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Osmotic delivery systems

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...
March 2, 2018: NeuroImage
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
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
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...
February 8, 2018: European Journal of Pharmacology
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...
February 5, 2018: Pharmacology, Biochemistry, and Behavior
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
Yanlan Liu, Xiaoyuan Ji, Winnie Tong, Diana Askhatova, Tingyuan Yang, Hongwei Cheng, Yuzhuo Wang, Jinjun Shi
Cancer hallmarks have been providing a logical framework for understanding the complexity and heterogeneity of tumor biology, leading to the discovery of various promising targets for cancer therapy. Herein, we report a novel amorphous iron oxide nanoparticle (NP)-based RNAi strategy 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...
December 24, 2017: Angewandte Chemie
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
Haoyang Wen, Xue Li, Yuenan Li, Haiying Wang, Wang Yanyan, Wang Tuanjie, 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...
November 13, 2017: Drug Development and Industrial Pharmacy
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)...
November 2, 2017: AAPS PharmSciTech
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
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
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
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
The precise mechanisms governing the central distribution of macromolecules from the cerebrospinal fluid (CSF) to the brain and spinal cord remain poorly understood, despite their importance for physiological processes such as antibody trafficking for central immune surveillance as well as several ongoing intrathecal clinical trials. Here, we clarify how immunoglobulin G (IgG) and smaller single-domain antibodies (sdAb) distribute throughout the whole brain in a size-dependent manner after intrathecal infusion in rats using ex vivo fluorescence and in vivo 3D magnetic resonance imaging...
October 12, 2017: Journal of Physiology
Qingliang Yang, Yingliang Ma, Jesse Zhu
Dry powder coated osmotic drug delivery system (ODDS) were prepared and characterized using an innovative powder coating technology. Coating powder adhesion to the surface of the ODDS core was firstly performed through an electrostatic spray gun, followed by a curing step to allow those electrically deposited particles coalesce and form a continuous, uniform and strong coating film, which is the semipermeable membrane of the ODDS. Triethyl citrate (TEC) was found to be a better liquid plasticizer than PEG 400 both in reducing the glass transition temperature of the coating polymer (cellulose acetate) and in increasing the electrical conductivity of the ODDS cores, both of which led to an enhanced coating powder adhesion and film formation...
October 3, 2017: European Journal of Pharmaceutical Sciences
Mahsa Narenji, Mohammad Reza Talaee, Hamid Reza Moghimi
Liposomes are used widely as drug delivery systems in different forms including nanosuspensions, osmotic pumps, infusion pumps, and IV injections. Some of these systems (e.g. infusion or osmotic pumps) might stay stagnant for a long time during or before administration, and therefore, might face phase separation. In spite of these, there are no data available about the behavior of liposomal systems upon stagnation in such drug delivery systems. As a part of a series of investigations on convective flow and stagnation of liposomes, the current work represents the effects of charge on liposomes separation upon stagnation...
2017: Iranian Journal of Pharmaceutical Research: IJPR
Jukka Pajarinen, Akira Nabeshima, Tzu-Hua Lin, Taishi Sato, Emmanuel Gibon, Eemeli Jämsen, Laura Lu, Karthik Nathan, Zhenyu Yao, Stuart B Goodman
Periprosthetic osteolysis and subsequent aseptic loosening of total joint replacements are driven by byproducts of wear released from the implant. Wear particles cause macrophage mediated inflammation that culminates with periprosthetic bone loss. Most current animal models of particle- induced osteolysis are based on the acute inflammatory reaction induced by wear debris, which is distinct from the slowly progressive clinical scenario. To address this limitation we previously developed a murine model of periprosthetic osteolysis that is based on slow continuous delivery of wear particles into the murine distal femur over a period of 4 weeks...
October 5, 2017: Tissue Engineering. Part C, Methods
Lili Du, Junhui Zhou, Lingwei Meng, Xiaoxia Wang, Changrong Wang, Yuanyu Huang, Shuquan Zheng, Liandong Deng, Huiqing Cao, Zicai Liang, Anjie Dong, Qiang Cheng
Small interfering RNA (siRNA) therapies have been hampered by lack of delivery systems in the past decades. Nowadays, a few promising vehicles for siRNA delivery have been developed and it is gradually revealed that enhancing siRNA release from endosomes into cytosol is a very important factor for successful delivery. Here, we designed a novel pH-sensitive nanomicelle, PEG-PTTMA-P(GMA-S-DMA) (PTMS), for siRNA delivery. Owing to rapid hydrolysis in acidic environment, PTMS NPs underwent hydrophobic-to-hydrophilic transition in endosomes that enabled combination of proton sponge effect and raised osmotic pressure in endosomes, resulting in vigorous release of siRNAs from endosomes into cytosol...
2017: Theranostics
Aditya Pareek, Shantanu Maheshwari, Sivakumar Cherlo, Rama Subba Reddy Thavva, Venkataramana Runkana
There is a rising interest in stimuli-responsive hydrogels to achieve controlled and self-regulated drug delivery. Stimuli responsive polymer hydrogels with their ability to swell/de-swell under varying pH conditions present themselves as a potential candidate for controlled drug delivery. It is important to develop a mechanistic understanding of the underlying phenomena that will help suggest ways to control the drug release from a polymer hydrogel. We present a mathematical model that couples Nernst-Planck, Poisson and force balance equations to incorporate diffusion of ionic species and drug along with deformation of hydrogel under osmotic pressure...
October 30, 2017: International Journal of Pharmaceutics
Virginia D McLane, Ivy Bergquist, James Cormier, Deborah J Barlow, Karen L Houseknecht, Edward J Bilsky, Ling Cao
AIMS: Slow-release morphine sulfate pellets and osmotic pumps are common routes of chronic morphine delivery in mouse models, but direct comparisons of these drug delivery systems are lacking. In this study, we assessed the efficacy of slow-release pellets versus osmotic pumps in delivering morphine to adult mice. MAIN METHODS: Male C57BL/6NCr mice (8weeksold) were implanted subcutaneously with slow-release pellets (25mg morphine sulfate) or osmotic pumps (64mg/mL, 1...
September 15, 2017: Life Sciences
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