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Article

Micro- and Nano-Systems Developed for Tolcapone in Parkinson’s Disease

1
Department of Pharmaceutics and Food Technology, School of Pharmacy, Universidad Complutense de Madrid, Ciudad Universitaria s/n, 28040 Madrid, Spain
2
Institute of Industrial Pharmacy, Universidad Complutense de Madrid, Ciudad Universitaria s/n, 28040 Madrid, Spain
3
Department of Pharmacology, Pharmacognosy and Botany, School of Pharmacy, Universidad Complutense de Madrid, Ciudad Universitaria s/n, 28040 Madrid, Spain
4
Brain Mapping Lab, Pluridisciplinary Research Institute, Universidad Complutense de Madrid, Ciudad Universitaria s/n, 28040 Madrid, Spain
*
Author to whom correspondence should be addressed.
Academic Editor: Patrick T. Ronaldson
Pharmaceutics 2022, 14(5), 1080; https://doi.org/10.3390/pharmaceutics14051080
Received: 21 April 2022 / Revised: 12 May 2022 / Accepted: 17 May 2022 / Published: 17 May 2022
(This article belongs to the Special Issue Brain-Targeted Drug Delivery)
To date there is no cure for Parkinson’s disease (PD), a devastating neurodegenerative disorder with levodopa being the cornerstone of its treatment. In early PD, levodopa provides a smooth clinical response, but after long-term therapy many patients develop motor complications. Tolcapone (TC) is an effective adjunct in the treatment of PD but has a short elimination half-life. In our work, two new controlled delivery systems of TC consisting of biodegradable PLGA 502 (poly (D,L-lactide-co-glycolide acid) microparticles (MPs) and nanoparticles (NPs) were developed and characterized. Formulations MP-TC4 and NP-TC3 were selected for animal testing. Formulation MP-TC4, prepared with 120 mg TC and 400 mg PLGA 502, exhibited a mean encapsulation efficiency (EE) of 85.13%, and zero-order in vitro release of TC for 30 days, with around 95% of the drug released at this time. Formulation NP-TC3, prepared with 10 mg of TC and 50 mg of PLGA 502, exhibited mean EE of 56.69%, particle size of 182 nm, and controlled the release of TC for 8 days. Daily i.p. (intraperitoneal) doses of rotenone (RT, 2 mg/kg) were given to Wistar rats to induce neurodegeneration. Once established, animals received TC in saline (3 mg/kg/day) or encapsulated within formulations MP-TC4 (amount of MPs equivalent to 3 mg/kg/day TC every 14 days) and NP-TC3 (amount of NPs equivalent to 3 mg/kg/day TC every 3 days). Brain analyses of Nissl-staining, GFAP (glial fibrillary acidic protein), and TH (tyrosine hydroxylase) immunohistochemistry as well as behavioral testing (catalepsy, akinesia, swim test) showed that the best formulation was NP-TC3, which was able to revert PD-like symptoms of neurodegeneration in the animal model assayed. View Full-Text
Keywords: tolcapone; microparticles; nanoparticles; PLGA; Parkinson’s disease tolcapone; microparticles; nanoparticles; PLGA; Parkinson’s disease
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MDPI and ACS Style

Casanova, Y.; Negro, S.; Slowing, K.; García-García, L.; Fernández-Carballido, A.; Rahmani, M.; Barcia, E. Micro- and Nano-Systems Developed for Tolcapone in Parkinson’s Disease. Pharmaceutics 2022, 14, 1080. https://doi.org/10.3390/pharmaceutics14051080

AMA Style

Casanova Y, Negro S, Slowing K, García-García L, Fernández-Carballido A, Rahmani M, Barcia E. Micro- and Nano-Systems Developed for Tolcapone in Parkinson’s Disease. Pharmaceutics. 2022; 14(5):1080. https://doi.org/10.3390/pharmaceutics14051080

Chicago/Turabian Style

Casanova, Yaquelyn, Sofía Negro, Karla Slowing, Luis García-García, Ana Fernández-Carballido, Mahdieh Rahmani, and Emilia Barcia. 2022. "Micro- and Nano-Systems Developed for Tolcapone in Parkinson’s Disease" Pharmaceutics 14, no. 5: 1080. https://doi.org/10.3390/pharmaceutics14051080

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