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Andrew J Clulow, Malinda Salim, Adrian Hawley, Elliot P Gilbert, Ben Boyd
Efforts to develop orally-administered drugs tend to place an exceptional focus on aqueous solubility as this is an essential criterion for their absorption in the gastro-intestinal tract. In this work we examine the solid state behaviour and solubility of OZ439, a promising single-dose cure for malaria being developed as the highly water-soluble mesylate salt. The aqueous phase behaviour of the OZ439 mesylate salt was determined using a combination of small angle neutron and X-ray scattering (SANS and SAXS, respectively)...
March 20, 2018: Molecular Pharmaceutics
Hyon-Min Song, Jeffrey I Zink
Seedless synthesis of Pd nanorods and their self-assembly into the layered smectic ordering is described. Aqueous Pluronic triblock copolymers (14.3% - 35.7%) are used as a soft template along with cetyltrimethylammonium bromide (CTAB) for inducing one-dimensional growth of Pd nanorods. Pluronic triblock copolymers are probably the most used polymer surfactants, and they are composed of PEO(polyethylene oxide)-PPO(polypropylene oxide)-PEO triblocks. Neither pH adjustment, nor AgNO3, nor other additives such as polyvinyl pyrolidone, and ethylene glycol are required to obtain Pd nanorods...
March 20, 2018: Langmuir: the ACS Journal of Surfaces and Colloids
Kuldeep K Bansal, Jitendra Gupta, Ari Rosling, Jessica M Rosenholm
Polymers from natural resources are attracting much attention in various fields including drug delivery as green alternatives to fossil fuel based polymers. In this quest, novel block copolymers based on renewable poly(δ-decalactone) (PDL) were evaluated for their drug delivery capabilities and compared with a fossil fuel based polymer i.e. methoxy-poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-b-PCL). Using curcumin as a hydrophobic drug model, micelles of PDL block copolymers with different orientation i...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Xue Liu, Yanxiang Wang, Peng Yun, Xin Shen, Feng Su, Yangsheng Chen, Suming Li, Danqing Song
Polylactide-poly(ethylene glycol) (PLA-PEG) block copolymers were synthesized by ring opening polymerization of l-lactide using a monomethoxy PEG (mPEG) as macroinitiator and zinc lactate as catalyst. The resulting diblock copolymers were characterized by1 H NMR and GPC. Polymeric micelles were prepared by self-assembly of copolymers in distilled water using co-solvent evaporation or membrane hydration methods. The resulting micelles are worm-like in shape as shown by TEM measurements. A hydrophobic anticancer drug, cycloprotoberberine derivative A35, was successfully loaded in PLA-PEG filomicelles with high encapsulation efficiency (above 88%)...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Ganesh R Kokil, Rakesh N Veedu, Bao Tri Le, Grant A Ramm, Harendra S Parekh
Despite advancements in the development of high generation cationic-dendrimer systems for delivery of nucleic acid-based therapeutics, commercially available chemical agents suffer from major drawbacks such as cytotoxicity while being laborious and costly to synthesize. To overcome the aforementioned limitations, low-generation cationic peptide asymmetric dendrimers with side arm lipid (cholic and decanoic acid) conjugation were designed, synthesized and systematically screened for their ability to self-assemble into micelles using dynamic light scattering...
March 19, 2018: Scientific Reports
Ka Yee Wan, Ka Wai Wong, Albert Hee Lum Chow, Shing Fung Chow
Flash nanoprecipitation (FNP) is a controlled antisolvent precipitation process that has proven effective for consistent production of drug nanoparticles with a defined mean particle size and narrow particle size distribution. However, physical instability of the generated nanoparticles remains a major challenge in the application of this technology in pharmaceutical formulation. Aimed at resolving this problem, the present study has investigated the FNP process and associated stabilization mechanism of itraconazole (ITZ) nanoparticles through in-depth nanoparticle characterization...
March 16, 2018: International Journal of Pharmaceutics
Micelle Haydel
No abstract text is available yet for this article.
March 20, 2018: Annals of Internal Medicine
Vijay Patel, Debes Ray, Anita Bahadur, Junhe Ma, V K Aswal, Pratap Bahadur
The present study was aimed to examine the interaction of two bile salts viz. sodium cholate (NaC) and sodium deoxycholate (NaDC) with three ethylene polyoxide-polypropylene polyoxide (PEO-PPO-PEO) triblock copolymers with similar PPO but varying PEO micelles with a focus on the effect of pH on mixed micelles. Mixed micelles of moderately hydrophobic Pluronic® P123 were examined in the presence of two bile salts and compared with those from very hydrophobic L121 and very hydrophilic F127. Both the bile salts increase the cloud point (CP) of copolymer solution and decreased apparent micelle hydrodynamic diameter (Dh )...
March 2, 2018: Colloids and Surfaces. B, Biointerfaces
Satyajit Mondal, Bijan Das
The interactions of a protein cytochrome c with some selected conventional and ionic liquid surfactants have been investigated at pH7.4 using ultraviolet-visible and fluorescence spectroscopic techniques. We used four conventional surfactants - cetyltrimethylammonium bromide (CTAB), dodecyltrimethylammonium bromide (DTAB), sodium N-dodecanoylsarcosinate (SDDS), and N-decanoyl-N-methylglucamine (Mega 10), and a surface active ionic liquid 1-hexadecyl-3-methylimidazolium chloride (C16 MeImCl). All the investigated surfactants were found to induce an unfolding of the protein cytochrome c...
March 12, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Zheng-Rong Lu, Peter Qiao
The treatment of malignancies has undergone dramatic changes in the past few decades. Advances in drug delivery techniques and nanotechnology have allowed for new formulations of old drugs, so as to improve the pharmacokinetics, to enhance accumulation in solid tumors, and to reduce the significant toxic effects of these important therapeutic agents. Here, we review the published clinical data in cancer therapy of several major drug delivery systems, including targeted radionuclide therapy, antibody drug conjugates, liposomes, polymer drug conjugates, polymer implants, micelles, and nanoparticles...
March 19, 2018: Molecular Pharmaceutics
Xinyi Ding, Yuxiang Sun, Yanming Chen, Wanchuan Ding, Steven Emory, Tianhao Li, Zixing Xu, Ning Han, Jun Wang, Gang Ruan
Micellar nanocrystals (micelles with encapsulated nanocrystals) have become an emerging major class of nanobiomaterials. We describe a method of fabricating micellar nanocrystals based on combining top-down electrospray, bottom-up self-assembly, and solvent-based structure control. This method involves first using electrospray to generate uniform ultrafine liquid droplets, each of which functions as a micro-reactor in which self-assembly reaction occurs forming micellar nanocrystals, with the structures (micelle shape and nanocrystal encapsulation) controlled by the organic solvent used...
February 11, 2018: Journal of Visualized Experiments: JoVE
Ying Li, Li-Fang Wang, Jin-Ling Wang, Peng-Fei Tu
This study aimed to prepare andrographolide (AP)-loaded glycyrrhizic acid (GA) micelles (AP-GA)-PMs to enhance the solubility and anti-tumor effect of andrographolide. Firstly, andrographolide (AP) was used as the model drug and glycyrrhizic acid (GA) as carriers to prepare (AP-GA)-PMs. Then the preparation methods and the ratios of drug and carrier were screened and optimized based on particle size, encapsulation efficiency (EE) and loading capacity of micelles. Finally, the pharmaceutical characters and the inhibition rate on HepG2 cells were evaluated on the (AP-GA)-PMs prepared by optimal process...
January 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Wen Chen, Jyoti Dev, Julija Mezhyrova, Liqiang Pan, Alessandro Piai, James J Chou
The p7 protein of the hepatitis C virus (HCV) can oligomerize in membrane to form cation channels. Previous studies showed that the channel assembly in detergent micelles adopts a unique flower-shaped oligomer, but the unusual architecture also presented problems for understanding how this viroporin resides in the membrane. Moreover, the oligomeric state of p7 remains controversial, as both hexamer and heptamer have been proposed. Here we address the above issues using p7 reconstituted in bicelles that mimic a lipid bilayer...
February 27, 2018: Structure
Tingsheng Yan, Jinju Cheng, Zongjun Liu, Feng Cheng, Xinjing Wei, Yudong Huang, Jinmei He
Liver cancer is one of the top death causing cancers, traditional treatments have not settled for the requirement of patients. In this work, a smart acid-responsive micelle based on glycyrrhetinic acid modified chitosan-polyethyleneimine-4-Hydrazinobenzoic acid-doxorubicin (GA-CS-PEI-HBA-DOX) was synthesized for targeted delivery of DOX to liver cancer. A dual pH-sensitive and receptor-mediated strategy has been exploited to enhance the delivery efficiency. The micelle possesses positive charges under pH 6...
June 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Kehu Zhang, Jiangtao Liu, Yinzhou Guo, Yan Li, Xiao Ma, Zhongli Lei
Herein, we prepared a novel quintuple-stimuli-responsive shell-crosslinked (SCL) nanocontainer in respond to temperature, pH, light, and oxidation or reduction species. The well-defined amphiphilic diblock copolymer poly(2-methacryloyloxyethyl ferrocenecarboxylate)-(5-propargylether-2-nitrobenzyl bromoisobutyrate)-poly(dimethylaminoethyl methacrylate) (PMAEFc-ONB-PDMAEMA) was synthesized via atom transfer radical polymerization (ATRP) and click chemistry. The diblock copolymer self-assembled into spherical micelles with a uniform size in aqueous media as non-crosslinked (NCL) micelles, and then the micelles were crosslinked by N,N'-bis(bromoacetyl) cystamine (BBAC) through quaternization reaction between the nitrogen of DMAEMA and the bromine of BBAC to receive the SCL micelles which shrunk at higher temperature, swelled at acidic pH or a low concentration of hydrogen peroxide (H2 O2 ), decrosslinked by a small amount of DL-dithiothreitol (DTT), and were disrupted with DTT and UV light...
June 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Weibing Dong, Ziang Liu, Liying Sun, Cui Wang, Yue Guan, Xiaoman Mao, Dejing Shang
The threshold hydrophobicity and amphipathic structure of the peptidic chain are important for the biological function of antimicrobial peptides. Chensinin-1b exhibits broad-spectrum bactericidal activity with no hemolytic activity but has almost no anticancer ability against the selected cancer cell lines. In this study, the conjugation of aliphatic acid was designed with different lengths of N-terminal of chensinin-1b, the antimicrobial activity of the resulting lipo-chensinin-1b was examined, in which OA-C1b showed much stronger activity than those of cheninin-1b and the other two lipopeptides...
March 10, 2018: European Journal of Medicinal Chemistry
Chunyan Chen, Ni Sun, Dongsheng Li, Sihua Long, Xiaoyu Tang, Guoqing Xiao, Linyuan Wang
Kitchen waste oil (KWO) from catering industries or households was used as a low-cost carbon source for producing biosurfactants by self-isolated Pseudomonas aeruginosa. Fermentation performance with KWO was superior to those with four other carbon sources, with higher optical density (OD600 ) of 2.33 and lower interfacial tension of 0.57 mN/m. Culture conditions for biosurfactant production were optimized, with optimal pH of 8.0 and nitrogen source concentration of 2.0 g/L, respectively. The results of infrared spectroscopy and liquid chromatography-mass spectrometry (LC-MS) showed that the biosurfactant was a mixture of six rhamnolipid congeners, among which Rha-Rha-C10 -C10 and Rha-C10 -C10 were the main components, with mass fraction of approximately 34...
March 16, 2018: Environmental Science and Pollution Research International
Stefan A Boers, Saskia D Hiltemann, Andrew P Stubbs, Ruud Jansen, John P Hays
Microbiota profiling has the potential to greatly impact on routine clinical diagnostics by detecting DNA derived from live, fastidious, and dead bacterial cells present within clinical samples. Such results could potentially be used to benefit patients by influencing antibiotic prescribing practices or to generate new classical-based diagnostic methods, e.g., culture or PCR. However, technical flaws in 16S rRNA gene next-generation sequencing (NGS) protocols, together with the requirement for access to bioinformatics, currently hinder the introduction of microbiota analysis into clinical diagnostics...
March 16, 2018: European Journal of Clinical Microbiology & Infectious Diseases
P R G Fernandes, J N Maki, L B Gonçalves, B F de Oliveira, H Mukai
In this work, the frequency dependence of the known mechano-optical effect which occurs in the micellar isotropic phases (I) of mixtures of potassium laurate (KL), decanol (DeOH), and water is investigated in the range from 200mHz to 200Hz. In order to fit the experimental data, a model of superimposed damped harmonic oscillators is proposed. In this phenomenological approach, the micelles (microscopic oscillators) interact very weakly with their neighbors. Due to shape anisotropy of the basic structures, each oscillator i (i=1,2,3,...
February 2018: Physical Review. E
Tadashi Sugahara, Yuichiro Takamatsu, Avinash Bhadani, Masaaki Akamatsu, Kenichi Sakai, Masahiko Abe, Hideki Sakai
In this study, we synthesize a novel oleic acid-based gemini surfactant with carboxylate headgroups, and study the effect of stereochemistry (anti- vs. syn-) on self-aggregation properties in water. We investigate these properties using phase diagrams, static surface tension, and one-dimensional and two-dimensional nuclear magnetic resonance (NMR) measurements. We find that a phase transition from a hexagonal liquid crystal (H1) phase to a lamellar liquid crystal (Lα) phase occurs at a lower surfactant concentration in the syn form, when compared with the anti form...
March 16, 2018: Physical Chemistry Chemical Physics: PCCP
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