International Journal of Nanomedicine (Feb 2020)
Rhynchophylline Loaded-mPEG-PLGA Nanoparticles Coated with Tween-80 for Preliminary Study in Alzheimer’s Disease
Abstract
Ruiling Xu, 1 Junying Wang, 1 Juanjuan Xu, 1 Xiangrong Song, 2 Hai Huang, 2 Yue Feng, 3 Chunmei Fu 1 1Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, People’s Republic of China; 2State Key Laboratory of Biotherapy/Geriatrics and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center for Biotherapy, Sichuan University, Chengdu, People’s Republic of China; 3College of Pharmacy, Southwest University for Nationalities, Chengdu 610041, People’s Republic of ChinaCorrespondence: Chunmei FuKey Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry and Sichuan Province, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, People’s Republic of ChinaEmail [email protected]: Alzheimer’s disease (AD) is a growing concern in the modern society. The current drugs approved by FDA are not very promising. Rhynchophylline (RIN) is a major active tetracyclic oxindole alkaloid stem from traditional Chinese medicine uncaria species, which has potential activities beneficial for the treatment of AD. However, the application of rhynchophylline for AD treatment is restricted by the low water solubility, low concentration in brain tissue and low bioavailability. And there is no study of brain-targeting therapy with RIN. In this work, we prepared rhynchophylline loaded methoxy poly (ethylene glycol)–poly (dl-lactide-co-glycolic acid) (mPEG-PLGA) nanoparticles (NPS-RIN), which coupled with Tween 80 (T80) further for brain targeting delivery (T80-NPS-RIN).Methods: Preparation and characterization of T80-NPS-RIN were followed by the detection of transportation across the blood–brain barrier (BBB) model in vitro, biodistribution and neuroprotective effects of nanoparticles.Results: The results indicated T80-NPS-RIN could usefully assist RIN to pass through the BBB to the brain. T80-NPS-RIN treatment regulated the activity of neurons in vitro.Conclusion: The presented data confirmed that rhynchophylline encapsulated mPEG-PLGA nanoparticles coated with Tween 80 could across through the BBB and exhibited efficient neuroprotective effects. The T80-NPS-RIN nanoparticles have a chance to be an alternative drug to the therapy of AD.Keywords: Alzheimer’s disease, rhynchophylline, nanoparticles, blood–brain barrier, neuroprotective effect
