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Pharmaceutical nanocrystals

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https://www.readbyqxmd.com/read/29326082/pharmaceutical-nanocrystals-production-by-wet-milling-and-applications
#1
REVIEW
Maria Malamatari, Kevin M G Taylor, Stavros Malamataris, Dennis Douroumis, Kyriakos Kachrimanis
Nanocrystals are regarded as an important nanoformulation approach exhibiting advantages of increased dissolution and saturation solubility with chemical stability and low toxicity. Nanocrystals are produced in the form of nanosuspensions using top-down (e.g., wet milling or high pressure homogenization) and bottom-up methods (e.g., antisolvent precipitation). Wet milling is a scalable method applicable to drugs with different physicochemical and mechanical properties. Nanocrystalline-based formulations, either as liquid nanosuspensions or after downstream processing to solid dosage forms, have been developed as drug delivery systems for various routes of administration (i...
January 8, 2018: Drug Discovery Today
https://www.readbyqxmd.com/read/29285948/translation-of-combination-nanodrugs-into-nanomedicines-lessons-learned-and-future-outlook
#2
Qingxin Mu, Jesse Yu, Lisa A McConnachie, John C Kraft, Yu Gao, Gaurav K Gulati, Rodney J Y Ho
The concept of nanomedicine is not new. For instance, some nanocrystals and colloidal drug molecules are marketed that improve pharmacokinetic characteristics of single-agent therapeutics. For the past two decades, the number of research publications on single-agent nanoformulations has grown exponentially. However, formulations advancing to preclinical and clinical evaluations that lead to therapeutic products has been limited. Chronic diseases such as cancer and HIV/AIDS require drug combinations, not single agents, for durable therapeutic responses...
December 29, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/29244515/millisecond-self-assembly-of-stable-nano-dispersed-drug-formulations
#3
Vikram J Pansare, Aditya Rawal, Aaron Goodwin, Ron Beyerinck, Robert K Prud'homme, Dwayne T Friesen, Michael Grass, Annie Muske-Dukes, David T Vodak
We report the development of a new Spray-drying and Nanoparticle Assembly Process (SNAP), that enables the formation of stable, yet rapidly dissolving, sub-200 nm nano-crystalline particles within a high Tg glassy matrix. SNAP expands the class of drugs that Spray Dried Dispersion (SDD) processing can address to encompass highly crystalline, but modestly hydrophobic drugs that are difficult to process by conventional SDD. The process integrates rapid precipitation and spray drying within a custom designed nozzle to produce high supersaturations and precipitation of the drug and high Tg glassy polymer...
December 15, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29216759/pharmaceutical-potential-of-quantum-dots
#4
Swati Jha, Prateek Mathur, Suman Ramteke, Narendra Kumar Jain
Quantum dots (QDs) or fluorescent nanocrystals are designed nanoparticles that are promising for several biological and bio-medical applications as well as drug delivery and simultaneous cellular imaging. QD's have exhibited promising potential primarily in receptor based targeting as a result of their distinctive physicochemical properties. Functionalized QDs (f-QDs) have been developed as effective, safe, nano-sized smart systems to deliver a wide range of bio-actives. Surface modified fluorescent carbon QDs with surface modification have attracted attention as targeting ligand to accomplish cellular targeting with enhanced specificity...
December 7, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29186990/nanomedicine-approaches-for-sirolimus-delivery-a-review-of-pharmaceutical-properties-and-preclinical-studies
#5
Azadeh Haeri, Mahraz Osouli, Fereshteh Bayat, Sonia Alavi, Simin Dadashzadeh
Sirolimus (rapamycin) is a mammalian target of rapamycin (mTOR) inhibitor with immunosuppressive, antiproliferative, antiangiogenic, antifungal, anti-restenosis and anti-inflammatory properties. However, its clinical application is often hampered by poor aqueous solubility, first-pass metabolism, transport by p-glycoprotein efflux pump, limited oral bioavailability and nonspecific distribution in off-target sites. Recently, various formulation strategies have emerged to overcome these limitations. Among these, pharmaceutical nanotechnology with numerous advantages has great potential for sirolimus delivery...
November 29, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29183856/mesoporous-systems-for-poorly-soluble-drugs-recent-trends
#6
Joakim Riikonen, Wujun Xu, Vesa-Pekka Lehto
When poor aqueous solubility of active pharmaceutical ingredients is encountered during a drug formulation process, the toolbox typically utilized contains pharmaceutical salts, co-crystals, solid dispersions, cyclodextrins, lipids, liposomes and nanocrystals etc. Especially in the pharmaceutical industry, the option which confers the greatest benefit with the lowest risk is usually chosen. Several factors affect the final decision, but new technologies should also be considered especially if they can address several issues at the same time...
November 25, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29171679/self-assembled-hybrid-materials-based-on-organic-nanocrystals-and-carbon-nanotubes
#7
Angelica Niazov-Elkan, Haim Weissman, Sounak Dutta, Sidney R Cohen, Mark A Iron, Iddo Pinkas, Tatyana Bendikov, Boris Rybtchinski
Organic crystalline materials are used as dyes/pigments, pharmaceuticals, and active components of photonic and electronic devices. There is great interest in integrating organic crystals with inorganic and carbon nanomaterials to create nanocomposites with enhanced properties. Such efforts are hampered by the difficulties in interfacing organic crystals with dissimilar materials. Here, an approach that employs organic nanocrystallization is presented to fabricate solution-processed organic nanocrystal/carbon nanotube (ONC/CNT) hybrid materials based on readily available organic dyes (perylene diimides (PDIs)) and carbon nanotubes...
November 24, 2017: Advanced Materials
https://www.readbyqxmd.com/read/29128423/amorphous-solid-dispersions-and-nanocrystal-technologies-for-poorly-water-soluble-drug-delivery-an-update
#8
Scott V Jermain, Chris Brough, Robert O Williams
Poor water-solubility remains a typical property of drug candidates in pharmaceutical development pipelines today. Various processes have been developed to increase the solubility, dissolution rate, and bioavailability of these active ingredients belonging to biopharmaceutical classification system (BCS) II and IV classifications. Since the early 2000s, nanocrystal delivery and amorphous solid dispersions are more established techniques to overcome the limitations of poorly-water soluble drugs in FDA available products...
November 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28963600/ros-mediated-cytotoxic-activity-of-zno-and-ceo2-nanoparticles-synthesized-using-the-rubia-cordifolia-l-leaf-extract-on-mg-63-human-osteosarcoma-cell-lines
#9
Natarajan Sisubalan, Vijayan Sri Ramkumar, Arivalagan Pugazhendhi, Chandrasekaran Karthikeyan, Karuppusamy Indira, Kasi Gopinath, Abdulrahman Syedahamed Haja Hameed, Mohamed Hussain Ghouse Basha
In the present scenario, the synthesis and characterization of zinc oxide (ZnO) and cerium oxide (CeO2) nanoparticles (NPs) through biological routes using green reducing agents are quite interesting to explore various biomedical and pharmaceutical applications, particularly for the treatment of cancer. This study was focused on the phytosynthesis of ZnO and CeO2 NPs using the leaf extract of Rubia cordifolia L. The active principles present in the plant extract were liable for rapid reduction of Zn and Ce ions to metallic nanocrystals...
September 29, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28956456/production-of-drug-nanosuspensions-effect-of-drug-physical-properties-on-nanosizing-efficiency
#10
Tao Liu, Rainer H Müller, Jan P Möschwitzer
Objective Drug nanosuspension is one of the established methods to improve the bioavailability of poorly soluble drugs. Drug physical properties aspect (morphology, solid state, starting size et al) is a critical parameter determining the production efficiency. Some drug modification approaches such as spray-drying were proved to improve the millability of drug powders. However, the mechanism behind those improved performances is unclear. This study is to systematically investigate the influence of those physical properties...
September 28, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28917964/phenazopyridine-phthalimide-nano-cocrystal-release-rate-and-oral-bioavailability-enhancement
#11
Yu Huang, Jin-Mei Li, Zhi-Hui Lai, Jun Wu, Tong-Bu Lu, Jia-Mei Chen
Both cocrystal and nanocrystal technologies have been widely used in the pharmaceutical development for poorly soluble drugs. However, the synergistic effects due to the integration of these two technologies have not been well investigated. The aim of this study is to develop a nano-sized cocrystal of phenazopyridine (PAP) with phthalimide (PI) to enhance the release rate and oral bioavailability of PAP. A PAP-PI nano-cocrystal with particle diameter of 21.4±0.1nm was successfully prepared via a sonochemical approach and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and dynamic light scattering (DLS) analysis...
September 14, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28860715/aceclofenac-nanocrystals-with-enhanced-in-vitro-in-vivo-performance-formulation-optimization-characterization-analgesic-and-acute-toxicity-studies
#12
Haroon Rahim, Abdul Sadiq, Shahzeb Khan, Mir Azam Khan, Syed Muhammad Hassan Shah, Zahid Hussain, Riaz Ullah, Abdelaaty Abdelaziz Shahat, Khalid Ibrahim
This study was aimed to enhance the dissolution rate, oral bioavailability and analgesic potential of the aceclofenac (AC) in the form of nanosuspension using cost-effective simple precipitation-ultrasonication approach. The nanocrystals were produced using the optimum conditions investigated for AC. The minimum particle size (PS) and polydispersity index was found to be 112±2.01 nm and 0.165, respectively, using hydroxypropyl methylcellulose (1%, w/w), polyvinylpyrrolidone K30 (1%, w/w) and sodium lauryl sulfate (0...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28753280/nanoparticle-based-immunochemical-biosensors-and-assays-recent-advances-and-challenges
#13
REVIEW
Zdeněk Farka, Tomáš Juřík, David Kovář, Libuše Trnková, Petr Skládal
We review the progress achieved during the recent five years in immunochemical biosensors (immunosensors) combined with nanoparticles for enhanced sensitivity. The initial part introduces antibodies as classic recognition elements. The optical sensing part describes fluorescent, luminescent, and surface plasmon resonance systems. Amperometry, voltammetry, and impedance spectroscopy represent electrochemical transducer methods; electrochemiluminescence with photoelectric conversion constitutes a widely utilized combined method...
August 9, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28702816/enhancing-the-solubility-of-fenofibrate-by-nanocrystal-formation-and-encapsulation
#14
Raj Kumar, Prem Felix Siril
Development of techniques to enhance bioavailability of drugs having poor water solubility is a big challenge for pharmaceutical industry. Solubility can be enhanced by particle size reduction and encapsulation using hydrophilic polymers. Fenofibrate (FF) is a drug for regulating lipids. Multi-fold enhancement in solubility of FF has been achieved by nanocrystal formation in the present study. Nanoparticles were prepared by an evaporation-assisted solvent-antisolvent interaction (EASAI) approach. Water-soluble polymers, viz...
July 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28629862/sustained-delivery-of-bsa-hsa-from-biocompatible-plant-cellulose-nanocrystals-for-in-vitro-cholesterol-release-from-endothelial-cells
#15
Rubbel Singla, Sourabh Soni, Yogendra S Padwad, Amitabha Acharya, Sudesh Kumar Yadav
Nanocomposites of plant cellulose nanocrystals (CNCs) were developed by binding model proteins BSA and HSA onto CNCs by physical adsorption and chemical conjugation methods The spectroscopy and microscopy studies confirmed the protein binding onto CNCs. Phosphate buffer saline (pH=4.0, 7.4) and simulated gastric and intestinal fluids (SGF/SIF; pH=1.1/6.5) showed maximum protein release of ∼62% over a period of time. The released proteins were found to retain both structural integrity as well as≥90% of bioactivity...
November 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28603030/nanosizing-techniques-for-improving-bioavailability-of-drugs
#16
REVIEW
Raida Al-Kassas, Mahima Bansal, John Shaw
The poor solubility of significant number of Active Pharmaceutical Ingredients (APIs) has become a major challenge in the drug development process. Drugs with poor solubility are difficult to formulate by conventional methods and often show poor bioavailability. In the last decade, attention has been focused on developing nanocrystals for poorly water soluble drugs using nanosizing techniques. Nanosizing is a pharmaceutical process that changes the size of a drug to the sub-micron range in an attempt to increase its surface area and consequently its dissolution rate and bioavailability...
June 8, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28585942/progress-of-crystallization-in-microfluidic-devices
#17
REVIEW
Huan-Huan Shi, Yan Xiao, Steven Ferguson, Xin Huang, Na Wang, Hong-Xun Hao
Microfluidic technology provides a unique environment for the investigation of crystallization processes at the nano or meso scale. The convenient operation and precise control of process parameters, at these scales of operation enabled by microfluidic devices, are attracting significant and increasing attention in the field of crystallization. In this paper, developments and applications of microfluidics in crystallization research including: crystal nucleation and growth, polymorph and cocrystal screening, preparation of nanocrystals, solubility and metastable zone determination, are summarized and discussed...
June 6, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28530283/composite-cd-mof-nanocrystals-containing-microspheres-for-sustained-drug-delivery
#18
Haiyan Li, Nana Lv, Xue Li, Botao Liu, Jing Feng, Xiaohong Ren, Tao Guo, Dawei Chen, J Fraser Stoddart, Ruxandra Gref, Jiwen Zhang
Metal-organic frameworks (MOFs), which are typically embedded in polymer matrices as composites, are emerging as a new class of carriers for sustained drug delivery. Most of the MOFs and the polymers used so far in these composites, however, are not pharmaceutically acceptable. In the investigation reported herein, composites of γ-cyclodextrin (γ-CD)-based MOFs (CD-MOFs) and polyacrylic acid (PAA) were prepared by a solid in oil-in-oil (s/o/o) emulsifying solvent evaporation method. A modified hydrothermal protocol has been established which produces efficiently at 50 °C in 6 h micron (5-10 μm) and nanometer (500-700 nm) diameter CD-MOF particles of uniform size with smooth surfaces and powder X-ray diffraction patterns that are identical with those reported in the literature...
June 8, 2017: Nanoscale
https://www.readbyqxmd.com/read/28527464/-14-n-nqr-lineshape-in-nanocrystals-an-ab-initio-investigation-of-urea
#19
Alan Gregorovič
(14)N nuclear quadrupole resonance (NQR) lineshapes mostly contain information of low interest, although in nanocrystals they may display some unexpected behaviour. In this work, we present an ab initio computational study of the (14)N NQR lineshapes in urea nanocrystals as a function of the nanocrystal size and geometry, focusing on the surface induced broadening of the lineshapes. The lineshapes were obtained through a calculation of the electric field gradient for each nitrogen site in the nanocrystal separately, taking into account the individual crystal field by embedding the molecule of interest in a suitable lattice of point multipoles representing other urea molecules in the nanocrystal...
May 21, 2017: Journal of Chemical Physics
https://www.readbyqxmd.com/read/28504148/enhanced-emulsifying-properties-of-wood-based-cellulose-nanocrystals-as-pickering-emulsion-stabilizer
#20
Xiaoyu Gong, Yixiang Wang, Lingyun Chen
Cellulose nanocrystals are hydrophilic nanomaterials, which limits their applications as interfacial compounds. Herein, we propose using modified wood-based cellulose nanocrystals as Pickering emulsion stabilizer. Wood cellulose was consecutively oxidized and modified with phenyltrimethylammonium chloride to create hydrophobic domains comprised of phenyl groups. These modified oxidized cellulose nanocrystals (m-O-CNCs) were homogeneous/electrostatically stable in water and they can stabilize O/W Pickering emulsions...
August 1, 2017: Carbohydrate Polymers
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