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Pharmaceutical nanocrystals

Sonia Iurian, Cătălina Bogdan, Ioan Tomuță, Piroska Szabó-Révész, Anita Chvatal, Sorin E Leucuța, Mirela Moldovan, Rita Ambrus
The aim of this study was to develop oral lyophilisates with improved meloxicam (MEL) dissolution, optimizing each step of the preparation by design of experiments. First, meloxicam nanosuspensions were prepared by high-pressure homogenization (HPH), using PVP, Poloxamer or PEG as stabilizers and were subjected to freeze-drying using mannitol as cryoprotectant. The effects of the stabilizers and cryoprotectant were assessed and an optimal formulation was generated within the Design Space where the particle sizes and the PDIs are at their lowest values...
April 20, 2017: European Journal of Pharmaceutical Sciences
Mei-Ling Chen, Mathew John, Sau L Lee, Katherine M Tyner
Nanocrystal technology has emerged as a valuable tool for facilitating the delivery of poorly water-soluble active pharmaceutical ingredients (APIs) and enhancing API bioavailability. To date, the US Food and Drug Administration (FDA) has received over 80 applications for drug products containing nanocrystals. These products can be delivered by different routes of administration and are used in a variety of therapeutic areas. To aid in identifying key developmental considerations for these products, a retrospective analysis was performed on the submissions received by the FDA to date...
March 9, 2017: AAPS Journal
Conor Parks, Andy Koswara, Hsien-Hsin Tung, Nandkishor K Nere, Shailendra Bordawekar, Zoltan K Nagy, Doraiswami Ramkrishna
Nanocrystals are receiving increased attention for pharmaceutical applications due to their enhanced solubility relative to their micron-sized counterpart and, in turn, potentially increased bioavailability. In this work, a computational method is proposed to predict the following: (1) polymorph specific dissolution kinetics and (2) the multiplicative increase in the polymorph specific nanocrystal solubility relative to the bulk solubility. The method uses a combination of molecular dynamics and a parametric particle size dependent mass transfer model...
April 3, 2017: Molecular Pharmaceutics
Lingnan Wang, Zhenbang Liu, Dandan Wang, Shuang Ni, Dongxue Han, Wei Wang, Li Niu
Along with continuous growing widespread adulterations of botanical drugs, the necessity for drug quality monitoring has become more popular than ever. Considering that antioxidants are widely found in natural plant pharmaceuticals, gallic acid (GA) is often regarded as the reference standard to make sure whether these are up to grade as guided by Chinese Pharmacopeia. Herein, a novel Bi2MoO6/Bi2S3 photoelectrochemical sensor has been successfully involved toward selective GA analysis to supervise drug quality, in which γ-Bi2MoO6 nanobelts were treated as template nanocrystal and scaffold...
February 27, 2017: Biosensors & Bioelectronics
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...
February 2, 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
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