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https://www.readbyqxmd.com/read/28822195/-pharmacokinetics-of-%C3%AE-asarone-after-intranasal-and-intravenous-administration-with-pla-%C3%AE-asarone-nanoparticles
#1
Jin Lu, Li-Wei Guo, Ting-Ming Fu, Guo-Long Zhu, Zhen-Nan Dai, Guan-Jun Zhan, Li-Li Chen
PLA-α-asarone nanoparticles were prepared by using organic solvent evaporation method, and their in vivo distribution and brain targeting after intranasal administration were studied as compared with intravenous administration. The results showed that brain targeting coefficient of PLA-α-asarone nanoparticles after intranasal and intravenous administration was 1.65 and 1.16 respectively. The absolute bioavailability, brain-targeting efficiency and the percentage of nasal-brain delivery of PLA-α-asarone nanoparticles were 74...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28821618/region-specific-protein-misfolding-cyclic-amplification-reproduces-brain-tropism-of-prion-strains
#2
Nicolas Privat, Etienne Levavasseur, Serfildan Yildirim, Samia Hannaoui, Jean-Philippe Brandel, Jean-Louis Laplanche, Vincent Béringue, Danielle Seilhean, Stéphane Haïk
Human prion diseases such as Creutzfeldt-Jakob disease are transmissible brain proteinopathies, characterized by the accumulation of a misfolded isoform of the host cellular prion protein (PrP) in the brain. According to the prion model, prions are defined as proteinaceous infectious particles composed solely of this abnormal isoform of PrP (PrPSc). Even in the absence of genetic material, various prion strains can be propagated in experimental models. They can be distinguished by the pattern of disease they produce and especially by the localization of PrPSc deposits within the brain and the spongiform lesions they induce...
August 15, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28809432/intranasal-administration-of-brain-targeted-hp-%C3%AE-cd-chitosan-nanoparticles-for-delivery-of-scutellarin-a-compound-with-protective-effect-in-cerebral-ischaemia
#3
Shanshan Liu, Paul C Ho
OBJECTIVES: Scutellarin (SCU) is a traditional Chinese medicine used for the treatment of ischaemic cerebrovascular disease, but its clinic applications have been limited due to its poor water solubility, poor bioavailability and short half-life. In comparison with the conventional oral and intravenous administration, nasal administration may help targeting the drug more directly to brain. Thus, we proposed to employ a novel SCU-loaded HP-β-CD/chitosan nanoparticles (CD/CS-SCU-NPs) to deliver SCU to brain through the nasal route...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28805564/deep-brain-stimulation-and-nonmotor-symptoms
#4
Elliot Hogg, Jeffrey Wertheimer, Sarah Graner, Michele Tagliati
Deep brain stimulation (DBS) is currently the treatment of choice for advanced Parkinson's disease (PD). Several brain targets, including the subthalamic nucleus and the globus pallidus internus, have been successfully employed, with excellent motor outcomes. Despite less established knowledge, DBS may be a powerful tool for managing a wide variety of nonmotor symptoms (NMS) in PD patients, either directly or indirectly due to motor benefit or reduction of dopaminergic drug load. After an assessment of global nonmotor outcomes of DBS, as measured by currently available clinical scales and questionnaires, this chapter will address DBS effects on four main NMS categories: neurobehavioral, including cognitive and neuropsychiatric symptoms, autonomic dysfunction, including orthostatic hypotension, constipation, and urinary dysfunction, sleep disturbances, including insomnia, REM sleep behavior disorder, and restless leg syndrome, to conclude with sensory symptoms, mainly focusing on pain...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28797970/the-interaction-of-clozapine-loaded-nanocapsules-with-the-hcmec-d3-cells-in-vitro-model-of-blood-brain-barrier
#5
Sylwia Łukasiewicz, Ewa Błasiak, Krzysztof Szczepanowicz, Krzysztof Guzik, Małgorzata Bzowska, Piotr Warszyński, Marta Dziedzicka-Wasylewska
Despite progress in the development of novel pharmacological compounds, their efficacy in the treatment of neuropathologies is not satisfactory. One strategy to achieve safe and efficient brain targeting therapy is to design nanocarriers capable of transporting antipsychotic drugs through the BBB (without affecting the normal functions of the barrier) in a defined part of the brain. Here we investigate the interaction of clozapine-loaded polymeric Nano capsules (CLO-NCs) with hCMEC/D3 (human cerebral microvascular endothelial cells, D3 clone) cells that constitutes an in vitro model of the blood brain barrier (BBB)...
July 25, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28789524/glucuronidated-flavonoids-in-neurological-protection-structural-analysis-and-approaches-for-chemical-and-biological-synthesis
#6
Maite Docampo, Adiji Olubu, Xiaoqiang Wang, Giulio M Pasinetti, Richard Arthur Dixon
Both plant and mammalian cells express glucuronosyltransferases that catalyze glucuronidation of polyphenols such as flavonoids and other small molecules. Oral administration of select polyphenolic compounds leads to the accumulation of the corresponding glucuronidated metabolites at µM and sub-µM concentrations in the brain, associated with amelioration of a range of neurological symptoms. Determining the mechanisms whereby botanical extracts impact cognitive wellbeing and psychological resiliency will require investigation of the modes of action of the brain-targeted metabolites...
August 9, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28780138/insight-into-brain-targeted-drug-delivery-via-lat1-utilizing-prodrugs
#7
EDITORIAL
Kinam Park
No abstract text is available yet for this article.
September 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28771712/organization-of-alpha-transducin-immunoreactive-system-in-the-brain-and-retina-of-larval-and-young-adult-sea-lamprey-petromyzon-marinus-and-their-relationship-with-other-neural-systems
#8
Antón Barreiro-Iglesias, Blanca Fernández-López, Daniel Sobrido-Cameán, Ramón Anadón
We employed an anti-transducin antibody (Gαt-S), in combination with other markers, to characterize the Gαt-S-immunoreactive (ir) system in the CNS of the sea lamprey, Petromyzon marinus. Gαt-S immunoreactivity was observed in some neuronal populations and numerous fibers distributed throughout the brain. Double Gαt-S- and opsin-ir neurons (putative photoreceptors) are distributed in the hypothalamus (postoptic commissure nucleus, dorsal and ventral hypothalamus) and caudal diencephalon, confirming results of García-Fernández et al...
August 2, 2017: Journal of Comparative Neurology
https://www.readbyqxmd.com/read/28770390/genome-wide-significant-replicated-and-functional-risk-variants-for-alzheimer-s-disease
#9
Xiaoyun Guo, Wenying Qiu, Rolando Garcia-Milian, Xiandong Lin, Yong Zhang, Yuping Cao, Yunlong Tan, Zhiren Wang, Jing Shi, Jijun Wang, Dengtang Liu, Lisheng Song, Yifeng Xu, Xiaoping Wang, Na Liu, Tao Sun, Jianming Zheng, Justine Luo, Huihao Zhang, Jianying Xu, Longli Kang, Chao Ma, Kesheng Wang, Xingguang Luo
Genome-wide association studies (GWASs) have reported numerous associations between risk variants and Alzheimer's disease (AD). However, these associations do not necessarily indicate a causal relationship. If the risk variants can be demonstrated to be biologically functional, the possibility of a causal relationship would be increased. In this article, we reviewed all of the published GWASs to extract the genome-wide significant (p < 5×10(-8)) and replicated associations between risk variants and AD or AD-biomarkers...
August 2, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28769763/development-of-serotonergic-fibers-in-the-post-natal-mouse-brain
#10
Giacomo Maddaloni, Alice Bertero, Marta Pratelli, Noemi Barsotti, Annemarie Boonstra, Andrea Giorgi, Sara Migliarini, Massimo Pasqualetti
Serotonin (5-HT)-synthetizing neurons, which are confined in the raphe nuclei of the rhombencephalon, provide a pervasive innervation of the central nervous system (CNS) and are involved in the modulation of a plethora of functions in both developing and adult brain. Classical studies have described the post-natal development of serotonergic axons as a linear process of terminal field innervation. However, technical limitations have hampered a fine morphological characterization. With the advent of genetic mouse models, the possibility to label specific neuronal populations allowed the rigorous measurement of their axonal morphological features as well as their developmental dynamics...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28762846/biomimetic-synthesis-of-proline-derivative-templated-mesoporous-silica-for-increasing-the-brain-distribution-of-diazepam-and-improving-the-pharmacodynamics-of-nimesulide
#11
Heran Li, Jianxin Wang, Jialiang Cong, Chen Wei, Jing Li, Hongzhuo Liu, Sanming Li, Mingshi Yang
Herein a new kind of proline-derivative templated mesoporous silica with curved channels (CMS) was biomimetically synthesized and applied as carrier to improve the drug dissolution and bioavailability of hydrophobic diazepam (DZP) and nimesulide (NMS). Drugs can be incorporated into CMS with high efficiency; during this process, they successfully transformed to amorphous phase. As a result, the dissolution rate of DZP and NMS was significantly improved. Biodistribution study confirmed that CMS converted DZP distribution in mice with the tendency of lung targeting and brain targeting...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28759752/efavirenz-loaded-nanostructured-lipid-carrier-engineered-for-brain-targeting-through-intranasal-route-in-vivo-pharmacokinetic-and-toxicity-study
#12
Varsha Pokharkar, Arpana Patil-Gadhe, Prathyusha Palla
Intranasal delivery is a potential platform that can be employed in targeting the antiretrovirals (ARVs) to reach HIV that harbors in the central nervous system. The objective of the study was to develop an optimized efavirenz (EFV) loaded nanostructured lipid carrier (ENLC) and deliver it through intranasal route for brain targeting. Factorial design (2(3)) was used to identify the key formulation variables influencing particle size and percent drug encapsulation of efavirenz in the NLC. Optimised ENLC-6 batch exhibited a spherical morphology with a mean particle size of 162nm, high drug encapsulation of 95...
July 28, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28757483/association-of-blood-pressure-control-level-with-left-ventricular-morphology-and-function-and-with-subclinical-cerebrovascular-disease
#13
Koki Nakanishi, Zhezhen Jin, Shunichi Homma, Mitchell S V Elkind, Tatjana Rundek, Aylin Tugcu, Ralph L Sacco, Marco R Di Tullio
BACKGROUND: Left ventricular (LV) hypertrophy and subclinical cerebrovascular disease are early manifestations of cardiac and brain target organ damage caused by hypertension. This study aimed to investigate whether intensive office systolic blood pressure (SBP) control has beneficial effects on LV morphology and function and subclinical cerebrovascular disease in elderly patients with hypertension. METHODS AND RESULTS: We examined 420 patients treated for hypertension without history of heart failure and stroke from the CABL (Cardiovascular Abnormalities and Brain Lesions) study...
July 30, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28756656/targeting-fatty-acid-amide-hydrolase-with-prodrugs-for-cns-selective-therapy
#14
J Matthew Meinig, Skylar J Ferrara, Tania Banerji, Tapasree Banerji, Hannah S Sanford-Crane, Dennis Bourdette, Thomas S Scanlan
The blood-brain barrier (BBB) can be a substantial impediment to achieving therapeutic levels of drugs in the CNS. Certain chemical functionality such as the carboxylic acid is a general liability for BBB permeability preventing significant CNS distribution of a drug from a systemic dose. Here, we report a novel strategy for CNS-selective distribution of the carboxylic acid containing thyromimetic sobetirome using prodrugs targeted to fatty-acid amide hydrolase (FAAH), which is expressed in the brain. Two amide prodrugs of sobetirome were shown to be efficient substrates of FAAH with Vmax/KM values comparable to the natural endocannabinoid FAAH substrate anandamide...
July 30, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28754434/improved-method-for-cannula-fixation-for-long-term-intracerebral-brain-infusion
#15
Ádám Sike, Jonas Wengenroth, Jolanta Upīte, Thomas Brüning, Iván Eiriz, Petra Sántha, Henrik Biverstål, Baiba Jansone, Håvard Jostein Haugen, Markus Krohn, Jens Pahnke
BACKGROUND: Implanted osmotic minipumps are commonly used for long-term, brain-targeted delivery of a wide range of experimental agents by being connected to a catheter and a cannula. During the stereotactical surgery procedure, the cannula has to be placed correctly in the x-y directions and also with respect to the injection point in the z-direction (deepness). However, the flat fixation base of available cannula holders doesn't allow an easy, secure fixation onto the curve-shaped skull...
July 25, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/28748755/biotin-and-glutathione-targeting-of-solid-nanoparticles-to-cross-human-brain-endothelial-cells
#16
Szilvia Veszelka, Mária Mészáros, Lóránd Kiss, Zoltán Kóta, Tibor Páli, Zsófia Hoyk, Zsolt Bozsó, Lívia Fülöp, András Tóth, Gábor Rákhely, Mária A Deli
Background The blood-brain barrier restricts drug penetration to the central nervous system. Targeted nanocarriers are new potential tools to increase the brain entry of drugs. Ligands of endogenous transporters of the blood-brain barrier can be used as targeting vectors for brain delivery of nanoparticles. Objective We tested biotin-labeled solid nanoparticles for the first time and compared to biotinylated glutathione-labeled nanoparticles in brain endothelial cells. Method Neutravidin coated fluorescent polystyrene nanoparticles were derivatized with biotin and biotinylated glutathione...
July 27, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28745530/agomelatine-based-in-situ-gels-for-brain-targeting-via-the-nasal-route-statistical-optimization-in-vitro-and-in-vivo-evaluation
#17
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
Agomelatine (AGM) is an antidepressant drug with a low absolute bioavailability due to the hepatic first pass metabolism. AGM-loaded solid lipid nanoparticles were formulated in the form of an in situ gel to prolong the intranasal retention time and subsequently to increase the absorbed amount of AGM. The optimized in situ gel formula had a sol-gel transition temperature of 31 °C ± 1.40, mucociliary transport time of 27 min ±1.41%, released after 1 and 8 h of 46.3% ± 0.85 and 70.90% ± 1...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28733244/response-surface-optimization-ex-vivo-and-in-vivo-investigation-of-nasal-spanlastics-for-bioavailability-enhancement-and-brain-targeting-of-risperidone
#18
Fatma Elzahraa Abdelrahman, Ibrahim Elsayed, Mary Kamal Gad, Ahmed Hassen Elshafeey, Magdi Ibrahim Mohamed
Transnasal brain drug targeting could ensure better drug delivery to the brain through the olfactory pathway. Risperidone bioavailability is 66% in extensive metabolizers and 82% in slow metabolizers. The aim of this study is to investigate the ability of the nanovesicular spanlastics to effectively deliver risperidone through the nasal route to the brain and increase its bioavailability. Spanlastics formulae, composed of span and polyvinyl alcohol, were designed based on central composite statistical design...
July 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28731428/development-of-nasal-lipid-nanocarriers-containing-curcumin-for-brain-targeting
#19
Gustavo Richter Vaz, Gabriela Hädrich, Juliana Bidone, Jamile Lima Rodrigues, Mariana Corrêa Falkembach, Jean-Luc Putaux, Mariana Appel Hort, José Maria Monserrat, Antônio Sergio Varela Junior, Helder Ferreira Teixeira, Ana Luiza Muccillo-Baisch, Ana Paula Horn, Cristiana Lima Dora
BACKGROUND: Curcumin (CUR) has properties that can be useful for the treatment of Alzheimer's disease. Such properties are the inhibition of amyloid-β-protein (Aβ) aggregation, Aβ-induced inflammation, and activities of β-secretase and acetylcholinesterase. However, previous studies have revealed that CUR exhibited low bioavailability and difficulties in reaching the brain. OBJECTIVE: To overcome such drawbacks, this study aims at developing nasal lipid nanocarriers loaded with CUR to effectively target the brain...
2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28729175/brain-targeting-efficiency-of-antimigrain-drug-loaded-mucoadhesive-intranasal-nanoemulsion
#20
Ebtsam M Abdou, Soha M Kandil, Hala M F El Miniawy
Zolmitriptan (ZT) is a well-tolerated drug in migraine treatment suffering from low bioavailability due to low amount of the drug that reaches the brain after oral and nasal delivery. Development of new nasal mucoadhesive nanoemulsion formulation for zolmitriptan may success in delivering the drug directly from the nose to the brain to achieve rapid onset of action and high drug concentration in the brain which is required for treatment of acute migraine. ZT mucoadhesive nanoemulsion were prepared and characterized for drug content, zeta potential, particle size, morphology, residence time and permeation through the nasal mucosa...
July 17, 2017: International Journal of Pharmaceutics
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