John Garner

Mal-PEG-PLGA and mPEG-PLGA from PolySciTech used in development of nanoparticle-based Parkinson’s treatment

Blog Post created by John Garner on Jan 17, 2018

Yan, 2018 rotigotine brain parkinson polyscitech PEG-PLGA.png

Parkinson’s disease is a wide-spread neurodegenerative disorder with over 200,000 USA cases per year. The primary symptoms are loss of control over muscle movements which get progressively worse with time. This disease is caused by damage to dopaminergic neurons which leads to a lack of dopamine in the brain. Although incurable, there are drugs that can delay the progression of Parkinson’s. Because the drug action must occur within the brain, any medicine applied must cross the blood-brain-barrier, a screen that prevents most medicines from reaching the brain. Recently, researchers at Yantai University and Shandong Luye Pharmaceutics utilized mal-PEG-PLGA (Polyvivo AI109) and mPEG-PLGA (PolyVivo AK104) from PolySciTech (www.polyscitech.com) to generate lactoferin-decorated nanoparticles for rotigotine delivery across the blood-brain-barrier as a potential treatment for Parkinson’s disease. This research holds promise to halt the progress of this lethal disease. Read more: Yan X, Xu L, Bi C, Duan D, Chu L, Yu X, Wu Z, Wang A, Sun K “Lactoferrin-modified rotigotine nanoparticles for enhanced nose-to-brain delivery: LESA-MS/MS-based drug biodistribution, pharmacodynamics, and neuroprotective effects” International Journal of Nanomedicine, 9 January 2018 Volume 2018:13 Pages 273—281 https://www.dovepress.com/lactoferrin-modified-rotigotine-nanoparticles-for-enha nced-nose-to-bra-peer-reviewed-fulltext-article-IJN

“Introduction: Efficient delivery of rotigotine into the brain is crucial for obtaining maximum therapeutic efficacy for Parkinson’s disease (PD). Therefore, in the present study, we prepared lactoferrin-modified rotigotine nanoparticles (Lf-R-NPs) and studied their biodistribution, pharmacodynamics, and neuroprotective effects following nose-to-brain delivery in the rat 6-hydroxydopamine model of PD. Materials and methods: The biodistribution of rotigotine nanoparticles (R-NPs) and Lf-R-NPs after intranasal administration was assessed by liquid extraction surface analysis coupled with tandem mass spectrometry. Contralateral rotations were quantified to evaluate pharmacodynamics. Tyrosine hydroxylase and dopamine transporter immunohistochemistry were performed to compare the neuroprotective effects of levodopa, R-NPs, and Lf-R-NPs. Results: Liquid extraction surface analysis coupled with tandem mass spectrometry analysis, used to examine rotigotine biodistribution, showed that Lf-R-NPs more efficiently supplied rotigotine to the brain (with a greater sustained amount of the drug delivered to this organ, and with more effective targeting to the striatum) than R-NPs. The pharmacodynamic study revealed a significant difference (P<0.05) in contralateral rotations between rats treated with Lf-R-NPs and those treated with R-NPs. Furthermore, Lf-R-NPs significantly alleviated nigrostriatal dopaminergic neurodegeneration in the rat model of 6-hydroxydopamine-induced PD. Conclusion: Our findings show that Lf-R-NPs deliver rotigotine more efficiently to the brain, thereby enhancing efficacy. Therefore, Lf-R-NPs might have therapeutic potential for the treatment of PD. Keywords: lactoferrin-modified rotigotine nanoparticles, nose to brain, drug biodistribution, pharmacodynamics, neuroprotective effects, Parkinson’s disease”

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