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Eman Abd-Elrasheed, Sara Nageeb El-Helaly, Manal M El-Ashmoony, Salwa Salah
Intranasal Zaleplon solid dispersion was formulated to enhance the solubility, bioavailability and deliver an effective therapy. Zaleplon belongs to Class II drugs, and undergoes extensive first-pass metabolism after oral absorption exhibiting 30% bioavailability. A 23full factorial design was chosen for the investigation of solid dispersion formulations. The effects of different variables include drug to carrier ratio (1:1 and 1:2), carrier type (polyethylene glycol 4000 and poloxamer 407), and preparation method (solvent evaporation and freeze drying) on different dissolution parameters were studied...
December 13, 2017: Drug Development and Industrial Pharmacy
Ioannis N Mavridis
The concept of stereotactically standard areas (SSAs) within human brain nuclei belongs to the knowledge of the modern field of stereotactic brain microanatomy. These are areas resisting the individual variability of the nuclear location in stereotactic space. This paper summarizes the current knowledge regarding SSAs. A mathematical formula of SSAs was recently invented, allowing for their robust, reproducible, and accurate application to laboratory studies and clinical practice. Thus, SSAs open new doors for the application of stereotactic microanatomy to highly accurate brain targeting, which is mainly useful for minimally invasive neurosurgical procedures, such as deep brain stimulation...
December 11, 2017: Brain Sciences
Rehab Abdelmonem, Mohamed El Nabarawi, Alshaimaa Attia
The aim of this study was to formulate granisetron hydrochloride (GH) spanlastic in mucoadhesive gels and lyophilized inserts for intranasal administration to improve GH bioavailability and brain targeting. Carpapol 934 and HPMC were incorporated in GH spanlastic in nasal gels (GHSpNGs). Gelatin and HPMC as matrix former, glycine as a collapse protecting and mannitol as an insert filler and sweeting agent were used to prepare GH spanlastic loaded in lyophilized inserts (GHSpNIs). The prepared GHSpNGs were characterized for pH measurement, drug content, rheology, and in vitro drug release...
November 2018: Drug Delivery
Asahi Tomitaka, Hamed Arami, Zaohua Huang, Andrea Raymond, Elizette Rodriguez, Yong Cai, Marcelo Febo, Yasushi Takemura, Madhavan Nair
Image-guided drug delivery is an emerging strategy in the field of nanomedicine. The addition of image guidance to a traditional drug delivery system is expected to achieve highly efficient treatment by tracking the drug carriers in the body and monitoring their effective accumulation in the targeted tissues. In this study, we developed multifunctional magneto-plasmonic liposomes (MPLs), a hybrid system combining liposomes and magneto-plasmonic nanoparticles for a triple-modality image-guided drug delivery...
December 6, 2017: Nanoscale
Patrícia C Pires, Adriana O Santos
The treatment of neurodegenerative and psychiatric disorders remains a challenge in medical research. Several strategies have been developed over the years, either to overcome the blood-brain barrier or to achieve a safer or faster brain delivery, one of them being intranasal (IN) administration. The possibility of direct nose-to-brain transport offers enhanced targeting and reduced systemic side effects. Nevertheless, labile, low soluble, low permeant and/or less potent drugs might need a formulation other than the common solutions or suspensions...
November 30, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
Jing Sun, Wenjie Xie, Xufeng Zhu, Mengmeng Xu, Jie Liu
Functionalized nanomaterials, which have been applied widely to inhibit amyloid-β protein (Aβ) aggregation, show an enormous potential in the field of prevention and treatment of Alzheimer's disease (AD). A significant body of data has demonstrated that the morphology and size of nanomaterials have remarkable effects on their biological behaviors. In this paper, we proposed and designed three kinds of brain-targeting sulfur nanoparticles (RVG@Met@SNPs) with novel morphologies (volute-like, tadpole-like and sphere-like), and investigated the effect of different RVG@Met@SNPs on the Aβ-Cu2+ complex aggregation and their corresponding neurotoxicity...
December 1, 2017: ACS Chemical Neuroscience
Viral Shah, Pratiksha Kochar
BACKGROUND: Cancer is one of the leading causes of morbidity and mortality worldwide. Brain cancer is identified as one of the most formidable forms of cancer due to several hurdles posed by the anatomy and physiology of the brain on the therapeutic strategies employed for treating brain cancer. Poor prognosis and high relapse rate further aggravate the situation leading to the high mortality rate in brain cancer. OBJECTIVE: The present review gives a brief insight on different aspects of brain cancer by elucidating its types, causative factors, associated symptoms, diagnostic techniques, treatment strategies and limitations of current treatment strategies...
November 29, 2017: Recent Patents on Anti-cancer Drug Discovery
Eman Abd-Elrasheed, Sara Nageeb El-Helaly, Manal M El-Ashmoony, Salwa Salah
BACKGROUND: Zaleplon is a pyrazolopyrimidin derivative hypnotic drug indicated for the short-term management of insomnia. Zaleplon belongs to Class II drugs, according to the biopharmaceutical classification system (BCS), showing poor solubility and high permeability. It undergoes extensive first-pass hepatic metabolism after oral absorption, with only 30% of Zaleplon being systemically available. It is available in tablet form which is unable to overcome the previous problems. OBJECTIVE: The aim of this study is to enhance solubility and bioavailability via utilizing nanotechnology in the formulation of intranasal Zaleplon nano-emulsion (ZP-NE) to bypass the barriers and deliver an effective therapy to the brain...
November 30, 2017: Current Drug Delivery
Eleni Samaridou, Maria José Alonso
Nose-to-brain (N-to-B) delivery offers to protein and peptide drugs the possibility to reach the brain in a non-invasive way. This article is a comprehensive review of the state-of-the-art of this emerging peptide delivery route, as well as of the challenges associated to it. Emphasis is given on the potential of nanosized drug delivery carriers to enhance the direct N-to-B transport of protein or peptide drugs. In particular, polymer- and lipid- based nanocarriers are comparatively analyzed in terms of the influence of their physicochemical characteristics and composition on their in vivo fate and efficacy...
November 4, 2017: Bioorganic & Medicinal Chemistry
Roberta Dal Magro, Barbara Albertini, Silvia Beretta, Roberta Rigolio, Elisabetta Donzelli, Alessia Chiorazzi, Maurizio Ricci, Paolo Blasi, Giulio Sancini
Many potential therapeutic compounds for brain diseases fail to reach their molecular targets due to the impermeability of the blood-brain barrier, limiting their clinical development. Nanotechnology-based approaches might improve compounds pharmacokinetics by enhancing binding to the cerebrovascular endothelium and translocation into the brain. Adsorption of apolipoprotein E4 onto polysorbate(®) 80-stabilized nanoparticles to produce a protein corona allows the specific targeting of cerebrovascular endothelium...
November 17, 2017: Nanomedicine: Nanotechnology, Biology, and Medicine
Adi Miriam Goldenberg, Anne Minert, Yelena Fishman, Gilly Wolf, Marshall Devor
The MPTA (mesopontine tegmental anesthesia area) is a key node in a network of axonal pathways that collectively engage the key components of general anesthesia: immobility and atonia, analgesia, amnesia and loss-of-consciousness. In this study we have applied double retrograde tracing to analyze MPTA connectivity, with a focus on axon collateralization. Prior tracer studies have shown that collectively, MPTA neurons send descending projections to spinal and medullary brain targets associated with atonia and analgesia as well as ascending projections to forebrain structures associated with amnesia and arousal...
November 11, 2017: Neuroscience
Linmei Pan, Jing Zhou, Feng Ju, Huaxu Zhu
Alpha-asarone is a bioactive component of Acorus tatarincuii Schott with low bioavailability, which is often used for treatments of various brain diseases in clinical setting. This study was to formulate biodegradable methoxy polyethylene glycol-polylactic acid (mPEG-PLA) nanoparticles (NPs) surface-modified by lactoferrin (Lf), for delivering α-asarone into the brain following intranasal administration. Alpha-asarone NPs were prepared by premix membrane emulsification. The relative parameters were optimized by a Box-Behnken experimental design...
November 13, 2017: Drug Delivery and Translational Research
Na Huang, Shuai Lu, Xiao-Ge Liu, Jie Zhu, Yu-Jiong Wang, Rui-Tian Liu
Alzheimer's disease (AD) is the most common form of dementia, characterized by the formation of extracellular senile plaques and neuronal loss caused by amyloid β (Aβ) aggregates in the brains of AD patients. Conventional strategies failed to treat AD in clinical trials, partly due to the poor solubility, low bioavailability and ineffectiveness of the tested drugs to cross the blood-brain barrier (BBB). Moreover, AD is a complex, multifactorial neurodegenerative disease; one-target strategies may be insufficient to prevent the processes of AD...
October 6, 2017: Oncotarget
Jessica M Kelly, Amanda L Gross, Douglas R Martin, Mark E Byrne
AIM: Polymersomes are created to deliver an enzyme-based therapy to the brain in lysosomal storage disease patients. MATERIALS & METHODS: Polymersomes are formed via the injection method using poly(ethylene glycol)-b-poly(lactic acid) (PEGPLA) and bound to apolipoprotein E, to create a brain-targeted delivery vehicle. RESULTS: Polymersomes have a smallest average diameter of 145 ± 21 nm and encapsulate β-galactosidase at 72.0 ± 12...
November 7, 2017: Nanomedicine
Xiao-Yu Liu, Dan Cui, Dongyang Li, Runsheng Jiao, Xiaoran Wang, Shuwei Jia, Dan Hou, Tong Li, Haitao Liu, Ping Wang, Yu-Feng Wang
Social functions of oxytocin (OT) have been explored extensively; however, relationship between the effect of intranasally applied OT (nasal OT) on the social preference (SP) and intracerebral actions of endogenous OT remains unclear. To resolve this question, we first observed effects of nasal OT on the SP of virgin young adult male rats toward unfamiliar virgin estrous female (EF) vs. virgin male rats. The results showed that the test male rats exhibited significantly more times and longer duration accessing the female than the male, which were acutely eliminated by nasal OT...
2017: Frontiers in Cellular Neuroscience
Ya-Jie Dai, Xiao-Lan Chen, Hong-Yan Tang, Xian-Yi Deng, Lang Xie
To evaluate the optimum administration routes of saikosaponin in the treatment of epilepsy by comparing the plasma pharmacokinetics and the brain pharmacokinetics after different administration routes of saikosaponin. After receiving saikosaponin in different administration routes, the mice were sacrificed to collect the blood and brain tissues. The acetonitrile and methanol (9∶1) were used to precipitate the plasma protein. The concentration of the SSa in mice plasma and brain was determined by UPLC-MS/MS, and the pharmacokinetic parameters, bioavailability, the brain targeting coefficient (Re) and the brain drug targeting index (DTI) were calculated with Kinetica software...
July 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Nasim Hashempour Alamdari, Mahmood Alaei-Beirami, Seyed Ataollah Sadat Shandiz, Hadi Hejazinia, Rahimeh Rasouli, Mostafa Saffari, Seyed Esmaeil Sadat Ebrahimi, Artin Assadi, Mehdi Shafiee Ardestani
Designing a unique theranostic biocompatible, biodegradable, and cost-effective agent which is easy to be synthesized as a biohybrid material was the aim of this study. In this matter, asparagine attached to anionic linear globular dendrimer G2 (as a biocompatible, biodegradable, and cost-effective agent which is negatively charged nanosized and water soluble polymer that outweighs other traditionally used dendrimers) and finally contrast agent (Gd(3+)) was loaded (which made complexes) in synthesized asparagine-dendrimer...
2017: Contrast Media & Molecular Imaging
Jin-Ping Du, Yan-Ting Liu, Yi-Jing Wu, Hong-Hua Wu, Yan-Tong Xu
The existing antidepressants demonstrated delayed onset of clinical effects, so fast-onset antidepressants are required. Essential oil of herbs showed potentials fast-onset antidepressant potential. First, its aromatic odor can directly activate olfactory nerves; its high lipophilicity causes a high blood-brain barrier penetration rate; and its high volatility is suitable for nasal-brain targeting and inhalation delivery. Therefore, essential oils can rapidly regulate brain functions by multiple ways, suggesting a fast-onset antidepressant potential...
May 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
B Sriramoju, P Neerati, R K Kanwar, J R Kanwar
No abstract text is available yet for this article.
November 2017: Biochimica et Biophysica Acta
Yi Zhao, Li Zhang, Yao Peng, Qiming Yue, Li Hai, Li Guo, Qiantao Wang, Yong Wu
Venlafaxine, a novel third generation antidepressant drug, has been described as a reference treatment for major depression in clinical, owing to its ability of inhibiting both noradrenalin and serotonin neuronal reuptake, and inhibiting dopamine reuptake slightly. However, its clinical application is hampered by a limited brain distribution. Glucosylation is an effective way to enhance the brain targeting ability of drugs, but the bidirectional transport of glucose transporter 1 (GLUT1 ) might decrease the concentrations of venlafaxine-glucose (V-G) in brain before the release of parent drug venlafaxine...
October 24, 2017: Chemical Biology & Drug Design
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