotine for 48 h. Neither rotigotine NPs nor Lf-NPs reduced the viability of 16HBE and SH-SY5Y cells; in contrast, free rotigotine was cytotoxic. Qualitative and quantitative cellular uptake studies demonstrated that accumulation of Lf-NPs was greater than that of NPs in 16HBE and SH-SY5Y cells. Following intranasal administration, brain delivery of rotigotine was much more effective with Lf-NPs than with NPs. The brain distribution of rotigotine was heterogeneous, with a higher concentration in the striatum, the primary region affected in PD. This strongly suggested that Lf-NPs enable the targeted delivery of rotigotine for the treatment of PD. Taken together, these results demonstrated that Lf-NPs have potential as a carrier for nose-to-brain delivery of rotigotine for the treatment of PD. Keywords: rotigotine, lactoferrin-modified PEG-PLGA nanoparticles, brain targeting, intranasal delivery, Parkinson’s disease”