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Xiao-Juan Wang, Yin-Ping Gao, Nan-Nan Lu, Wei-Shuo Li, Ji-Fang Xu, Xiao-Ying Ying, Gang Wu, Mei-Hua Liao, Chao Tan, Ling-Xiao Shao, Ying-Mei Lu, Chen Zhang, Kohji Fukunaga, Feng Han, Yong-Zhong Du
Clinical treatment for vascular dementia still remains a challenge mainly due to Blood-Brain Barrier (BBB). Here, a micelle based on polysialic acid (PSA) which is a hydrophilic and endogenous carbohydrate polymer, was designed to deliver calmodulin antagonist for therapy of vascular dementia. PSA was firstly chemically conjugated with octadecylamine (ODA), and the obtained PSA-ODA copolymer could self-assemble into micelle in aqueous solution with a 120.0 μg/mL critical micelle concentration. The calmodulin antagonist loaded PSA-ODA micelle, featuring sustained drug release behaviour over a period of 72 h with 3...
October 17, 2016: ACS Applied Materials & Interfaces
Vanessa S S Gonçalves, Ana A Matias, Joana Poejo, Ana T Serra, Catarina M M Duarte
During the development of intranasal drug delivery systems for local/systemic effect or brain targeting, it is necessary to assess its cytotoxicity and drug transport through nasal epithelium. In order to avoid animal experiments or the use of excised tissues, in vitro cell models, such as RPMI 2650 cells, are being preferred during recent years. Nevertheless, the deposition of solid formulations into nasal cell layers with further transepithelial transport rate of drugs has been poorly studied or reported...
October 1, 2016: International Journal of Pharmaceutics
Mohammad Yusuf, Maria Khan, Riaz A Khan, Ibrahim Abdullah Maghrabi, Bahar Ahmed
Depression is a modern world epidemic. Its main causative factor is oxidative stress, as reported in study subjects. Natural products are yet to show significant therapeutic effects in comparison with synthetic drugs. Current study deals with the preparation of brain-targeted polysorbate-80-coated curcumin PLGA nanoparticles (PS-80-CUR-NP), and their characterisation via Spectral and optical methods. PS-80-CUR-NP were evaluated against the oxidative stress-mediated depressant (OSMD) activity via Force despair, Tail suspension tests and stress biomarker assay (SOD and catalase activity)...
October 14, 2016: Journal of Microencapsulation
Tengfei Li, Matthias Vandesquille, Fani Koukouli, Clémence Dudeffant, Ihsen Youssef, Pascal Lenormand, Christelle Ganneau, Uwe Maskos, Christian Czech, Fiona Grueninger, Charles Duyckaerts, Marc Dhenain, Sylvie Bay, Benoît Delatour, Pierre Lafaye
Detection of intracerebral targets with imaging probes is challenging due to the non-permissive nature of blood-brain barrier (BBB). The present work describes two novel single-domain antibodies (VHHs or nanobodies) that specifically recognize extracellular amyloid deposits and intracellular tau neurofibrillary tangles, the two core lesions of Alzheimer's disease (AD). Following intravenous administration in transgenic mouse models of AD, in vivo real-time two-photon microscopy showed gradual extravasation of the VHHs across the BBB, diffusion in the parenchyma and labeling of amyloid deposits and neurofibrillary tangles...
October 5, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Anam Khan, Syed Sarim Imam, Mohammed Aqil, Abdul Ahad, Yasmin Sultana, Asgar Ali, Khalid Khan
The aim of the present work was to investigate the efficacy of temozolomide nanostructured lipid carriers (TMZ-NLCs) to enhance brain targeting via nasal route administration. The formulation was optimized by applying a four-factor, three-level Box-Behnken design. The developed formulations and the functional relationships between their independent and dependent variables were observed. The independent variables used in the formulation were gelucire (X1), liquid lipid/total lipid (X2), Tween 80 (X3), and sonication time (X4), and their effects were observed with regard to size (Y1), % drug release (Y2), and drug loading (Y3)...
October 3, 2016: Molecular Pharmaceutics
Samia A Nour, Nevine S Abdelmalak, Marianne J Naguib, Hassan M Rashed, Ahmed B Ibrahim
Clonazepam (CZ) is an anti-epileptic drug used mainly in status epilepticus (SE). The drug belongs to Class II according to BCS classification with very limited solubility and high permeability and it suffers from extensive first-pass metabolism. The aim of the present study was to develop CZ-loaded polymeric micelles (PM) for direct brain delivery allowing immediate control of SE. PM were prepared via thin film hydration (TFH) technique adopting a central composite face-centered design (CCFD). The seventeen developed formulae were evaluated in terms of entrapment efficiency (EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and in vitro release...
September 20, 2016: Drug Delivery
Zi-Zhao Yang, Li Li, Lu Wang, Ming-Cheng Xu, Sai An, Chen Jiang, Jing-Kai Gu, Zai-Jie Jim Wang, Lu-Shan Yu, Su Zeng
Regulating main brain-uptake transporter of morphine may restrict its tolerance generation, then modify its antinociception. In this study, more than 2 fold higher intracellular uptake concentrations for morphine and morphine-6-glucuronide (M6G) were observed in stable expression cells, HEK293-hOATP2B1 than HEK293-MOCK. Specifically, the Km value of morphine to OATP2B1 (57.58 ± 8.90 μM) is 1.4-time more than that of M6G (80.31 ± 21.75 μM); Cyclosporine A (CsA), an inhibitor of OATP2B1, can inhibit their intracellular accumulations with IC50 = 3...
2016: Scientific Reports
Gülsel Yurtdaş Kırımlıoğlu, Yusuf Menceloğlu, Kevser Erol, Yasemin Yazan
Objectives of this study were the delivery of gamma aminobutyric acid (GABA) into the brain by means of developing brain targeted, nanosized, nontoxic and biocompatible polymeric nanoparticles, and investigating their effectiveness in epilepsy. For this purpose, GABA conjugated N,N-dimethylacrylamide based pegylated nanoparticles were designed and characterized for particle size, zeta potential, pH, morphology, DSC, XRD, FTIR, GABA quantification and in vitro release. Formulations showed smaller particle size, cationic zeta potential characteristic, possible GABA polymeric matrix interaction and prolonged release pattern...
September 8, 2016: Journal of Microencapsulation
Ania Dabrowski, Hisashi Umemori
Brain development involves multiple levels of molecular coordination in forming a functional nervous system. The hippocampus is a brain area that is important for memory formation and spatial reasoning. During early postnatal development of the hippocampal circuit, Fibroblast growth factor 22 (FGF22) and FGF7 act to establish a balance of excitatory and inhibitory tone. Both FGFs are secreted from CA3 dendrites, acting on excitatory or inhibitory axon terminals formed onto CA3 dendrites, respectively. Mechanistically, FGF22 utilizes FGFR2b and FGFR1b to induce synaptic vesicle recruitment within axons of dentate granule cells (DGCs), and FGF7 utilizes FGFR2b to induce synaptic vesicle recruitment within interneuron axons...
2016: Neurogenesis (Austin, Tex.)
Aron Tendler, Noam Barnea Ygael, Yiftach Roth, Abraham Zangen
Deep transcranial magnetic stimulation (dTMS) utilizes different H-coils to study and treat a variety of psychiatric and neurological conditions with identifiable brain targets. The availability of this technology is dramatically changing the practice of psychiatry and neurology as it provides a safe and effective way to treat even drug-resistant patients. However, up until now, no effort was made to summarize the different types of H-coils that are available, and the conditions for which they were tested. Areas covered: Here we assembled all peer reviewed publication that used one of the H-coils, together with illustrations of the effective field they generate within the brain...
October 2016: Expert Review of Medical Devices
Julia Fedotova, Vagif Soultanov, Tamara Nikitina, Victor Roschin, Natalia Ordyan, Lucian Hritcu
Previous studies indicated that reduced androgen levels may contribute to both physical and cognitive disorders in men, including Alzheimer's disease. New drug candidates for Alzheimer's disease in patients with androgen deficiency should ideally be able to act not only on multiple brain targets but also to correct impaired endocrine functions in hypogonadal men with Alzheimer's disease. Ropren(®) is one such candidate for the treatment of Alzheimer's disease in men with an imbalance of androgens. Accordingly, the aim of the current study was to examine the effects of long-term Ropren(®) administration (8...
September 3, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Reema Narayan, Mohan Singh, OmPrakash Ranjan, Yogendra Nayak, Sanjay Garg, Gopal V Shavi, Usha Y Nayak
The present paper is aimed at development of functionalized risperidone liposomes for brain targeting through nasal route for effective therapeutic management of schizophrenia. The risperidone liposomes were prepared by thin film hydration method. Various parameters such as lipid ratio and lipid to drug ratio were optimized by using Design-Expert(®) Software to obtain high entrapment with minimum vesicle size. The surface of the optimized liposomes was modified by coating stearylamine and MPEG-DSPE for enhanced penetration to the brain...
October 15, 2016: Life Sciences
Luisa Fiandra, Serena Mazzucchelli, Marta Truffi, Michela Bellini, Luca Sorrentino, Fabio Corsi
Brain microvascular endothelial cells, supported by pericytes and astrocytes endfeet, are responsible for the low permeation of large hydrosoluble drugs through the blood-brain barrier (BBB), causing difficulties for effective pharmacological therapies. In recent years, different strategies for promoting brain targeting have aimed to improve drug delivery and activity at this site, including innovative nanosystems for drug delivery across the BBB. In this context, an in vitro approach based on a simplified cellular model of the BBB provides a useful tool to investigate the effect of nanoformulations on the trans-BBB permeation of molecules...
2016: Journal of Visualized Experiments: JoVE
Yali Xu, Hai Cui, Qiong Zhu, Xing Hua, Hongmei Xia, Kaibin Tan, Yunhua Gao, Jing Zhao, Zheng Liu
Objective. Blood-brain barrier (BBB) is a key obstacle that prevents the medication from blood to the brain. Microbubble-enhanced cavitation by focused ultrasound can open the BBB and proves to be valuable in the brain drug delivery. The study aimed to explore the feasibility, efficacy, and safety of unilateral opening of BBB using diagnostic ultrasound targeted microbubbles destruction in rats. Methods. A transtemporal bone irradiation of diagnostic ultrasound and intravenous injection of lipid-coated microbubbles were performed at unilateral hemisphere...
2016: BioMed Research International
Nargess Gandomi, Reyhaneh Varshochian, Fatemeh Atyabi, Mohammad Hossein Ghahremani, Mohammad Sharifzadeh, Mohsen Amini, Rassoul Dinarvand
Multiple sclerosis (MS) is a chronic central nervous system (CNS) inflammation. Efficient drug delivery to brain is however hampered by blood brain barrier (BBB). In order to have highly efficient and safe delivery of drugs to brain, solid lipid nanoparticles (SLNs) have indicated promising potentials as smart carriers that can pass the blood brain barrier and deliver therapeutic biomolecules to the brain. In this study pegylated SLNs surface modified with using anti-Contactin2 or anti-Neurofascin, two axo-glial-glycoprotein antigens located in node of Ranvier, were prepared...
August 30, 2016: Pharmaceutical Development and Technology
Jifu Hao, Jing Zhao, Shupeng Zhang, Tiantian Tong, Qiannan Zhuang, Kai Jin, Wei Chen, Hua Tang
The objective of this study was to fabricate a composite in situ gelling formulation combining nanoparticulates and an ionic-triggered deacetylated gellan gum (DGG) matrix for challenging intranasal drug delivery. The prepared resveratrol nanosuspensions (Res-NSs) were distributed in DGG solutions. Parameters such as the in situ gelation capability, particle size, rheological properties, and texture profiles were used to describe the properties of the in situ gel. Pharmacokinetic and brain-targeting efficiency studies were performed after intranasal and intravenous administration, respectively...
November 1, 2016: Colloids and Surfaces. B, Biointerfaces
Snigdha Dagar, Shubhajit Roy Chowdhury, Raju Surampudi Bapi, Anirban Dutta, Dipanjan Roy
Stroke is the leading cause of severe chronic disability and the second cause of death worldwide with 15 million new cases and 50 million stroke survivors. The poststroke chronic disability may be ameliorated with early neuro rehabilitation where non-invasive brain stimulation (NIBS) techniques can be used as an adjuvant treatment to hasten the effects. However, the heterogeneity in the lesioned brain will require individualized NIBS intervention where innovative neuroimaging technologies of portable electroencephalography (EEG) and functional-near-infrared spectroscopy (fNIRS) can be leveraged for Brain State Dependent Electrotherapy (BSDE)...
2016: Frontiers in Neurology
Yuan Sun, Chen Kang, Fei Liu, Lei Song
Preclinical Research Psychosis remains one of the most challenging health problems for society, affecting hundreds of millions of people worldwide. Although current antipsychotics can alleviate the symptoms of psychosis, they are still far away from being perfect, often causing significant and even fatal side effects such as involuntary movement disorders and metabolic syndrome. With the lack of precise knowledge of the underlying mechanisms of psychosis, a rational approach to improve the efficiency of current antipsychotics is by nanoparticle-based administration...
August 22, 2016: Drug Development Research
Tingting Jia, Zhiguo Sun, Ying Lu, Jie Gao, Hao Zou, Fangyuan Xie, Guoqing Zhang, Hao Xu, Duxin Sun, Yuan Yu, Yanqiang Zhong
Due to the impermeability of the blood-brain barrier and the nonselective distribution of drugs in the brain, the therapeutic access to intractable neurological disorders is challenging. In this study, dual brain-targeting polymersomes (POs) functionalized by transferrin and Tet-1 peptide (Tf/Tet-1-POs) promoted the transportation of curcumin into the brain and provided neuroprotection. The modification of the ligands that bind to the surface of POs was revealed by X-ray photoelectron spectroscopy analysis...
2016: International Journal of Nanomedicine
Aruna Sharma, Preeti Menon, Dafin F Muresanu, Asya Ozkizilcik, Z Ryan Tian, José V Lafuente, Hari Sharma
The BBB is a physiological regulator of transport of essential items from blood to brain for the maintenance of homeostasis of the central nervous system (CNS) within the narrow limit. The BBB is also responsible for export of harmful or metabolic products from brain to blood to keep the fluid microenvironment of the CNS healthy. However, following any noxious insult to the brain caused by trauma, ischemia or environmental/chemical toxins the function of the BBB is altered to small as well as to large molecules e...
August 19, 2016: CNS & Neurological Disorders Drug Targets
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