Efficacy of Ropinirole-Loaded PLGA Microspheres for the Reversion of Rotenone- Induced Parkinsonism.

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.

journal_name

Curr Pharm Des

authors

Negro S,Boeva L,Slowing K,Fernandez-Carballido A,Garcia-García L,Barcia E

doi

10.2174/1381612822666160928145346

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

3423-3431

issue

23

eissn

1381-6128

issn

1873-4286

pii

CPD-EPUB-78654

journal_volume

23

pub_type

杂志文章
  • The Relevance of Dietary Polyphenols in Cardiovascular Protection.

    abstract::The chemical structure of polyphenols consisting of aromatic rings, capable of quenching free radicals, makes them ideal candidates to protect against oxidation. Polyphenols are present in a variety of foods including grapes, berries, dark chocolate, coffee and tea to mention a few. A number of studies have shown that...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612823666170329144307

    authors: Murillo AG,Fernandez ML

    更新日期:2017-01-01 00:00:00

  • Heme oxygenase-1 as a therapeutic target in neurodegenerative diseases and brain infections.

    abstract::Heme oxygenase-1 (HO-1) catalyzes the degradation of heme to generate carbon monoxide, biliverdin and free iron. Increased HO-1 levels constitute an anatomopathological feature of many neurological diseases, such as neurodegenerative disorders and brain infections, which correlate with exacerbated oxidative stress and...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161208783597407

    authors: Cuadrado A,Rojo AI

    更新日期:2008-01-01 00:00:00

  • Therapeutic potential of cannabinoids in neurodegenerative disorders: a selective review.

    abstract::The endocannabinoid system (ECS) is now recognised as an important modulator of various central nervous system processes. More recently, an increasing body of evidence has accumulated to suggest antioxidant, anti-inflammatory and neuroprotective roles of ECS. In this review we discuss the role and therapeutic potentia...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/13816128113199990434

    authors: Velayudhan L,Van Diepen E,Marudkar M,Hands O,Suribhatla S,Prettyman R,Murray J,Baillon S,Bhattacharyya S

    更新日期:2014-01-01 00:00:00

  • Peri-procedural Anticoagulation in Catheter Ablation for Atrial Fibrillation: A Review.

    abstract::Catheter ablation for rhythm control in atrial fibrillation has been recognized as an established treatment. Patients with atrial fibrillation suffer from an increased risk of thromboembolic events. Long-term stroke risk and mortality have been shown to be reduced after catheter ablation, still the procedure per se is...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612822666161205115101

    authors: Vrachatis DA,Giannopoulos G,Kossyvakis C,Panagopoulou V,Vavuranakis M,Papaioannou TG,Pagoni S,Pyrgakis VN,Cleman MW,Deftereos SG

    更新日期:2017-01-01 00:00:00

  • Radiolabelled peptides and monoclonal antibodies for therapy decision making in inflammatory diseases.

    abstract::Radiolabelled peptides and monoclonal antibodies are an emerging class of radiopharmaceuticals for imaging inflammation with clinical implications for several chronic inflammatory disorders for diagnosis, therapy decision making and follow up. In the last decades, a number of novel monoclonal antibodies and peptides h...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161208785777414

    authors: Malviya G,Signore A,Laganà B,Dierckx RA

    更新日期:2008-01-01 00:00:00

  • Epicardial adipose tissue as new cardio-metabolic risk marker and potential therapeutic target in the metabolic syndrome.

    abstract::Increased visceral adiposity, is an emerging cardiovascular risk factor. There is now a compelling need to quantify visceral adipose tissue not only for diagnostic purposes, but also for therapeutic interventions with weight reduction drugs or pharmaceuticals targeted to adipose tissue, as well as anti-obesity medicat...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161207781039670

    authors: Iacobellis G,Sharma AM

    更新日期:2007-01-01 00:00:00

  • Naturally Occurring Plectranthus-derived Diterpenes with Antitumoral Activities.

    abstract::The study of natural sources such as plants, microorganisms and marine organisms has developed interest among the scientific community in recent years for their extensive and diverse chemical composition and consequent biological potential. The search for antitumor compounds is among the lead causes that justify phyto...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612825666190115144241

    authors: Garcia C,Teodósio C,Oliveira C,Oliveira C,Díaz-Lanza A,Reis C,Duarte N,Rijo P

    更新日期:2018-01-01 00:00:00

  • MicroRNA-34a promotes cardiomyocyte apoptosis post myocardial infarction through down-regulating aldehyde dehydrogenase 2.

    abstract::MicroRNA-34a (miR-34a) promotes apoptosis via down-regulating many anti-apoptotic proteins. Aldehyde dehydrogenase 2 (ALDH2) is an anti-apoptotic enzyme whose activity decline associates with myocardial injury. We tested hypothesis that miR-34a might play a pro-apoptotic role in myocardial infarction (MI) by down-regu...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章

    doi:10.2174/13816128113199990325

    authors: Fan F,Sun A,Zhao H,Liu X,Zhang W,Jin X,Wang C,Ma X,Shen C,Zou Y,Hu K,Ge J

    更新日期:2013-01-01 00:00:00

  • Serotonergic system and its role in epilepsy and neuropathic pain treatment: a review based on receptor ligands.

    abstract::The serotonergic system is involved in pathomechanisms of both epilepsy and neuropathic pain. So far, participation in the epileptogenesis and maintenance of epilepsy was proved for 5-HT1A, 5-HT2C, 5-HT3, 5-HT4 and 5-HT7 receptors as well as 5-HTT serotonin transporter. Depending on the receptor type or its localizati...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612821666141121114917

    authors: Panczyk K,Golda S,Waszkielewicz A,Zelaszczyk D,Gunia-Krzyzak A,Marona H

    更新日期:2015-01-01 00:00:00

  • Colchicum Genus in the Writings of Ancient Greek and Byzantine Physicians.

    abstract::The plants of the Colchicum family were known during the archaic period in Greece for their deleterious properties. Later on, they were used for the treatment of podagra. The treatment was introduced by the ancient Greek physicians and passed on to the Byzantine and Arabian physicians to endure until nowadays. The fir...

    journal_title:Current pharmaceutical design

    pub_type: 历史文章,杂志文章,评审

    doi:10.2174/1381612824666180115111546

    authors: Tsoucalas G,Papaioannou T,Panayiotakopoulos G,Saridaki Z,Vrachatis DA,Karamanou M

    更新日期:2018-01-01 00:00:00

  • The STAT3 inhibitor stattic impairs cardiomyocyte mitochondrial function through increased reactive oxygen species formation.

    abstract::The signal transducer and activator of transcription 3 (STAT3) transduces stress signals from the plasma membrane to the nucleus but has recently also been identified in mitochondria. Inhibition of cardiomyocyte mitochondrial STAT3 with the STAT3-specific inhibitor Stattic decreases ADP-stimulated respiration and enha...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章

    doi:10.2174/138161281939131127115940

    authors: Boengler K,Ungefug E,Heusch G,Schulz R

    更新日期:2013-01-01 00:00:00

  • Obstacles and Opportunities for Cholinergic Drug Development in the Treatment of Cognitive Disorders.

    abstract::The frequency of neuropsychiatric disorders is greater than that of cancer, cardiovascular disease, and diabetes combined, and is growing at a faster rate than any other ailments in the United States or Europe. Despite a considerable need for the development of treatments for central nervous system disorders, pharmace...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612822666160127111453

    authors: Schroeder RA,Wecker L,Philpot RM

    更新日期:2016-01-01 00:00:00

  • Vitamins in Heart Failure: Friend or Enemy?

    abstract:BACKGROUND:The failing heart is characterized by a depleted metabolic energy reserve and the upregulation of several molecular mechanisms leading to cardiac hypertrophy, inflammation, fibrosis, angiogenesis, and apoptosis. Dietary or non-dietary supplementation of vitamins could potentially benefit energy balance. OBJ...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612823666170321094711

    authors: Georgiopoulos G,Chrysohoou C,Vogiatzi G,Magkas N,Bournelis I,Bampali S,Gruson D,Tousoulis D

    更新日期:2017-01-01 00:00:00

  • Perinatal gene transfer to the liver.

    abstract::The liver acts as a host to many functions hence raising the possibility that any one may be compromised by a single gene defect. Inherited or de novo mutations in these genes may result in relatively mild diseases or be so devastating that death within the first weeks or months of life is inevitable. Some diseases ca...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161211797247541

    authors: McKay TR,Rahim AA,Buckley SM,Ward NJ,Chan JK,Howe SJ,Waddington SN

    更新日期:2011-01-01 00:00:00

  • Deubiquitinating enzymes as promising drug targets for infectious diseases.

    abstract::Deubiquitinating enzymes (DUBs) remove ubiquitin and ubiquitin-like modifications from proteins and they have been known to contribute to processes relevant in microbial infection, such as immune responses pathways. Numerous viral and bacterial DUBs have been identified, and activities of several host DUBs are known t...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612811319180008

    authors: Nanduri B,Suvarnapunya AE,Venkatesan M,Edelmann MJ

    更新日期:2013-01-01 00:00:00

  • Application of MALDI-TOF mass spectrometry in screening and diagnostic research.

    abstract::During the last years, mass spectrometry has revolutionised protein biochemistry and has advanced to a superior tool for the identification and detailed analysis of peptides and proteins. The high throughput allowed by some mass spectrometry platforms has enabled the important step from analysis of individual proteins...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612054546932

    authors: Pusch W,Kostrzewa M

    更新日期:2005-01-01 00:00:00

  • Approaches to gastrointestinal cytoprotection: from isolated cells, via animal experiments to healthy human subjects and patients with different gastrointestinal disorders.

    abstract::Our clinical observations proved that the the duodenal ulcer in patients healed without any inhibition of gastric acid secretion (1965), and the healing rates of atropine vs cimetidine vs Carbenoxolone were equal and superior to that of placebo in randomized, prospective and multiclinical study of DU patients (1978). ...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章

    doi:10.2174/138161211796197016

    authors: Mózsik G,Szabó IL,Czimmer J

    更新日期:2011-01-01 00:00:00

  • A pharmacological review of competitive inhibitors and substrates of high-affinity, sodium-dependent glutamate transport in the central nervous system.

    abstract::The acidic amino acid L-glutamate acts as both a primary excitatory neurotransmitter and a potential neurotoxin within the mammalian central nervous system. Functionally juxtaposed between these neurophysiological and pathological actions are an assorted group of integral membrane transporter proteins that rapidly and...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:

    authors: Bridges RJ,Kavanaugh MP,Chamberlin AR

    更新日期:1999-05-01 00:00:00

  • Air Pollution Exposure and Blood Pressure: An Updated Review of the Literature.

    abstract::Both high arterial blood pressure (BP) and elevated levels of fine particulate matter (PM2.5) air pollution have been associated with an increased risk for several cardiovascular (CV) diseases, including stroke, heart failure, and myocardial infarction. Given that PM2.5 and high BP are each independently leading risk ...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612822666151109111712

    authors: Giorgini P,Di Giosia P,Grassi D,Rubenfire M,Brook RD,Ferri C

    更新日期:2016-01-01 00:00:00

  • Role of probiotics in the management of pouchitis.

    abstract::The concept that the gut microbiota plays a major role in the development of pouchitis in ulcerative colitis patients after restorative proctocolectomy with ileal pouch-anal anastomosis, is widely accepted and supported by a widespread use of some antibiotics (metronidazole and/or ciprofloxacin, rifaximin) to treat th...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章

    doi:10.2174/13816128113196660724

    authors: Guslandi M

    更新日期:2014-01-01 00:00:00

  • Epigenetic modification in neuropathic pain.

    abstract::Neuropathic pain is characterized by complicated combination of positive (e.g., hyperalgesia and allodynia) and negative (e.g., hypoesthesia and hypoalgesia) symptoms, and is often refractory to conventional pharmacological agents, including morphine. Although the molecular mechanisms for positive symptoms are extensi...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612820666141027113923

    authors: Ueda H,Uchida H

    更新日期:2015-01-01 00:00:00

  • Collagen-binding integrins as pharmaceutical targets.

    abstract::In recent years, our understanding of the molecular interaction of collagens with their cognate integrin receptors has remarkably improved. Structural elucidations of both the integrin and the collagenous triple helix have contributed to this achievement. The structures of an entire integrin ectodomain and of an A-dom...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612053381738

    authors: Eble JA

    更新日期:2005-01-01 00:00:00

  • Bioactive peptides: are there more antihypertensive mechanisms beyond ACE inhibition?

    abstract::Diet has a high relevance in health. Hypertension is a major risk factor for cardiovascular diseases and has an important impact on public health, and consequently on countries economy. Scientific research gathered strong evidence about the role of several dietary factors either in etiology or in treatment/prevention ...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161212802651670

    authors: Marques C,Amorim MM,Pereira JO,Pintado ME,Moura D,Calhau C,Pinheiro H

    更新日期:2012-01-01 00:00:00

  • High-throughput screening identifies small molecule inhibitors of molecular chaperones.

    abstract::Heat shock proteins (HSPs) are involved in a number of cellular processes, including cell cycle, growth, and survival, apoptosis, stress responses, angiogenesis, and oncogenesis. Among the characterized HSPs, the molecular chaperone HSP90 has emerged as an exciting molecular target for cancer therapy since its discove...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:

    authors: Kondoh Y,Osada H

    更新日期:2013-01-01 00:00:00

  • The role of metabolism and toxicokinetics in retinoid teratogenesis.

    abstract::Retinoids (vitamin A and its analogs) exert profound effects on a wide variety of life processes, including morphogenesis and embryonic development. Several retinoids are also effective drugs for therapy of skin diseases and some types of cancer. However, the applicability of this class of compounds is limited by thei...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612013397708

    authors: Tzimas G,Nau H

    更新日期:2001-06-01 00:00:00

  • Recent advances of fluorescent technologies for drug discovery and development.

    abstract::Recent progresses in the development of fluorescent technologies become a reliable device for drug discovery research. The fluorescence tools offer attractive options for an opportunity to visualize the effects of drug candidates in the cells. The fluorescent tools, such as fluorescent protein, are regularly used in a...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161209789207006

    authors: Chakraborty C,Hsu CH,Wen ZH,Lin CS

    更新日期:2009-01-01 00:00:00

  • Drug carriers in pharmaceutical design: promises and progress.

    abstract::Ever since pure molecular entities have been adapted as drug, varied manifestations other than elimination of infections are frequently been acknowledged as side effects. Contemporary drug research focuses on these issues besides developing new molecules for the restoration of unnatural functional deviations in variou...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161207780249119

    authors: Dutta RC

    更新日期:2007-01-01 00:00:00

  • Toward a design of affordable, topical microbicides: acylcarnitine analogues.

    abstract::Most heterosexual women want to reduce the risk of acquiring a sexually transmitted infection; many also want to control their fertility. Several chemical agents have been proposed to dramatically slow the spread of HIV infections. Ideally, vaginal microbicides, with or without contraceptive properties, should be safe...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161205774580705

    authors: Gandour RD

    更新日期:2005-01-01 00:00:00

  • Supraventricular tachycardia in infants: epidemiology and clinical management.

    abstract::Supraventricular tachycardias (SVTs) are observed in 0,1-0,4% of the paediatric population and represent an important clinical problem with related significant health and social issues. Most tachycardias are paroxysmal, being associated with sudden onset and termination, and only a relatively small number of them is p...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/138161208784007761

    authors: Calabrò MP,Cerrito M,Luzza F,Oreto G

    更新日期:2008-01-01 00:00:00

  • Endothelial Progenitor Cells as a Therapeutic Approach for Intracerebral Hemorrhage.

    abstract:BACKGROUND:Intracerebral hemorrhage (ICH) is the most lethal subtype of stroke, a leading cause of death and disability in developed countries. Therapeutic options are notably limited. There is no specific pharmacological treatment, and early surgery has few indications that represent only a small clinically relevant s...

    journal_title:Current pharmaceutical design

    pub_type: 杂志文章,评审

    doi:10.2174/1381612822666161221153937

    authors: Pías-Peleteiro J,Campos F,Perez-Mato M,Lopez-Arias E,Rodriguez-Yanez M,Castillo J,Sobrino T

    更新日期:2017-01-01 00:00:00