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Liposome BBB

Vieri Piazzini, Elisa Landucci, Giulia Graverini, Domenico E Pellegrini-Giampietro, Anna Rita Bilia, Maria Camilla Bergonzi
(1) Background: Andrographolide (AG) is a natural compound effective for the treatment of inflammation-mediated neurodegenerative disorders. The aim of this investigation was the preparation of liposomes to enhance the penetration into the brain of AG, by modifying the surface of the liposomes by adding Tween 80 (LPs-AG) alone or in combination with Didecyldimethylammonium bromide (DDAB) (CLPs-AG). (2) Methods: LPs-AG and CLPs-AG were physically and chemically characterized. The ability of liposomes to increase the permeability of AG was evaluated by artificial membranes (PAMPA) and hCMEC/D3 cells...
August 13, 2018: Pharmaceutics
Khwaja Salahuddin Siddiqi, Azamal Husen, Sayed Sartaj Sohrab, Mensur Osman Yassin
Nanomaterials (NMs) are receiving remarkable attention due to their unique properties and structure. They vary from atoms and molecules along with those of bulk materials. They can be engineered to act as drug delivery vehicles to cross blood-brain barriers (BBBs) and utilized with better efficacy and safety to deliver specific molecules into targeted cells as compared to conventional system for neurological disorders. Depending on their properties, various metal chelators, gold nanoparticles (NPs), micelles, quantum dots, polymeric NPs, liposomes, solid lipid NPs, microparticles, carbon nanotubes, and fullerenes have been utilized for various purposes including the improvement of drug delivery system, treatment response assessment, diagnosis at early stage, and management of neurological disorder by using neuro-engineering...
August 10, 2018: Nanoscale Research Letters
Tatiana N Pashirova, Irina V Zueva, Konstantin A Petrov, Svetlana S Lukashenko, Irek R Nizameev, Natalya V Kulik, Aleksandra D Voloshina, Laszlo Almasy, Marsil K Kadirov, Patrick Masson, Eliana B Souto, Lucia Ya Zakharova, Oleg G Sinyashin
New mixed cationic liposomes based on L-α-phosphatidylcholine and dihexadecylmethylhydroxyethylammonium bromide (DHDHAB) were designed to overcome the BBB crossing by using the intranasal route. Synthesis and self-assembly of DHDHAB were performed. A low critical association concentration (0.01 mM), good solubilization properties toward hydrophobic dye Orange OT and antimicrobial activity against gram-positive bacteria Staphylococcus aureus (MIC=7.8 μg mL-1 ) and Bacillus cereus (MIC=7.8 μg mL-1 ), low hemolytic activities against human red blood cells (less than 10%) were achieved...
July 24, 2018: Colloids and Surfaces. B, Biointerfaces
Sushant Lakkadwala, Jagdish Singh
Drug delivery to the brain has been a major challenge due to the presence of the blood brain barrier (BBB), which limits the uptake of most chemotherapeutics into brain. We developed a dual-functionalized liposomal delivery system, conjugating cell penetrating peptide penetratin to transferrin-liposomes (Tf-Pen-conjugated liposomes) to enhance the transport of an anticancer chemotherapeutic drug, 5-fluorouracil (5-FU), across the BBB into the tumor cells. The in vitro cellular uptake study showed that the dual-functionalized liposomes are capable of higher cellular uptake in glioblastoma (U87) and brain endothelial (bEnd...
July 25, 2018: Journal of Pharmaceutical Sciences
Jianlou Niu, Junjun Xie, Kaiwen Guo, Xiaomin Zhang, Feng Xia, Xinyu Zhao, Lintao Song, Deli Zhuge, Xiaokun Li, Yingzheng Zhao, Zhifeng Huang
Fibroblast growth factor-20 (FGF20) is a paracrine member of the FGF family that is preferentially expressed in the substantia nigra pars compacta (SNpc). Previous studies have demonstrated that FGF20 enhances the survival of dopaminergic neurons suggesting the potential use of FGF20 to treat Parkinson's disease (PD). However, the reduced solubility of the bacterial recombinant human FGF20 (rhFGF20) and the absence of efficient strategies to transport rhFGF20 across the blood-brain barrier (BBB) have halted its clinical application...
November 2018: Drug Delivery
Lorena F Fernandes, Gisele E Bruch, André R Massensini, Frédéric Frézard
The complexity of the central nervous system (CNS), its limited self-repairing capacity and the ineffective delivery of most CNS drugs to the brain contribute to the irreversible and progressive nature of many neurological diseases and also the severity of the outcome. Therefore, neurological disorders belong to the group of pathologies with the greatest need of new technologies for diagnostics and therapeutics. In this scenario, nanotechnology has emerged with innovative and promising biomaterials and tools...
2018: Frontiers in Neuroscience
Antonietta Arcella, Sara Palchetti, Luca Digiacomo, Daniela Pozzi, Anna Laura Capriotti, Luigi Frati, Maria Antonietta Oliva, Georgia Tsaouli, Rossella Rota, Isabella Screpanti, Morteza Mahmoudi, Giulio Caracciolo
Temozolomide (TMZ) is the current first-line chemotherapy for treatment of glioblastoma multiforme (GBM). However, similar to other brain therapeutic compounds, access of TMZ to brain tumors is impaired by the blood-brain barrier (BBB) leading to poor response for GBM patients. To overcome this major hurdle, we have synthesized a set of TMZ-encapsulating nanomedicines made of four cationic liposome (CL) formulations with systematic changes in lipid composition and physical-chemical properties. The targeting nature of this nanomedicine is provided by the recruitment of proteins, with natural targeting capacity, in the biomolecular corona (BC) layer that forms around CLs after exposure to human plasma (HP)...
July 31, 2018: ACS Chemical Neuroscience
Ana Tari Ashizawa, Jenny Holt, Kelsey Faust, Weier Liu, Anjana Tiwari, Nan Zhang, Tetsuo Ashizawa
Cerebellar Purkinje cells (PCs) show conspicuous damages in many ataxic disorders. Targeted delivery of short nucleic acids, such as antisense oligonucleotides, to PCs may be a potential treatment for ataxic disorders, especially spinocerebellar ataxias (SCAs), which are mostly caused by a gain of toxic function of the mutant RNA or protein. However, oligonucleotides do not cross the blood-brain barrier (BBB), necessitating direct delivery into the central nervous system (CNS) through intra-thecal, intra-cisternal, intra-cerebral ventricular, or stereotactic parenchymal administration...
July 9, 2018: Cerebellum
Hanmei Wei, Tuo Liu, Ning Jiang, Kang Zhou, Kangqiang Yang, Weimin Ning, Yang Yu
The blood-brain barrier (BBB) poses a challenge for the treatment of cerebrovascular diseases including cerebral ischemia-reperfusion injury, Parkinson's syndrome, and cerebral tumors. Nanotechnology has developed as a promising strategy for drug delivery applications to the brain, especially liposomes (Lps) that have shown an intrinsic ability to cross the BBB. Angiopep-2 (ANG), a ligand for low-density lipoprotein receptor-related protein-1 (LRP1), is a good prospect for use as a targeting ligand for brain delivery using Lps...
July 1, 2018: Journal of Biomedical Nanotechnology
Man Li, Kairong Shi, Xian Tang, Jiaojie Wei, Xingli Cun, Yang Long, Zhirong Zhang, Qin He
Cancer associated fibroblasts (CAFs) which shape the tumor microenvironment (TME) and the presence of blood brain barrier (BBB) remain great challenges in targeting breast cancer and its brain metastasis. Herein, we reported a strategy using PTX-loaded liposome co-modified with acid-cleavable folic acid (FA) and BBB transmigrating cell penetrating peptide dNP2 peptide (cFd-Lip/PTX) for enhanced delivery to orthotopic breast cancer and its brain metastasis. Compared with single ligand or non-cleavable Fd modified liposomes, cFd-Lip exhibited synergistic TME targeting and BBB transmigration...
August 2018: Nanomedicine: Nanotechnology, Biology, and Medicine
Man Ying, Songli Wang, Mingfei Zhang, Ruifeng Wang, Hangchang Zhu, Huitong Ruan, Danni Ran, Zhilan Chai, Xiaoyi Wang, Weiyue Lu
The clinical treatment of aggressive glioma has been a great challenge, mainly because of the complexity of the glioma microenvironment and the existence of the blood-brain tumor barrier (BBTB)/blood-brain barrier (BBB), which severely hampers the effective accumulation of most therapeutic agents in the glioma region. Additionally, vasculogenic mimicry (VM), angiogenesis, and glioma stem cells (GSC) in malignant glioma also lead to the failure of clinical therapy. To address the aforementioned issues, a whole-process glioma-targeted drug delivery strategy was proposed...
June 13, 2018: ACS Applied Materials & Interfaces
Nisi Zhang, Fei Yan, Xiaolong Liang, Manxiang Wu, Yuanyuan Shen, Min Chen, Yunxue Xu, Guangyang Zou, Peng Jiang, Caiyun Tang, Hairong Zheng, Zhifei Dai
Rationale: Treatment for Parkinson's disease (PD) is challenged by the presence of the blood-brain barrier (BBB) that significantly limits the effective drug concentration in a patient's brain for therapeutic response throughout various stages of PD. Curcumin holds the potential for α-synuclein clearance to treat PD; however, its applications are still limited due to its low bioavailability and poor permeability through the BBB in a free form. Methods: Herein, this paper fabricated curcumin-loaded polysorbate 80-modified cerasome (CPC) nanoparticles (NPs) with a mean diameter of ~110 nm for enhancing the localized curcumin delivery into the targeted brain nuclei via effective BBB opening in combination with ultrasound-targeted microbubble destruction (UTMD)...
2018: Theranostics
Tongcheng Dai, Kuan Jiang, Weiyue Lu
The blood-brain barrier (BBB) and the blood-brain tumor barrier (BBTB) prevent drug and nano-drug delivery systems from entering the brain. However, ligand-mediated nano-drug delivery systems have significantly enhanced the therapeutic treatment of glioma. In this study we investigated the mechanism especially the integrity of liposomes and lipid disks while traversing the BBB and BBTB both in vitro and in vivo . Fluorophores (DiO, DiI and DiD) were loaded into liposomes and lipid disks to form Förster resonance energy transfer (FRET) nano-drug delivery systems...
March 2018: Acta Pharmaceutica Sinica. B
Tianzhi Yang, Laine Ferrill, Leanne Gallant, Sarah McGillicuddy, Tatiana Fernandes, Nicole Schields, Shuhua Bai
Riluzole is currently one of two approved medications for the treatment of amyotrophic lateral sclerosis (ALS). However, brain disposition of riluzole, as a substrate of P-glycoprotein (P-gp), is limited by the efflux transporters at the blood-brain barrier (BBB). We propose to develop a liposomal co-delivery system that could effectively transport riluzole to brain cells by reducing efflux pumps with a P-gp inhibitor, verapamil. Riluzole and verapamil cocktail liposomes were prepared by lipid film hydration...
July 30, 2018: European Journal of Pharmaceutical Sciences
Diego B Borin, Nathana J Mezzomo, Rodrigo A Vaucher, Guilherme DO Carmo, Luiz C Rodrigues Junior, Fernando B Sulczewski, Claiton I Schwertz, Ricardo E Mendes, Adriani P Damiani, Vanessa M DE Andrade, Virgínia C Rech, Carina R Boeck
Creatine acts intracellularly as energy buffer and storage, demonstrating protective effects in animal models of neurodegenerative diseases. However, its permeability throught blood-brain barrier (BBB) is reduced. The aim of the present study was developing a carrier to facilitate the delivery of creatine to the central nervous system. Creatine nanoliposomes were produced, characterized and assayed in models of toxicity in vitro and in vivo. Particles showed negative zeta potential (-12,5 mV), polydispersity index 0...
April 23, 2018: Anais da Academia Brasileira de Ciências
Amy Lee Bredlau, Anjan Motamarry, Chao Chen, M A McCrackin, Kris Helke, Kent E Armeson, Katrina Bynum, Ann-Marie Broome, Dieter Haemmerich
Most drugs cannot penetrate the blood-brain barrier (BBB), greatly limiting the use of anti-cancer agents for brain cancer therapy. Temperature sensitive liposomes (TSL) are nanoparticles that rapidly release the contained drug in response to hyperthermia (>40 °C). Since hyperthermia also transiently opens the BBB, we hypothesized that localized hyperthermia can achieve drug delivery across the BBB when combined with TSL. TSL-encapsulated doxorubicin (TSL-Dox) was infused intravenously over 30 min at a dose of 0...
November 2018: Drug Delivery
Simona Mancini, Luca Nardo, Maria Gregori, Inês Ribeiro, Francesco Mantegazza, Cristina Delerue-Matos, Massimo Masserini, Clara Grosso
BACKGROUND: Multi-target drugs have gained significant recognition for the treatment of multifactorial diseases such as depression. Under a screening study of multi-potent medicinal plants with claimed antidepressant-like activity, the phenolic-rich Annona muricata aqueous extract (AE) emerged as a moderate monoamine oxidase A (hMAO-A) inhibitor and a strong hydrogen peroxide (H2 O2 ) scavenger. PURPOSE: In order to protect this extract from gastrointestinal biotransformation and to improve its permeability across the blood-brain barrier (BBB), four phospholipid nanoformulations of liposomes and phytosomes functionalized with a peptide ligand promoting BBB crossing were produced...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Mengke Qu, Qing Lin, Shanshan He, Luyao Wang, Yao Fu, Zhirong Zhang, Ling Zhang
Parkinson's disease (PD) remains one of the most common neurodegenerative movement disorders with limited treatment options available. A dopamine derivative N-3,4-bis(pivaloyloxy)-dopamine (BPD) previously developed in our group has demonstrated superior therapeutic outcome compared to levodopa in a PD mice model. To further improve the therapeutic performance of BPD, a brain targeted drug delivery system was designed using a 29 amino-acid peptide (RVG29) derived from rabies virus glycoprotein as the targeting ligand...
May 10, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Muthupandian Saravanan, Tsehaye Asmalash, Atsebaha Gebrekidan, Dawit Gebreegziabiher, Tadele Araya, Haftamu Hilekiros, Hamed Barabadi, Kumaresan Ramanathan
BACKGROUND: Human Immuno deficiency Virus (HIV) infection has attained pandemic level due to its complexity on both the HIV infection cycle and on the targets for drug delivery. This limits medication and consequently requires prominent and promising drug delivery systems to be invented. Notably, various nanomaterial have been studied to enhance effective delivery of the antiretroviral drugs for HIV prevention, diagnosis and cure. Some of these nanomaterials are liposomes, dendrimers, inorganic nanoparticles (NPs), polymeric micelles, natural and synthetic polymers...
2018: Pharmaceutical Nanotechnology
Layton Lamsam, Eli Johnson, Ian D Connolly, Max Wintermark, Melanie Hayden Gephart
Magnetic resonance-guided focused ultrasound (MRgFUS) has been used extensively to ablate brain tissue in movement disorders, such as essential tremor. At a lower energy, MRgFUS can disrupt the blood-brain barrier (BBB) to allow passage of drugs. This focal disruption of the BBB can target systemic medications to specific portions of the brain, such as for brain tumors. Current methods to bypass the BBB are invasive, as the BBB is relatively impermeable to systemically delivered antineoplastic agents. Multiple healthy and brain tumor animal models have suggested that MRgFUS disrupts the BBB and focally increases the concentration of systemically delivered antitumor chemotherapy, immunotherapy, and gene therapy...
February 2018: Neurosurgical Focus
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