Nanotechnology-based drug delivery of ropinirole for Parkinson’s disease

Drug Delivery

Sofía Negro¹  Emilia Barcia¹  Yaquelyn Casanova¹  Liudmila Boeva¹  Ana Fernández-Carballido¹  Karla Slowing²  Luis García-García³ 

[1] Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Madrid, Spain;Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, Madrid, Spai;Unidad de Cartografía Cerebral, Instituto Pluridisciplinar, Universidad Complutense de Madrid, Madrid, Spain;

关键词: Ropinirole;    nanoparticles;    poly (D,L-lactide-co-glycolide);    Parkinson’s disease;   

DOI  :  10.1080/10717544.2017.1359862

来源: Taylor & Francis

【 摘 要 】

A new drug delivery system is developed for ropinirole (RP) for the treatment of Parkinson’s disease (PD) consisting of biodegradable poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles (NPs). The formulation selected was prepared with 8 mg RP and 50 mg PLGA 502. This formulation exhibited mean encapsulation efficiency of 74.8 ± 8.2%, mean particle size lower than 155 nm, the zeta potential of −14.25 ± 0.43 mV and zero-order in vitro release of RP (14.13 ± 0.17 μg/h/10 mg NPs) for 5 d. Daily doses of the neurotoxin rotenone (2 mg/kg) given i.p. to male Wistar rats induced neuronal and behavioral changes similar to those of PD. Once neurodegeneration was established (15 d) animals received RP in saline (1 mg/kg/d for 35 d) or encapsulated within PLGA NPs (amount of NPs equivalent to 1 mg/kg/d RP every 3 d for 35 d). Brain histology and immunochemistry (Nissl-staining, glial fibrillary acidic protein and tyrosine hydroxylase immunohistochemistry) and behavioral testing (catalepsy, akinesia, rotarod and swim test) showed that RP-loaded PLGA NPs were able to revert PD-like symptoms of neurodegeneration in the animal model assayed.

【 授权许可】

CC BY