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Pharmaceutical nanocrystals

Sandeep K Singh, Vishal Makadia, Shweta Sharma, Mamunur Rashid, Sudhir Shahi, Prabhat R Mishra, Mohammed Wahajuddin, Jiaur R Gayen
Trans -resveratrol (t-RES) is a natural polyphenolic compound with extensive therapeutic activities; however, its clinical application is circumscribed due to its poor solubility and low bioavailability. The purpose of this study was to prepare stable t-RES nanocrystals (t-RES-NCs) with different stabilizers to improve its oral bioavailability. t-RES-NCs were fabricated by the probe sonication method and optimized by particles size, poly dispersive index and zeta potential. The pharmaceutical characterization of t-RES-NCs was further performed systematically...
February 13, 2017: Drug Delivery and Translational Research
Djalal Trache, M Hazwan Hussin, M K Mohamad Haafiz, Vijay Kumar Thakur
Cellulose nanocrystals, a class of fascinating bio-based nanoscale materials, have received a tremendous amount of interest both in industry and academia owing to its unique structural features and impressive physicochemical properties such as biocompatibility, biodegradability, renewability, low density, adaptable surface chemistry, optical transparency, and improved mechanical properties. This nanomaterial is a promising candidate for applications in fields such as biomedical, pharmaceuticals, electronics, barrier films, nanocomposites, membranes, supercapacitors, etc...
January 24, 2017: Nanoscale
Rohan Ghadi, Neha Dand
BCS class IV drugs (e.g., amphotericin B, furosemide, acetazolamide, ritonavir, paclitaxel) exhibit many characteristics that are problematic for effective oral and per oral delivery. Some of the problems associated include low aqueous solubility, poor permeability, erratic and poor absorption, inter and intra subject variability and significant positive food effect which leads to low and variable bioavailability. Also, most of the class IV drugs are substrate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further potentiates the problem of poor therapeutic potential of these drugs...
January 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
Junidah Lamaming, Rokiah Hashim, Cheu Peng Leh, Othman Sulaiman
Cellulose nanocrystals were isolated from oil palm trunk by total chlorine free method. The samples were either water pre-hydrolyzed or non-water pre-hydrolyzed, subjected to soda pulping, acidified and ozone bleached. Cellulose and cellulose nanocrystal (CNC) physical, chemical, thermal properties, and crystallinity index were investigated by composition analysis, scanning electron microscopy, transmission electron microscopy, fourier transform infrared, thermogravimetric analysis and X-ray diffraction. Water pre-hydrolysis reduced lignin (<0...
January 20, 2017: Carbohydrate Polymers
Shreya Thakkar, Viral Shah, Manju Misra, Kiran Kalia
BACKGROUND: Most of the chemical substances which emerge out as potential drug candidates (Active Pharmaceutical Ingredients) are either weak acids or weak bases. Poor aqueous solubility of these drug substances is a common concern. Several R&D centers are focused on developing suitable, economic, simpler and more feasible solubility enhancement techniques for increasing the solubility and thereby bioavailability of such drug substances. Nanocrystals is one of the preferred approaches for solubility enhancement in last few decades...
October 14, 2016: Recent Patents on Nanotechnology
Mariana T Farcas, Elena R Kisin, Autumn L Menas, Dmitriy W Gutkin, Alexander Star, Richard S Reiner, Naveena Yanamala, Kai Savolainen, Anna A Shvedova
Over the past several years there has been an increased number of applications of cellulosic materials in many sectors, including the food industry, cosmetics, and pharmaceuticals. However, to date, there are few studies investigating the potential adverse effects of cellulose nanocrystals (CNC). The objective of this study was to determine long-term outcomes on the male reproductive system of mice upon repeated pharyngeal aspiration exposure to CNC. To achieve this, cauda epididymal sperm samples were analyzed for sperm concentration, motility, morphological abnormalities, and DNA damage...
2016: Journal of Toxicology and Environmental Health. Part A
Yogendra Nayak, Kiran Avadhani, Srinivas Mutalik, Usha Y Nayak
BACKGROUND: HIV infection persists for a longer time in AIDS patient compared to many other viral diseases. This is mainly because the HIV resides maximally in lymphatic system mainly the lymph nodes. Most of the present anti-HIV drugs have very poor bioavailability at lymphatic tissue. Hence, pharmaceutical scientists have made many efforts to formulate anti-HIV drugs for targeting lymphatic system. The exploration of nanoparticulate drug delivery systems have been popularly investigated for lymphatic targeting and for improving therapeutic efficacy...
2016: Recent Patents on Nanotechnology
Bryan J Harper, Alicea Clendaniel, Federico Sinche, Daniel Way, Michael Hughes, Jenna Schardt, John Simonsen, Aleksandr B Stefaniak, Stacey L Harper
Cellulose is an abundant and renewable resource currently being investigated for utility in nanomaterial form for various promising applications ranging from medical and pharmaceutical uses to mechanical reinforcement and biofuels. The utility of nanocellulose and wide implementation ensures increasing exposure to humans and the environment as nanocellulose-based technologies advance. Here, we investigate how differences in aspect ratio and changes to surface chemistry, as well as synthesis methods, influence the biocompatibility of nanocellulose materials using the embryonic zebrafish...
June 2016: Cellulose
Dritan Hasa, Carlotta Giacobbe, Beatrice Perissutti, Dario Voinovich, Mario Grassi, Antonio Cervellino, Norberto Masciocchi, Antonietta Guagliardi
Microcrystalline vinpocetine, coground with cross-linked polyvinylpyrrolidone, affords hybrids containing nanosized drug nanocrystals, the size and size distributions of which depend on milling times and drug-to-polymer weight ratios. Using an innovative approach to microstructural characterization, we analyzed wide-angle X-ray total scattering data by the Debye function analysis and demonstrated the possibility to characterize pharmaceutical solid dispersions obtaining a reliable quantitative view of the physicochemical status of the drug dispersed in an amorphous carrier...
September 6, 2016: Molecular Pharmaceutics
Afshin Faridi Esfanjani, Seid Mahdi Jafari
Phenolic compounds are major micronutrients in our diet,(1) and evidence for their role in the prevention of degenerative diseases such as cancer, inflammation and neurodegenerative diseases is emerging. The easily destruction against environment stresses and low bioavailability of phenolics are main limitations of their application. Therefore, nano-encapsulated phenolics as a fine delivery system can solve their restrictions. Polymeric nanoparticles and natural nano-carriers are one of the most effective and industrial techniques which can be used for protection and delivery of phenolics...
October 1, 2016: Colloids and Surfaces. B, Biointerfaces
Masatoshi Karashima, Kouya Kimoto, Katsuhiko Yamamoto, Takashi Kojima, Yukihiro Ikeda
The aim of the present study was to develop a novel solubilization technique consisting of a nano-cocrystal suspension by integrating cocrystal and nanocrystal formulation technologies to maximize solubilization over current solubilizing technologies. Monodisperse carbamazepine-saccharin, indomethacin-saccharin, and furosemide-caffeine nano-cocrystal suspensions, as well as a furosemide-cytosine nano-salt suspension, were successfully prepared with particle sizes of less than 300nm by wet milling with the stabilizers hydroxypropyl methylcellulose and sodium dodecyl sulfate...
October 2016: European Journal of Pharmaceutics and Biopharmaceutics
Abu Zayed Md Badruddoza, P Douglas Godfrin, Allan S Myerson, Bernhardt L Trout, Patrick S Doyle
Although roughly 40% of pharmaceuticals being developed are poorly water soluble, this class of drugs lacks a formulation strategy capable of producing high loads, fast dissolution kinetics, and low energy input. In this work, a novel bottom-up approach is developed for producing and formulating nanocrystals of poorly water-soluble active pharmaceutical ingredients (APIs) using core-shell composite hydrogel beads. Organic phase nanoemulsion droplets stabilized by polyvinyl alcohol (PVA) and containing a model hydrophobic API (fenofibrate) are embedded in the alginate hydrogel matrix and subsequently act as crystallization reactors...
August 2016: Advanced Healthcare Materials
Martina Urbanova, Marketa Gajdosova, Miloš Steinhart, David Vetchy, Jiri Brus
Mucoadhesive buccal films (MBFs) provide an innovative way to facilitate the efficient site-specific delivery of active compounds while simultaneously separating the lesions from the environment of the oral cavity. The structural diversity of these complex multicomponent and mostly multiphase systems as well as an experimental strategy for their structural characterization at molecular scale with atomic resolution were demonstrated using MBFs of ciclopirox olamine (CPX) in a poly(ethylene oxide) (PEO) matrix as a case study...
May 2, 2016: Molecular Pharmaceutics
Anvar S Baimuratov, Yurii K Gun'ko, Alexander V Baranov, Anatoly V Fedorov, Ivan D Rukhlenko
Since chiral nanoparticles are much smaller than the optical wavelength, their enantiomers show little difference in the interaction with circularly polarized light. This scale mismatch makes the enhancement of enantioselectivity in optical excitation of nanoobjects a fundamental challenge in modern nanophotonics. Here we demonstrate that a strong dissymmetry of optical response from achiral nanoobjects can be achieved through their arrangement into chiral superstructures with the length scale comparable to the optical wavelength...
March 18, 2016: Scientific Reports
N Sonnenberger, N Anders, Y Golitsyn, M Steinhart, D Enke, K Saalwächter, M Beiner
DSC and NMR results prove the existence of an amorphous acetaminophen nanolayer between acetaminophen nanocrystals (form I and form III) and pore walls in controlled porous glasses. This nanolayer controls the surface energy. This finding is highly relevant for approaches towards crystal engineering in nanopores and indicates similarities to the situation during the early stages of crystallization in polymorphic bulk samples.
March 25, 2016: Chemical Communications: Chem Comm
E van Genderen, M T B Clabbers, P P Das, A Stewart, I Nederlof, K C Barentsen, Q Portillo, N S Pannu, S Nicolopoulos, T Gruene, J P Abrahams
Until recently, structure determination by transmission electron microscopy of beam-sensitive three-dimensional nanocrystals required electron diffraction tomography data collection at liquid-nitrogen temperature, in order to reduce radiation damage. Here it is shown that the novel Timepix detector combines a high dynamic range with a very high signal-to-noise ratio and single-electron sensitivity, enabling ab initio phasing of beam-sensitive organic compounds. Low-dose electron diffraction data (∼ 0.013 e(-) Å(-2) s(-1)) were collected at room temperature with the rotation method...
March 2016: Acta Crystallographica. Section A, Foundations and Advances
Ganesh Shete, Arvind Kumar Bansal
Drug nanocrystals have rapidly evolved into a mature drug delivery strategy in the last decade, with almost 16 products currently on the market. Several "top-down" technologies are available in the market for generation of nanocrystals. Despite several advantages, very few bottom-up technologies have been explored for commercial purpose. This short communication highlights a novel, bottom-up, spray drying based technology-NanoCrySP-to generate drug nanocrystals. Nanocrystals are generated in the presence of non-polymeric excipients that act as crystallization inducer for the drug...
August 2016: Drug Delivery and Translational Research
Jing Shi, Fei Guo, Aiping Zheng, Xiaoyan Zhang, Jianxu Sun
The poor water solubility of many candidate drugs remains a major obstacle to their development and clinical use, especially for oral drug delivery. Nanocrystal technology can improve the solubility and dissolution rates of many poorly water-soluble drugs very effectively, significantly improving their oral bioavailability and decreasing the food effect. For this reason, this technology is becoming a key area of drug delivery research. This review presents much of the recent progress in nanocrystal drug pharmaceuticals, including the characteristics, composition, preparation technology, and clinical applications of these drugs...
December 2015: Die Pharmazie
L M Dwyer, V K Michaelis, M O'Mahony, R G Griffin, A S Myerson
Producing stable nanocrystals confined to porous excipient media is a desirable way to increase the dissolution rate and improve the bioavailability of poorly water soluble pharmaceuticals. The poorly soluble pharmaceutical fenofibrate was crystallized in controlled pore glass (CPG) of 10 different pore sizes between 12 nm and 300 nm. High drug loadings of greater than 20 wt% were achieved across all pore sizes greater than 20 nm. Nanocrystalline fenofibrate was formed in pore sizes greater than 20 nm and showed characteristic melting point depressions following a Gibbs-Thomson relationship as well as enhanced dissolution rates...
November 7, 2015: CrystEngComm
Shalaka Dhat, Swati Pund, Chandrakant Kokare, Pankaj Sharma, Birendra Shrivastava
The designing of surface engineered nanocrystals for improved stability and bioavailability is a multivariate process depending on several critical formulation and process variables. The present investigation deals with formulation of stable nanocrystals of poorly soluble satranidazole (SAT) for improving dissolution rate and pharmacokinetic profiling. SAT has low polar surface area, high dose and dosing frequency. Based on goniometric and stability studies of formulations prepared with various stabilizers, a unique combination of Span 20 and HPMC E-5 was selected for detailed investigation...
March 2016: European Journal of Pharmaceutics and Biopharmaceutics
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