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Osmotic delivery systems

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https://www.readbyqxmd.com/read/29780259/delivery-of-bevacizumab-by-intracranial-injection-assessment-in-glioma-model
#1
Yu-Xiao Liu, Wen-Jia Liu, Hui-Ru Zhang, Zhi-Wen Zhang
Background: Many reports have indicated that the intravenous administration of bevacizumab produces a number of systemic side effects. Therefore, we investigated the therapeutic effects of intratumoral bevacizumab administration using a glioma animal model. Methods: The glioma cell lines U251 and U87 that carried luciferase were implanted into the brains of mice to develop glioma models. Glioma-bearing mice were treated with bevacizumab intravenously or intratumorally by Alzet micro-osmotic pumps, and the survival time of mice was monitored...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29778822/formulation-techniques-for-high-dose-dry-powders
#2
Ashlee D Brunaugh, Hugh D C Smyth
Delivery of drugs to the lungs via dry powder inhaler (DPI) is a promising approach for the treatment of both local pulmonary conditions and systemic diseases. Though DPIs are widely used for the pulmonary deposition of potent bronchodilators, anticholinergics, and corticosteroids, there is growing interest in the utilization of this delivery system for the administration of high drug doses to the lungs, as made evident by recent regulatory approvals for anti-microbial, anti-viral and osmotic agents. However, the formulation of high dose DPIs carries several challenges from both a physiological and physicochemical standpoint...
May 17, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29740759/characterization-and-in-vitro-permeation-study-of-cubic-liquid-crystal-containing-sinomenine-hydrochloride
#3
Xiaoqin Chu, Qian Li, Shuangying Gui, Zhengguang Li, Jiaojiao Cao, Jianqin Jiang
This study developed a new transdermal delivery system for the improved delivery of sinomenine hydrochloride (SH). The delivery system utilized the advantages of lyotropic liquid crystals (LLC) creating an adaptable system that offers a variety of options for the field of transdermal delivery. The formulation was prepared, characterized, and evaluated for its skin penetration in vitro. In the study, the appearance of samples was characterized by visual observation, and these LLC gels were colorless and transparent...
May 8, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29659246/membrane-nanotubes-increase-the-robustness-of-giant-vesicles
#4
Tripta Bhatia, Jaime Agudo-Canalejo, Rumiana Dimova, Reinhard Lipowsky
Giant unilamellar vesicles (GUVs) provide a direct connection between the nano- and the microregime. On the one hand, these vesicles represent biomimetic compartments with linear dimensions of many micrometers. On the other hand, the vesicle walls are provided by single molecular bilayers that have a thickness of a few nanometers and respond sensitively to molecular interactions with small solutes, biopolymers, and nanoparticles. These nanoscopic responses are amplified by the GUVs and can then be studied on much larger scales...
April 16, 2018: ACS Nano
https://www.readbyqxmd.com/read/29596011/slow-infusion-of-recombinant-adeno-associated-viruses-into-the-mouse-cerebrospinal-fluid-space
#5
Dan Wang, Jia Li, Karen Tran, Daniel R Burt, Li Zhong, Guangping Gao
Recombinant adeno-associated viruses (rAAVs) are the leading in vivo gene delivery platform, and have been extensively studied in gene therapy targeting various tissues, including the central nervous system (CNS). A single-bolus rAAV injection to the cerebrospinal fluid (CSF) space has been widely used to target the CNS, but it suffers from several drawbacks, such as leakage to peripheral tissues. Here, a protocol is described using an osmotic pump to infuse rAAV slowly into the mouse CSF space. Compared to the single-bolus injection technique, pump infusion can lead to higher CNS transduction and lower transduction in the peripheral tissues...
March 29, 2018: Human Gene Therapy Methods
https://www.readbyqxmd.com/read/29572254/parp1-targeted-radiotherapy-in-mouse-models-of-glioblastoma
#6
Stephen A Jannetti, Giuseppe Carlucci, Brandon Carney, Susanne Kossatz, Larissa Shenker, Lukas M Carter, Beatriz Salinas, Christian Brand, Ahmad Sadique, Patrick L Donabedian, Kristen M Cunanan, Mithat Gönen, Vladimir Ponomarev, Brian M Zeglis, Mark M Souweidane, Jason S Lewis, Wolfgang A Weber, John L Humm, Thomas Reiner
The DNA repair enzyme PARP1 is over-expressed in glioblastoma, with overall low expression in healthy brain tissue. Paired with the availability of specific molecularly targeted small molecules for this biomarker, PARP1 is a near-ideal target for novel radiotherapeutics. A successful PARP1-targeted radiotherapeutic would induce DNA damage and apoptosis in cancer cells, while sparing healthy brain tissue. We synthesized a131 I-labeled poly(ADP-ribose) polymerase 1 (PARP1) therapeutic and investigated its pharmacology using in vitro and in vivo methodologies...
March 23, 2018: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29505831/continuous-manganese-delivery-via-osmotic-pumps-for-manganese-enhanced-mouse-mri-does-not-impair-spatial-learning-but-leads-to-skin-ulceration
#7
Dulcie A Vousden, Elizabeth Cox, Rylan Allemang-Grand, Christine Laliberté, Lily R Qiu, Zsuzsa Lindenmaier, Brian J Nieman, Jason P Lerch
Manganese-enhanced magnetic resonance imaging (MEMRI) is a widely used technique in rodent neuroimaging studies. Traditionally, Mn2+ is delivered to animals via a systemic injection; however, this can lead to toxic effects at high doses. Recent studies have shown that subcutaneously implanted mini-osmotic pumps can be used to continuously deliver manganese chloride (MnCl2 ), and that they produce satisfactory contrast while circumventing many of the toxic side effects. However, neither the time-course of signal enhancement nor the effect of continuous Mn2+ delivery on behaviour, particularly learning and memory, have been well-characterized...
June 2018: NeuroImage
https://www.readbyqxmd.com/read/29491204/morphological-control-of-microtubule-encapsulating-giant-vesicles-by-changing-hydrostatic-pressure
#8
Kingo Takiguchi, Masahito Hayashi, Yuki Kazayama, Taro Toyota, Yoshie Harada, Masayoshi Nishiyama
For the development of artificial cell-like machinery, liposomes encapsulating cytoskeletons have drawn much recent attention. However, there has been no report showing isothermally reversible morphological changes of liposomes containing cytoskeletons. We succeeded in reversibly changing the shape of cell-sized giant vesicles by controlling the polymerization/depolymerization state of cytoskeletal microtubules that were encapsulated in the vesicles using pressure changes. The result indicates that it is possible to manipulate artificial cell models composed of molecules such as lipids and proteins...
2018: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29441977/production-and-in-vitro-evaluation-of-a-lamotrigine-extended-release-tablet-based-on-a-controlled-porosity-osmotic-pump-system
#9
Cheng Ma, Zhengwei Huang, Yuanming Zhu, Xiaona Chen, Vikramjeet Singh, Ying Huang, Xin Pan, Chuanbin Wu
Osmotic pump delivery systems have made significant advances in the past decades for controlled drug release over a long period of time. Usually, osmotic pump products require sophisticated and expensive laser drill technology resulting in increase in production cost and decrease in production efficiency. In this study, a lamotrigine extended release tablet based on a controlled-porosity osmotic pump (CPOP) system was developed to circumvent laser drill technology in reference, Lamictal XR®. The tablet core was coated by a polymer blend of Acryl-EZE® and HPMC E5...
September 1, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29428471/efficacy-of-constant-long-term-delivery-of-ym-58483-for-the-treatment-of-rheumatoid-arthritis
#10
Maya Miyoshi, Shuang Liu, Asuka Morizane, Erika Takemasa, Yashuyuki Suzuki, Takeshi Kiyoi, Kazutaka Maeyama, Masaki Mogi
The aim of this study was to investigate the efficacy and safety of YM-58483, a small molecular antagonist of Ca2+ release-activated Ca2+ (CRAC) channels, for the treatment of rheumatoid arthritis (RA), in vivo and ex vivo. YM-58483 was continuously injected subcutaneously in a collagen-induced arthritis (CIA) mouS.E.M.odel using an implanted osmotic pump. The severity of CIA was evaluated using the following parameters: body weight, hind paw volume, clinical score, histological analysis, cytokine levels, Ca2+ influx, and specific IgG production...
April 5, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29421366/chronic-administration-of-morphine-using-mini-osmotic-pumps-affects-spatial-memory-in-the-male-rat
#11
Erika Brolin, Sofia Zelleroth, Anna Jonsson, Mathias Hallberg, Alfhild Grönbladh, Fred Nyberg
The use of opioid analgesics to treat non-cancer pain has increased over the years. Many chronic pain patients suffer from numerous adverse effects, such as reduced quality of life, development of dependence, and cognitive impairments. Cognitive processes are regulated by several systems, one of which involves growth hormone (GH) and its secondary mediator insulin-like growth factor-1 (IGF-1), but also glutamatergic transmission, including receptors such as the N-methyl-d-aspartate (NMDA)-receptor complex. In the laboratory, repeated injections are commonly used to establish animal models of long-term or chronic drug exposure...
April 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29340982/controlled-release-of-the-nimodipine-loaded-self-microemulsion-osmotic-pump-capsules-development-and-characterization
#12
Yaping Huang, Sisi Zhang, Huifen Shen, Jinqing Li, Chongkai Gao
The present study was intended to develop a controlled released osmotic pump capsule based on Nimodipine (NM)-loaded self-microemulsifying drug delivery systems (SMEDDSs) in order to improve the low oral bioavailability of NM. To optimize the NM-loaded SMEDDS composition, the experiments of NM solubility in different oils, the pseudo-ternary phase diagram experiments and the different drug loading experiments were conducted in the preliminary screening studies. Controlled release of NM required an osmotic pump capsule comprising a coated semi-permeable capsule shell, plasticizer, and pore-forming agent...
January 16, 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29276823/engineering-multifunctional-rnai-nanomedicine-to-concurrently-target-cancer-hallmarks-for-combinatorial-therapy
#13
Yanlan Liu, Xiaoyuan Ji, Winnie W L Tong, Diana Askhatova, Tingyuan Yang, Hongwei Cheng, Yuzhuo Wang, Jinjun Shi
Cancer hallmarks allow the complexity and heterogeneity of tumor biology to be better understood, leading to the discovery of various promising targets for cancer therapy. An amorphous iron oxide nanoparticle (NP)-based RNAi strategy is developed to co-target two cancer hallmarks. The NP technology can modulate the glycolysis pathway by silencing MCT4 to induce tumor cell acidosis, and concurrently exacerbate oxidative stress in tumor cells via the Fenton-like reaction. This strategy has the following features for systemic siRNA delivery: 1) siRNA encapsulation within NPs for improving systemic stability; 2) effective endosomal escape through osmotic pressure and/or endosomal membrane oxidation; 3) small size for enhancing tumor tissue penetration; and 4) triple functions (RNAi, Fenton-like reaction, and MRI) for combinatorial therapy and in vivo tracking...
February 5, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29175643/sustained-release-multiparticulates-for-oral-delivery-of-a-novel-peptidic-ghrelin-agonist-formulation-design-and-in-vitro-characterization
#14
Ken Howick, Ryan Alam, Barbara Chruscicka, Dalia Kandil, Dara Fitzpatrick, Aoife M Ryan, John F Cryan, Harriët Schellekens, Brendan T Griffin
There is an impetus to provide appropriate sustained release oral delivery vehicles to protect biofunctional peptide loads from gastric degradation in vivo. This study describes the generation of a high load capacity pellet formulation for sustained release of a freely water-soluble dairy-derived hydrolysate, FHI-2571. The activity of this novel peptidic ghrelin receptor agonist is reported using in vitro calcium mobilization assays. Conventional extrusion spheronization was then used to prepare peptide-loaded pellets which were subsequently coated with ethylcellulose (EC) film coats using a fluid bed coating system in bottom spray (Wurster) mode...
January 30, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29130753/in-vitro-and-in-vivo-evaluation-of-controlled-release-matrix-tablets-of-highly-water-soluble-drug-applying-different-mw-polyethylene-oxides-peo-as-retardants
#15
Haoyang Wen, Xue Li, Yuenan Li, Haiying Wang, Yanyan Wang, Tuanjie Wang, Weisan Pan, Xinggang Yang
The aim of the work presented is to prepare a controlled-release hydrophilic matrix tablet (CMT) controlling release of highly water-soluble drug applying pure combination of high- and low-Mw PEO as matrix materials, to avoid the lag time of drug release, and to overcome incomplete release in later stages. The influences of types and amounts of different Mw PEOs used, drug loading, pH of release medium and agitation rate on drug release were evaluated. The study of uptake and erosion of matrix was conducted and mechanism of improving drug release was discussed...
April 2018: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/29098644/melts-of-octaacetyl-sucrose-as-oral-modified-release-dosage-forms-for-delivery-of-poorly-soluble-compound-in-stable-amorphous-form
#16
Dorota Haznar-Garbacz, Ewa Kaminska, Daniel Zakowiecki, Marek Lachmann, Kamil Kaminski, Grzegorz Garbacz, Przemysław Dorożyński, Piotr Kulinowski
The presented work describes the formulation and characterization of modified release glassy solid dosage forms (GSDFs) containing an amorphous nifedipine, as a model BCS (Biopharmaceutical Classification System) class II drug. The GSDFs were prepared by melting nifedipine together with octaacetyl sucrose. Dissolution profiles, measured under standard and biorelevant conditions, were compared to those obtained from commercially available formulations containing nifedipine such as modified release (MR) tablets and osmotic release oral system (OROS)...
February 2018: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29089185/cannula-based-drug-delivery-to-the-guinea-pig-round-window-causes-a-lasting-hearing-loss-that-may-be-temporarily-mitigated-by-bdnf
#17
Phillip J P Sale, Aaron Uschakov, Tasfia Saief, David P Rowe, Carla J Abbott, Chi D Luu, Amy J Hampson, Stephen J O'Leary, David J Sly
Sustained local delivery of drugs to the inner ear may be required for future regenerative and protective strategies. The round window is surgically accessible and a promising delivery route. To be viable, a delivery system should not cause hearing loss. This study determined the effect on hearing of placing a drug-delivery microcatheter on to the round window, and delivering either artificial perilymph (AP) or brain-derived neurotrophic factor (BDNF) via this catheter with a mini-osmotic pump. Auditory brainstem responses (ABRs) were monitored for 4 months after surgery, while the AP or BDNF was administered for the first month...
December 2017: Hearing Research
https://www.readbyqxmd.com/read/29066778/structural-physicochemical-and-dynamic-features-conserved-within-the-aerolysin-pore-forming-toxin-family
#18
Nuria Cirauqui, Luciano A Abriata, F Gisou van der Goot, Matteo Dal Peraro
Aerolysin is the founding member of a major class of β-pore-forming toxins (β-PFTs) found throughout all kingdoms of life. PFTs are cytotoxic proteins produced as soluble monomers, which oligomerize at the membrane of target host cells forming pores that may lead to osmotic lysis and cell death. Besides their role in microbial infection, they have become interesting for their potential as biotechnological sensors and delivery systems. Using an approach that integrates bioinformatics with molecular modeling and simulation, we looked for conserved features across this large toxin family...
October 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29054822/determining-the-effects-of-pei-adsorption-on-the-permeability-of-1-2-dipalmitoylphosphatidylcholine-bis-monoacylglycero-phosphate-membranes-under-osmotic-stress
#19
Scott R Clark, Keel Yong Lee, Hoyoung Lee, Jawahar Khetan, Hyun Chang Kim, Yun Hwa Choi, Kwanwoo Shin, You-Yeon Won
Polycations are used for a number of biological applications, including antibiotics and gene therapy. One aspect of the use of polycation gene carriers such as polyethylenemine (PEI) in gene therapy that is not well understood is their ability to escape from the vesicles they are internalized in. Here, in an attempt to gain a better understanding of PEI interaction with endosomal lipids under osmotic stress, we performed investigations using monolayers and vesicles derived from a mixture of neutral and negative lipids (1,2-dipalmitoylphosphatidylcholine (DPPC) and bis(monoacylglycero)phosphate (BMP), respectively)...
January 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29023798/intrathecal-antibody-distribution-in-the-rat-brain-surface-diffusion-perivascular-transport-and-osmotic-enhancement-of-delivery
#20
Michelle E Pizzo, Daniel J Wolak, Niyanta N Kumar, Eric Brunette, Christina L Brunnquell, Melanie-Jane Hannocks, N Joan Abbott, M Elizabeth Meyerand, Lydia Sorokin, Danica B Stanimirovic, Robert G Thorne
KEY POINTS: It is unclear precisely how macromolecules (e.g. endogenous proteins and exogenous immunotherapeutics) access brain tissue from the cerebrospinal fluid (CSF). We show that transport at the brain-CSF interface involves a balance between Fickian diffusion in the extracellular spaces at the brain surface and convective transport in perivascular spaces of cerebral blood vessels. Intrathecally-infused antibodies exhibited size-dependent access to the perivascular spaces and tunica media basement membranes of leptomeningeal arteries...
February 1, 2018: Journal of Physiology
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