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https://www.readbyqxmd.com/read/28719859/-curcumin-loaded-poly-d-l-lactide-co-glycolide-nanovesicles-induce-antinociceptive-effects-and-reduce-pronociceptive-cytokine-and-bdnf-release-in-spinal-cord-after-acute-administration-in-mice
#1
Stefano Pieretti, Amalendu P Ranjan, Amalia Di Giannuario, Anindita Mukerjee, Francesca Marzoli, Rita Di Giovannandrea, Jamboor K Vishwanatha
Given the poor bioavailability of curcumin, its antinociceptive effects are produced after chronic intravenous administration of high doses, while poly (d,l-lactide-co-glycolide)-loaded vesicles (PLGA) can improve drug delivery. This paper investigates the antinociceptive effects of curcumin-loaded PLGA nanovesicles (PLGA-CUR) administered via intravenous (i.v.) or intrathecal (i.t.) routes at low and high doses. The following models of pain were used: formalin test, zymosan-induced hyperalgesia and sciatic nerve ligation inducing neuropathic allodynia and hyperalgesia...
July 10, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28719857/in-situ-adjuvant-therapy-using-a-responsive-doxorubicin-loaded-fibrous-scaffold-after-tumor-resection
#2
Ziming Yuan, Wei Wu, Zhongwei Zhang, Zhiyong Sun, Ruoyu Cheng, Guoqin Pan, Xuemin Wang, Wenguo Cui
As tumor microenvironment becoming more and more important in tumor study, the acid pH around or in solid tumors drew lots of attentions. And the progress of drug delivery systems made the responsive-release possible. This time, we fabricated a new-type composite electrospun poly (L-lactide) (PLLA) fibrous scaffolds, that blent with the mesoporous silica particles (MSNs). Further more, we used sodium bicarbonate (SB) as acid sensitive agent which was wrapped inside the MSNs. And doxorubicin (DOX) was also wrapped into MSNs in order to achieve a sustained release to inhibit tumors in mice, which mimicked the remnant breast cancer with surgery...
July 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28719744/high-resolution-insights-into-the-stepwise-self-assembly-of-nanofiber-from-bioactive-peptides
#3
Fude Sun, Long Chen, Xiufang Ding, Lida Xu, Xirui Zhou, Peng Wei, Jun-Feng Liang, Shi-Zhong Luo
Peptide self-assembly has a profound biological significance since self-assembled bioactive peptides are gifted with improved bioactivity as well as life-span. In this study, peptide self-assembly was investigated using a therapeutic peptide, PTP-7S (EENFLGALFKALSKLL). Combining experiments of atomic force microscopy (AFM), circular dichroism (CD) and 8-anilino-1-naphthalenesulfonic acid (ANS) fluorescence spectra, PTP-7S showing α-helix was found self-assembling into nanofibers in solution. Relying on the coarse-grained (CG) dynamic simulations, the self-assembling of PTP-7S was revealed as a stepwise process that peptide monomers first clustered into peptide-assembling units (PUs) with charged surface, and then the PUs integrated together to construct nano-fibril aggregates...
July 18, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28719635/differential-protein-expression-profile-in-the-hypothalamic-gt1-7-cell-line-after-exposure-to-anabolic-androgenic-steroids
#4
Freddyson J Martínez-Rivera, Juliana Pérez-Laspiur, María E Santiago-Gascot, Abner G Alemán-Reyes, Emanuel García-Santiago, Yolanda Rodríguez-Pérez, Cristhian Calo-Guadalupe, Inelia Otero-Pagán, Roxsana N Ayala-Pagán, Magdiel Martínez, Yisel M Cantres-Rosario, Loyda M Meléndez, Jennifer L Barreto-Estrada
The abuse of anabolic androgenic steroids (AAS) has been considered a major public health problem during decades. Supraphysiological doses of AAS may lead to a variety of neuroendocrine problems. Precisely, the hypothalamic-pituitary-gonadal (HPG) axis is one of the body systems that is mainly influenced by steroidal hormones. Fluctuations of the hormonal milieu result in alterations of reproductive function, which are made through changes in hypothalamic neurons expressing gonadotropin-releasing hormone (GnRH)...
2017: PloS One
https://www.readbyqxmd.com/read/28719222/how-drug-life-cycle-management-patent-strategies-may-impact-formulary-management
#5
Jan Berger, Jeffrey D Dunn, Margaret M Johnson, Kurt R Karst, W Chad Shear
Drug manufacturers may employ various life-cycle management patent strategies, which may impact managed care decision making regarding formulary planning and management strategies when single-source, branded oral pharmaceutical products move to generic status. Passage of the Hatch-Waxman Act enabled more rapid access to generic medications through the abbreviated new drug application process. Patent expirations of small-molecule medications and approvals of generic versions have led to substantial cost savings for health plans, government programs, insurers, pharmacy benefits managers, and their customers...
October 2016: American Journal of Managed Care
https://www.readbyqxmd.com/read/28719196/thermoresponsive-elastin-b-collagen-like-peptide-bioconjugate-nanovesicles-for-targeted-drug-delivery-to-collagen-containing-matrices
#6
Tianzhi Luo, Michael A David, Lucas C Dunshee, Rebecca A Scott, Morgan A Urello, Christopher Price, Kristi L Kiick
Over the past few decades, (poly)peptide block copolymers have been widely employed in generating well-defined nanostructures as vehicles for targeted drug delivery applications. We previously reported the assembly of thermoresponsive nanovesicles from an elastin-b-collagen like peptide (ELP-CLP). The nanoparticles were observed to dissociate at elevated temperatures, despite the LCST-like behavior of the tethered ELP domain, which is suggested to be triggered by the unfolding of the CLP domain. Here, the potential of using the nanoparticles as drug delivery vehicles for targeting collagen-containing matrices is evaluated...
July 18, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28719022/engineering-the-surface-of-smart-nanocarriers-using-a-ph-thermal-gsh-responsive-polymer-zipper-for-precise-tumor-targeting-therapy-in-vivo
#7
Penghui Zhang, Yan Wang, Jing Lian, Qi Shen, Chen Wang, Bohan Ma, Yuchao Zhang, Tingting Xu, Jianxin Li, Yongping Shao, Feng Xu, Jun-Jie Zhu
Nanocarrier surface chemistry plays a vital role in mediating cell internalization and enhancing delivery efficiency during in vivo chemotherapy. Inspired by the ability of proteins to alter their conformation to mediate functions, a pH-/thermal-/glutathione-responsive polymer zipper consisting of cell-penetrating poly(disulfide)s and thermosensitive polymers bearing guanidinium/phosphate (Gu(+) /pY(-) ) motifs to spatiotemporally tune the surface composition of nanocarriers for precise tumor targeting and efficient drug delivery is developed...
July 18, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28718703/nanoliposome-improves-inhibitory-effects-of-naringenin-on-nonalcoholic-fatty-liver-disease-in-mice
#8
Cong Chen, Xu Jie, Yangjie Ou, Yini Cao, Lu Xu, Yunxia Wang, Rong Qi
AIM: To prepare naringenin nanoliposome (NRG-Nanolipo) and investigate its inhibitory effects on nonalcoholic fatty liver disease (NAFLD). MATERIALS & METHODS: NRG-Nanolipo was prepared by thin-film rehydration method. Its characterizations and effects on NAFLD in mice induced by methionine choline deficient diet were investigated. RESULTS: NRG-Nanolipo had high-drug loading percentage and showed a sustained release profile. The nanoliposome formulation significantly increased oral absorption of naringenin (NRG)...
July 18, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28718641/in-silico-skin-model-a-multiscale-simulation-study-of-drug-transport
#9
Kishore Gajula, Rakesh Gupta, D B Sridhar, Beena Rai
Accurate in-silico models are required to predict the release of drug molecules through skin in order to supplement the in-vivo experiments for faster development/testing of drugs. The upper most layer of the skin, stratum corneum (SC), offers main resistance for permeation of actives. Most of the SC's molecular level models comprise of cholesterol, and phospholipids only, which is far from the reality. In this study we have implemented a multiscale modelling framework to obtain the release profile of three drugs namely Caffeine, Fentanyl and Naphthol through skin SC...
July 18, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28718478/gsh-responsive-supramolecular-nanoparticles-constructed-by-%C3%AE-d-galactose-modified-pillar-5-arene-and-camptothecin-prodrug-for-targeted-anticancer-drug-delivery
#10
Xin Liu, Wei Shao, Yanjing Zheng, Chenhao Yao, Luming Peng, Dongmei Zhang, Xiao-Yu Hu, Leyong Wang
Supramolecular construction of a targeted and stimuli-responsive drug delivery system is still a challenging task. Herein, GSH-responsive supramolecular prodrug nanoparticles were constructed by the host-guest complexation between a β-d-galactose-functionalized water-soluble pillar[5]arene (GalP5) and a disulfide bond containing camptothecin prodrug (G). The obtained prodrug nanoparticles were stable under physiological conditions, whereas efficient drug release was triggered in a simulated tumor environment with high GSH concentration...
July 18, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28717995/ovomucin-nanoparticles-promising-carriers-for-mucosal-delivery-of-drugs-and-bioactive-compounds
#11
Ali Akbari, Jianping Wu
Ovomucin, with a similar structure to mucin and gelation ability at room temperature, is a potential mucosal carrier. To evaluate this potential, the mucoadhesive property of ovomucin was studied by the tensile strength and rheology methods, and compared with three known mucoadhesive polymers, chitosan, polyacrylic acid (PAA), and alginate. Ovomucin particles were basically spherical in shape with an average size of ~572, 235 and 54 nm prepared at pH 5, 6.5, and 9, respectively. The absolute value of the zeta potential increased from ~ -51 mV at pH 5 to ~ -59 and -91 mV at pH 6...
July 17, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28717974/improvement-of-oral-bioavailability-of-lopinavir-without-co-administration-of-ritonavir-using-microspheres-of-thiolated-xyloglucan
#12
Ashwini R Madgulkar, Mangesh R Bhalekar, Ashwini A Kadam
Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation. The aim of this research was to formulate and characterize microspheres of lopinavir using thiolated xyloglucan (TH-MPs) as carrier to improve its oral bioavailability without co-administration of ritonavir. Thiomeric microspheres were prepared by ionotropic gelation between alginic acid and calcium ions. Interaction studies were performed using Fourier transform infrared spectroscopy (FT-IR). The thiomeric microspheres were characterized for its entrapment efficiency, T80, surface morphology, and mucoadhesion employing in vitro wash off test...
July 17, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28717926/clinical-evaluation-of-modified-release-and-immediate-release-tacrolimus-formulations
#13
Simon Tremblay, Rita R Alloway
The science of drug delivery has evolved considerably and has led to the development of multiple sustained release formulations. Each of these formulations can present particular challenges in terms of clinical evaluation and necessitate careful study to identify their optimal use in practice. Tacrolimus is an immunosuppressive agent that is widely used in organ transplant recipients. However, it is poorly soluble, has an unpredictable pharmacokinetic profile subject to important genetic polymorphisms and drug-drug interactions, and has a narrow therapeutic index...
July 17, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28717423/contribution-of-neuroblastoma-derived-exosomes-to-the-production-of-pro-tumorigenic-signals-by-bone-marrow-mesenchymal-stromal-cells
#14
Rie Nakata, Hiroyuki Shimada, G Esteban Fernandez, Rob Fanter, Muller Fabbri, Jemily Malvar, Pascale Zimmermann, Yves A DeClerck
The bone marrow (BM) niche is a microenvironment promoting survival, dormancy and therapeutic resistance in tumor cells. Central to this function are mesenchymal stromal cells (MSCs). Here, using neuroblastoma (NB) as a model, we demonstrate that NB cells release an extracellular vesicle (EVs) whose protein cargo is enriched in exosomal proteins but lacks cytokines and chemokines. Using three different purification methods, we then demonstrate that NB-derived exosomes were captured by MSCs and induced the production of pro-tumorigenic cytokines and chemokines, including interleukin-6 (IL-6), IL-8/CXCL8, vascular endothelial cell growth factor and monocyte-chemotactic protein-1, with exosomes prepared by size exclusion chromatography having the highest activity...
2017: Journal of Extracellular Vesicles
https://www.readbyqxmd.com/read/28717337/effect-of-surface-modification-on-the-in-vitro-protein-adsorption-and-cell-cytotoxicity-of-vinorelbine-nanoparticles
#15
Nandhakumar Sathyamoorthy, Dhanaraju Dasaratha Magharla, Sundar Devendaran Vankayalu
CONTEXT: Nanocarriers possessing long-circulating abilities could take advantage of the pathophysiology of tumor vasculature to achieve spatial placement. To attain such qualities, the drug carriers should possess suitable physicochemical properties such as size and surface hydrophilicity. AIM: The aim of this study was to prepare poly(ε-caprolactone) nanoparticles (NPs) loaded with vinorelbine bitartrate (VB) and to modify its steric properties using polyethylene glycol and poloxamer...
April 2017: Journal of Pharmacy & Bioallied Sciences
https://www.readbyqxmd.com/read/28717204/a-drug-carrier-for-sustained-zero-order-release-of-peptide-therapeutics
#16
Ya-Nan Zhao, Xiaoyu Xu, Na Wen, Rui Song, Qingbin Meng, Ying Guan, Siqi Cheng, Danni Cao, Yansheng Dong, Jiankun Qie, Keliang Liu, Yongjun Zhang
Peptides have great potential as therapeutic agents, however, their clinic applications are severely hampered by their instability and short circulation half-life. Zero-order release carriers could not only extend the circulation lifetime of peptides, but also maintain the plasma drug level constant, and thus maximize their therapeutic efficacy and minimize their toxic effect. Here using PEGylated salmon calcitonin (PEG-sCT)/tannic acid (TA) film as an example, we demonstrated that hydrogen-bonded layer-by-layer films of a PEGylated peptide and a polyphenol could be a platform for zero-order peptide release...
July 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28716778/thrombotic-microangiopathy-associated-with-intravenous-injection-of-extended-release-oxycodone
#17
Kate J Robson, Danielle Clucas, Robin Filshie, Harshal Nandurkar
We describe the case of a 35-year-old man presenting with thrombotic microangiopathy (TMA) and renal impairment following, as he later disclosed, intravenous injection of oral formulation tamper-resistant extended-release oxycodone hydrochloride (Oxycontin). Recurrent misuse of this agent was associated with relapsing TMA despite treatment with terminal complement inhibitor eculizumab. Cases of TMA have been reported in the USA in association with intravenous misuse of extended-release oxymorphone (Opana ER) after the introduction of a new non-crushable formulation in 2012...
July 17, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28716757/saturated-phosphatidylcholine-as-matrix-former-for-oral-extended-release-dosage-forms
#18
Marina Kolbina, Roland Bodmeier, Martin Körber
The aim of this study was to evaluate the suitability of saturated phosphatidylcholine (Phospholipon® 90H) as extended release excipient in matrix tablets for three model drugs with different aqueous solubility (theophylline, caffeine and diprophylline). The tablets could be prepared by direct compression because of the favorable phospholipid powder flow properties (Carr's index: 12.64 and angle of repose: 28.85) and good compactibility. Tablets of low porosity were formed already at low pressure of 40MPa and with drug loadings up to 70% due to high plasticity of the phospholipid...
July 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28716746/controlled-release-and-anti-proliferative-effect-of-imatinib-mesylate-loaded-sporopollenin-microcapsules-extracted-from-pollens-of-betula-pendula
#19
Idris Sargin, Lalehan Akyuz, Murat Kaya, Gamze Tan, Talip Ceter, Kevser Yildirim, Seymanur Ertosun, Gozde Hatun Aydin, Muge Topal
Sporopollenin is a promising material for drug encapsulation due to its excellent properties; uniformity in size, non-toxicity, chemically and thermally resilient nature. Herein, morphologically intact sporopollenin microcapsules were extracted from Betula pendula pollens. Cancer therapeutic agent (imatinib mesylate) was loaded into the microcapsules. The encapsulation efficiency by passive loading technique was found to be 21.46%. Release behaviour of the drug from microcapsules was found to be biphasic, with an initial fast release followed by a slower rate of release...
July 14, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28715864/in-vitro-and-in-vivo-anticancer-activity-of-2-acetyl-benzylamine-isolated-from-adhatoda-vasica-l-leaves
#20
C Balachandran, Y Arun, B Sangeetha, V Duraipandiyan, S Awale, N Emi, S Ignacimuthu, P T Perumal
One of the important aims of drug discovery for cancer is to find therapeutic agents from natural products that are effective and safe for cancer treatment. In the current study, an alkaloid, 2-acetyl-benzylamine, isolated from Adhatoda vasica, was screened for potent anticancer properties against leukemia cells. We used seven different types of leukemia cells such as CEM, NB-4, MOLM-14, Jurkat, IM-9, K562 and HL-60 for cytotoxic studies. 2-acetyl-benzylamine showed significant cytotoxic properties against MOLM-14 and NB-4 cells with IC50 values of 0...
July 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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