Abstract
A new controlled delivery system has been developed for ropinirole (RP) for the treatment of Parkinson´s Disease (PD) consisting in PLGA microparticles (MPs) which exhibited in vitro constant release of RP (78.23 µg/day/10 mg MPs) for 19 days. The neuroprotective effects of RP released from MPs were evaluated in SKN-AS cells after exposure to rotenone (20 µM). Cell apoptosis was significantly reduced by RP (100-120 µM). Daily doses of rotenone (2 mg/kg) given i.p. to rats induced neuronal and behavioral changes similar to those of PD. After 15 days, animals received RP in saline (1 mg/kg/day for 45 days) or as MPs at two dose levels (amount of MPs equivalent to 7.5 mg/kg or 15 mg/kg RP given on days 15 and 30). Brain immunochemistry (Nisslstaining, GFAP and TH immunohistochemistry) and behavioral testing (catalepsy, akinesia, rotarod and swim test) showed that animals receiving RP either in solution or encapsulated within the MPs reverted the PD symptoms with the best results obtained in animals receiving RP microspheres at the highest dose assayed, thereby confirming the potential therapeutic interest of the new RP delivery system.
Keywords: Ropinirole, PLGA, microspheres, rotenone, Parkinson´s disease, brain immunochemistry.
Current Pharmaceutical Design
Title:Efficacy of Ropinirole-Loaded PLGA Microspheres for the Reversion of Rotenone- Induced Parkinsonism
Volume: 23 Issue: 23
Author(s): Sofia Negro, Liudmilla Boeva, Karla Slowing, Ana Fernandez-Carballido, Luis Garcia-García and Emilia Barcia*
Affiliation:
- Dpto. Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia, Plaza Ramon y Cajal s/n, 28040 Madrid,Spain
Keywords: Ropinirole, PLGA, microspheres, rotenone, Parkinson´s disease, brain immunochemistry.
Abstract: A new controlled delivery system has been developed for ropinirole (RP) for the treatment of Parkinson´s Disease (PD) consisting in PLGA microparticles (MPs) which exhibited in vitro constant release of RP (78.23 µg/day/10 mg MPs) for 19 days. The neuroprotective effects of RP released from MPs were evaluated in SKN-AS cells after exposure to rotenone (20 µM). Cell apoptosis was significantly reduced by RP (100-120 µM). Daily doses of rotenone (2 mg/kg) given i.p. to rats induced neuronal and behavioral changes similar to those of PD. After 15 days, animals received RP in saline (1 mg/kg/day for 45 days) or as MPs at two dose levels (amount of MPs equivalent to 7.5 mg/kg or 15 mg/kg RP given on days 15 and 30). Brain immunochemistry (Nisslstaining, GFAP and TH immunohistochemistry) and behavioral testing (catalepsy, akinesia, rotarod and swim test) showed that animals receiving RP either in solution or encapsulated within the MPs reverted the PD symptoms with the best results obtained in animals receiving RP microspheres at the highest dose assayed, thereby confirming the potential therapeutic interest of the new RP delivery system.
Export Options
About this article
Cite this article as:
Negro Sofia, Boeva Liudmilla, Slowing Karla, Fernandez-Carballido Ana, Garcia-García Luis and Barcia Emilia*, Efficacy of Ropinirole-Loaded PLGA Microspheres for the Reversion of Rotenone- Induced Parkinsonism, Current Pharmaceutical Design 2017; 23 (23) . https://dx.doi.org/10.2174/1381612822666160928145346
DOI https://dx.doi.org/10.2174/1381612822666160928145346 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Recent Multi-target Approaches on the Development of Anti- Alzheimer's Agents Integrating Metal Chelation Activity
Current Medicinal Chemistry Effects of Vitamin A Deficiency and Opioids on Parvalbumin + Interneurons in the Hippocampus of the HIV-1 Transgenic Rat
Current HIV Research Developing Histone Deacetylase Inhibitors as Anti-Cancer Therapeutics
Current Medicinal Chemistry Mechanisms of Drug Resistance in Cancer Chemotherapy: Coordinated Role and Regulation of Efflux Transporters and Metabolizing Enzymes
Current Pharmaceutical Design ChemoImmunoModulation: Immune Regulation by the Antineoplastic Chemotherapeutic Agents
Current Medicinal Chemistry Gene Therapy for Parkinsons Disease: Progress and Challenges
Current Gene Therapy Separation of Ginseng Active Ingredients and their Roles in Cancer Metastasis Supplementary Therapy
Current Drug Metabolism Network Propagation Reveals Novel Features Predicting Drug Response of Cancer Cell Lines
Current Bioinformatics <i>In Vitro</i> Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of <i>Croton fluviatilis, Croton acutifolius</i>, and <i>Croton thorelii</i>
The Natural Products Journal Mechanism of Action of Limonene in Tumor Cells: A Systematic Review and Meta-Analysis
Current Pharmaceutical Design Nitroxides as Cancer Imaging Agents
Anti-Cancer Agents in Medicinal Chemistry FK506-Binding Proteins and Their Diverse Functions
Current Molecular Pharmacology Cyclodepsipeptides - Potential Drugs and Lead Compounds in the Drug Development Process
Current Medicinal Chemistry Curcumin and Curcumin-like Molecules: From Spice to Drugs
Current Medicinal Chemistry Metal Ions and Metal Complexes in Alzheimer’s Disease
Current Pharmaceutical Design Carbon Nano Tubes: Novel Drug Delivery System in Amelioration of Alzheimer’s Disease
Combinatorial Chemistry & High Throughput Screening Protective Effects of Pomegranate in Endothelial Dysfunction
Current Pharmaceutical Design Islet-Brain (IB)/JNK-Interacting Proteins (JIPs): Future Targets for the Treatment of Neurodegenerative Diseases?
Current Neurovascular Research Intercellular Crosstalk Via Extracellular Vesicles in Tumor Milieu as Emerging Therapies for Cancer Progression
Current Pharmaceutical Design Histone Deacetylase Inhibitors: Recent Insights from Basic to Clinical Knowledge & Patenting of Anti-Cancer Actions
Recent Patents on Anti-Cancer Drug Discovery