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Pharmaceutical nanocrystals

A R Fernandes, J Dias-Ferreira, C Cabral, M L Garcia, E B Souto
The clinical use of poorly water-soluble drugs has become a big challenge in pharmaceutical development due to the compromised bioavailability of the drugs in vivo. Nanocrystals have been proposed as a formulation strategy to improve the dissolution properties of these drugs. The benefits of using nanocrystals in drug delivery, when compared to other nanoparticles, are related to their production facilities, simple structure, and suitability for a variety of administration routes. High pressure homogenization (HPH) is the most promising production process, which can be employed at low or high temperatures...
March 5, 2018: Colloids and Surfaces. B, Biointerfaces
Juan Zhao, Yangyang Liu, Lulu Wang, Yuqi Zhou, Juan Du, Yancai Wang
In the face of a large number of insoluble drugs, the development of nanocrystals is effective in destroying the limits of poorly soluble drug applications and becoming an indispensable route of drug delivery in the pharmaceutical industry. In addition, the proposed delivery goal is to provide more convenience and benefits and the number of researchers who are developing a number of advanced technologies try to use improved nano-drugs to improve the bioavailability of drug, drug dissolution velocity and solubility...
August 1, 2018: Journal of Nanoscience and Nanotechnology
Pascal Pellen-Mussi, Sylvie Tricot-Doleux, Chrystelle Neaime, Nicolas Nerambourg, Francisco Cabello-Hurtado, Stéphane Cordier, Fabien Grasset, Sylvie Jeanne
CONTEXT: as a kind of non-metal oxide SiO2 NPs have been extensively used in biomedicine, pharmaceuticals and other industrial manufacturing fields, such as DNA delivery, cancer therapy… Our group had developed a method based on microemulsion process to prepare SiO2 NPs incorporating photonic or magnetic nanocrystals and luminescent nanosized inorganic metal atom clusters. However, the toxicity of nanoparticles is known to be closely related to their physico-chemical characteristics and chemical composition...
May 1, 2018: Journal of Nanoscience and Nanotechnology
Lucía López-Hortas, Patricia Pérez-Larrán, María Jesús González-Muñoz, Elena Falqué, Herminia Domínguez
Ursolic acid (UA) is a pentacyclic triterpenoid widely found in herbs, leaves, flowers and fruits; update information on the major natural sources or agro-industrial wastes is presented. Traditional (maceration, Soxhlet and heat reflux) and modern (microwave-, ultrasound-, accelerated solvent- and supercritical fluid) extraction and purification technologies of UA, as well as some patented process, are summarized. The great interest in this bioactive compound is related to the beneficial effects in human health due to antioxidant, antimicrobial, anti-inflammatory, hepatoprotective, immunomodulatory, anti-tumor, chemopreventive, cardioprotective, antihyperlipidemic and hypoglycemic activities, and others...
January 2018: Food Research International
Puneet Tyagi, J Anand Subramony
Nanotechnology ushered the field of medicine in to a new era. Miniaturization, increased surface area, and the unique physicochemical properties in the nano dimension were explored for new applications. Pharmaceutical industry picked up the technology and early success came fast for oral drug delivery through improvement in dissolution properties of the active molecules. Many products were launched using the nanocrystal technology on the oral side. Further development of polymeric nanoparticles led to wide spread research of nanocarriers for parenteral delivery...
January 16, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Xia Li, Jun Li, Jie Gong, Yishan Kuang, Lihuan Mo, Tao Song
In recent years, nanocelluloses have attracted a lot of interests as promising stabilizers for Pickering emulsion particularly in food, cosmetics and pharmaceutics industries. In this work, two cellulose nanocrystals (named CNCs-I and CNCs-II) with different crystalline allomorph were investigated as stabilizers for oil-water Pickering emulsion. CNCs were prepared by sulfuric acid hydrolysis of unmodified and mercerized microcrystalline cellulose (MCC), respectively. CNCs-I was needle-like particles (length - 200 nm, width - 16...
March 1, 2018: Carbohydrate Polymers
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
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
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
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
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
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...
January 30, 2018: International Journal of Pharmaceutics
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...
January 2018: Advanced Materials
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...
January 15, 2018: International Journal of Pharmaceutics
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
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
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
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
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
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
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