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Current Drug Delivery

Ekaterina S Dolinina, Elena V Parfenyuk
BACKGROUND: Warfarin, commonly used anticoagulant in clinic, has serious shortcomings due to its unsatisfactory pharmacodynamics. One of efficient ways of improvement of pharmacological and consumer properties of drugs is development of optimal drug delivery systems. OBJECTIVE: The aim of this work is synthesis of novel warfarin - silica composites and study in vitro the drug release kinetics to obtain the composites with controlled release. METHODS: The composites of warfarin with unmodified (UMS) and mercaptopropy modified silica (MPMS) were synthesized by sol-gel method...
October 21, 2016: Current Drug Delivery
Vinoth Lakshmanan
Flutamide (FLT) is a non steroidal antiandrogenic drug used to treat prostate cancer. Its poor aqueous solubility and toxicity are the major hindrance for oral drug delivery. The nanoformulation of flutamide increases its aqueous solubility thereby improves the therapeutic efficacy of the chemodrug. Poly (vinyl alcohol) (PVA) coated flutamide nanoparticles (PVA FLT NPs) were formulated by nanoprecipitation method and characterized by DLS, TEM and FTIR. The nanoparticles were about 300nm size and spherical in shape...
October 18, 2016: Current Drug Delivery
Prabhakar Panzade, Giridhar R Shendarkar
Pharmaceutical cocrystal is an emerging approach to tailor physicochemical and mechanical properties of drug substances. Cocrystals are composed of API and pharmaceutically acceptable coformer. It can be used to address the solubility, dissolution, mechanical properties, stability of drugs. This review discusses introduction to cocrystal, preparation and characterization, what USFDA says on cocrystal and role of Hansen solubility parameter to predict cocrystal. The effect of cocrystal on drug properties, dependence of cocrystal solubility on pH, concept of drug-drug cocrystal and aerosil 200 as novel cocrystal former and impact of cocrystal on drug pharmacokinetic has also been presented in this review along with highly selected examples of cocrystals...
October 18, 2016: Current Drug Delivery
Inderbir Singh, Vikas Rana
BACKGROUND: The study was aimed to enhance the mucoadhesive potential of Eudragit RS 100 and RL 100 using iron oxide. METHODS: Microspheres of Eudragit RS/RL100, containing cinnarizine, were prepared by emulsification solvent evaporation technique employing 32 full factorial design. Eudragit RS or RL (X1) and iron oxide (X2) concentrations were the independent variables. Particle size, entrapment efficiency, mucoadhesion, zeta potential and t90% were the response variables...
October 18, 2016: Current Drug Delivery
Prabodh Chander Sharma, Mona Piplani, Harish Rajak
In the present study, a novel strategy was developed to construct lipid prodrug of norfloxacin. N-Mannich base of norfloxacin was synthesized. The prodrug was obtained by covalently coupling this N-Mannich base with fatty acid hydrazide. The synthesized prodrug was characterized by spectral as well as other physical analysis. The hydrolytic studies of prodrug in buffers (pH 1.2 and 7.4), simulated gastric and intestinal fluid by HPLC analysis were undertaken. The studies revealed that prodrug liberates only about 2% of norfloxacin in HCl buffer (pH 1...
October 18, 2016: Current Drug Delivery
Shoriya Aruni Abdul Manaf, Gurumurthy Hedge, Uttam Kumar Mandal, Wong Tin Wui, Partha Roy
BACKGROUND: Nano-scale carbon systems are emerging alternatives in drug delivery and bioimaging applications of which they gradually replace the quantum dots characterized by toxic heavy metal content in the latter application. OBJECTIVE: The work intended to use carbon nanospheres synthesized from biowaste Sago bark for cancer cell imaging applications. METHODS: This study synthesised carbon nanospheres from biowaste Sago bark using a catalyst-free pyrolysis technique...
October 17, 2016: Current Drug Delivery
Marianne Hiorth
Dental caries: Dental caries and periodontitis were for many decades considered the most important global oral health burden. During the last 40 years when more focus was put on the prevention of dental caries by using products with fluoride, the problem decreased. However, our new lifestyle with more sugar has given rise to concern, and in US the amount of children being diagnosed with dental caries has increased [1]. In addition the increasing amount of elderly in the population using many different types of medicines giving dry mouth has a negative impact of the status of their teeth [2]...
October 13, 2016: Current Drug Delivery
Juliana Hotta, Wilson Gustavo Cral, Vinicius Tatsuyuji Sakima, Vanessa Soares Lara, Vanessa Migliorini Urban, Karin Hermana Neppelenbroek
BACKGROUND: Antifungal agents incorporated into temporary denture resilient liners as drug carries and delivery have been suggested as an alternative treatment for denture stomatitis. However, to test the in vivo biocompatibility of this protocol, standardization of an intraoral device for optimal drug delivery is required. OBJECTIVE: Standardized criteria were produced to adjust an acrylic intraoral device (IOD) for rats feasible for denture stomatitis treatment by sustained drug-delivery based on minimal inhibitory drug concentrations (MICs) of antifungals for Candida albicans biofilm...
October 13, 2016: Current Drug Delivery
Seunghee Cha, Hong-Kyun Kim, Hong-Seop Kho, Young Seok Park
Pilocarpine hydrochloride is commonly prescribed to patients with dry mouth and eye using a frequent dosing schedule. The aim of this study was to evaluate the sustained effects of this highly soluble drug carried by a gelatin hydrogel, which was administered by an implant mediated drug delivery system (IMDDS). The IMDDS was installed in a total of 24 rabbits. After complete healing, pilocarpine hydrochloride was administered as 30 mg per se (Group 1; n=8), 30 mg in gelatin hydrogel (Group 2; n=8), and 60 mg in gelatin hydrogel (Group 3; n=8)...
October 13, 2016: Current Drug Delivery
Chintan A Dalwadi, Gayatri C Patel
BACKGROUND: The objective of the study was to investigate the cytotoxicity and cellular uptake of prepared 5-Fluorouracil (5-FU) nanohydrogel formulation using KB oral cancer cell line and VERO fibroblast cell line. METHOD: The biodegradable thermoresponsive modified methylcellulose (MMC) polymer was used for the preparation of nanohydrogel whereas it shows sol-gel phase transition at 36˚C to 40˚C. The physical crosslinking method was used followed by probe sonication for the preparation of 5-FU loaded MMC nanohydrogel...
October 13, 2016: Current Drug Delivery
Somayeh Kadkhodayan, Azam Bolhassani, Seyed Mehdi Sadat, Shiva Irani, Fatemeh Fotouhi
Cell penetrating peptides (CPPs) or protein transduction domains (PTDs) have been known as a new field in cargo delivery. These peptides such as Tat, Pep-1 and Cady-2 are able to deliver genes and biologically active proteins to cytoplasmic compartments via the plasma membrane. In current study, the efficiency of pEGFP-N1 eukaryotic vector for expression of HIV-1 Tat-Nef fusion was evaluated in HEK-293T cells using TurboFect transfection reagent. In addition, the recombinant GST-Tat-Nef protein was generated in E...
October 6, 2016: Current Drug Delivery
Andrés Felipe Cartagena, Amanda Lyra, Aline Cristina Kapuchczinski, Amanda Miglirioni Urban, Luiz Antônio Esmerino, Traudi Klein, Jessica Mendes Nadal, Paulo Vitor Farago, Nara Hellen Campanha
The aim of this study was to prepare and to evaluate Eudragit L100 and Gantrez MS-955 microparticles containing miconazole nitrate for buccal delivery. Microparticles were prepared by spray-drying method in order to achieve high encapsulation efficiency and increased drug solubility. The microparticles were obtained containing 10% and 20% (w/w) of drug:polymer ratio using Eudragit L100 (E10 and E20), Gantrez MS-955 (G10 and G20) or their combination (EG10 and EG20). The influence of formulation factors (drug:polymer ratio, type of polymer) on yield, encapsulation efficiency, particle size, Fourier-transformed infrared spectroscopy (FTIR), X-ray diffraction, differential scanning calorimetry, in vitro drug release and antifungal activity were investigated...
October 6, 2016: Current Drug Delivery
Jaleh Varshosaz, Mohsen Minayian, Shila Yazdekhasti
Tacrolimus, an immunosuppressive drug has a variable pharmacokinetic and poor oral bioavailability due to poor solubility. The aim of the present study was enhancing the solubility and oral bioavailability of this drug. Tacrolimus nanoparticles were prepared by precipitation anti-solvent evaporation method. The effect of different parameters including: surfactant type, solvent to nonsolvent ratio and drug to surfactant ratio were studied on the particle size, saturated solubility and dissolution rate of the drug...
October 3, 2016: Current Drug Delivery
Xiaoxi Li, Meiyan Yang, Yueqing Li, Wei Gong, Yuli Wang, Li Shan, Shuai Shao, Chunsheng Gao, Wu Zhong
The solubilization of poorly water-soluble drugs remains challenging. The purpose of this study was to design a liquid formulation that can improve the solubility of poorly water-soluble weakly acidic ST-246, an anti-smallpox drug. Soluble ternary cyclodextrin complexations (t-CDs) containing ST-246, 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) and meglumine (MEG) were prepared and optimized. Interestingly, the solubility of ST-246 was improved dramatically from 3µg/ml (in water, 37ºC) to 50mg/ml in the optimized t-CDs (ST-246/MEG/HP-β-CD, 1:2:6 weight ratio)...
October 3, 2016: Current Drug Delivery
Norihito Shimamura, Naoya Matsuda, Kosuke Katayama, Kiyohide Kakuta, Takeshi Katagai, Harumitsu Yamanaka, Hiroki Ohkuma
BACKGROUND: An insult due to intracerebral hemorrhage (ICH) is critical to patients. So, breakthroughs in ICH treatment are very important. OBJECTIVE: Advances in the stem cell treatment of stroke have been remarkable. And stem cell experimentation on ischemic stroke, however, preceded such work on ICH and did not emphasized ICH therapy. METHOD: We review recent stem cell treatments for ICH, an experimental model of ICH, the medical care of ICH, and several stem cell therapies for ICH along with future prospects...
September 22, 2016: Current Drug Delivery
Jaywant N Pawar, Meer Tarique Ali, Ritesh A Fule, Kailas K Moravkar, Madhavsingh Seervi, Sadhana S Sathaye, Purnima D Amin
A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug. BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder...
September 20, 2016: Current Drug Delivery
Kamil Duris, Jolana Lipkova
BACKGROUND: Stroke is the second leading cause of death worldwide. Understanding of gene expression dynamics could bring new approaches in diagnostics and therapy of stroke. Small noncoding molecules termed "microRNA" represent the most flexible network of gene expression regulators. METHODS: The aim of this review was to briefly describe the structure and function of microRNA and summarize the current knowledge about the involvement of microRNAs in the pathophysiology of ischemic and hemorrhagic stroke based on both experimental and clinical studies...
September 19, 2016: Current Drug Delivery
Angélica A Ochoa-Flores, Josafat A Hernández-Becerra, Adriana Cavazos-Garduño, Ida Soto-Rodriguez, Maria Guadalupe Sanchez-Otero, Eduardo J Vernon-Carter, Hugo S Garcia
Curcumin is a natural, oil-soluble polyphenolic compound with potent anticancer, antiinflammatory, and antioxidant activities. In its free form it is very poorly absorbed in the gut due to its very low solubility. The use of nanoemulsions as carrier is a feasible way for improving curcumin bioavailability. To this end, the choice of emulsifying agent for stabilizing the nanoemulsions is of the upmost importance for achieving a desired functionality. In this work, phosphatidylcholine (PC) and phosphatidycholine enriched (PCE) with medium chain fatty acids (42...
September 19, 2016: Current Drug Delivery
Danay Dupeyrón, Monique Kawakami, Jacques Rieumont, José Carvalho
Açaí berry, from the Euterpe oleracea Mart. Palm, has been described as the most important fruit in the Brazilian Amazon. Several studies have reported that anthocyanins (ACNs), one of the major components of the açaí, have enormous potential for pharmaceuticals applications. However, the bioavailability of anthocyanins is relatively low compared to that of other flavonoids. Then, in the present work, anthocyanins-loaded nanoparticles have been developed to overcome their poor bioavailability. Also, the effect of EUDRAGIT® L100, polyethylene glycol 2000 (PEG 2000) and polysorbate 80 on encapsulation efficiency (EE) of anthocyanins has been evaluated...
September 15, 2016: Current Drug Delivery
Yu Hasegawa, Ken Uekawa, Takayuki Kawano, Hidenori Suzuki, Shokei Kim-Mitsuyama
BACKGROUND: Although sphingosine 1-phosphate (S1P) receptor activation by FTY720 (fingolimod) has been suggested to improve the prognosis of experimental stroke, the effect of the drug in early brain injury (EBI) after subarachnoid hemorrhage (SAH) and the precise mechanism of the effect are undetermined. In this study, we investigated the protective effect of systemic administration of FTY720 in EBI after SAH and assessed the mechanism using intracerebroventricular infusion of VPC23019 which is the S1P receptor antagonist...
September 6, 2016: Current Drug Delivery
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