Search

Myo-inositol and its derivatives have been extensively used in the pharmaceutics, cosmetics, and food and feed industries. In recent years, compared with traditional chemical acid hydrolysis, biological methods have been taken as viable and cost-effective ways to myo-inositol production from cheap raw materials. In this review, we provide a thorough overview of the development, progress, current status, and future direction of myo-inositol production (e.g., chemical acid hydrolysis, microbial fermentation, and in vitro enzymatic biocatalysis). The chemical acid hydrolysis of phytate suffers from serious phosphorous pollution and intricate product separation, resulting in myo-inositol production at a high cost. For microbial fermentation, creative strategies have been provided for the efficient myo-inositol biosynthesis by synergetic utilization of glucose and glycerol in Escherichia coli. in vitro cascade enzymatic biocatalysis is a multienzymatic transformation of various substrates to myo-inositol. Here, the different in vitro pathways design, the source of selected enzymes, and the catalytic condition optimization have been summarized and analyzed. Also, we discuss some important existing challenges and suggest several viewpoints. The development of in vitro enzymatic biosystems featuring low cost, high volumetric productivity, flexible compatibility, and great robustness could be one of the promising strategies for future myo-inositol industrial biomanufacturing.

The aim of this study was to develop a fast and an efficient method to determine the Hydrophile-Lipophile Balance (HLB) number of cosmetic and pharmaceutics surfactants.This method is based on the deviation of the phase inversion temperature induced by the addition of the test compound, with respect to the phase inversion temperature of a reference system, which includes an ethoxylated surfactant. This method is called PIT-deviation.Three calibration curves are set up with three reference ethoxylated surfactants. These calibration curves make it possible to evaluate the interfacial behaviour of certain chemicals. More particularly, these curves make it possible to easily determine the surfactant HLB.In this study, a fast and accurate method has been developed to determine the hydrophilic-lipophilic balance (HLB) number of amphiphilic chemicals. This new method can be applied to establish an HLB number of all commercial amphiphilic ingredients. Compounds which have a PIT-deviation close to zero are also discussed.Le but de cette étude était de développer une méthode rapide et efficace pour déterminer le nombre Hydrophiles-Lipophiles Balance (HLB) d'agents tensioactifs cosmétiques et pharmaceutiques. MÉTHODES: Cette méthode est basée sur le déplacement de la température d'inversion de phase induite par l'addition du composé à tester par rapport à la température d'inversion de phase d'un système de référence, comprenant un tensioactif éthoxylé. Cette méthode s'appelle PIT-déviation. RÉSULTATS: Trois courbes d'étalonnage sont établies avec trois tensioactifs éthoxylés de référence. Ces courbes d'étalonnage permettent d'évaluer le comportement interfacial de certains produits chimiques. Plus particulièrement, ces courbes permettent de déterminer facilement le HLB de tensioactif.Dans cette étude, une méthode rapide et précise a été développée pour déterminer le Hydrophile-Lipophile Balance (HLB) de produits chimiques amphiphiles. Cette nouvelle méthode peut être appliquée pour établir un HLB de tous les ingrédients amphiphiles. Les composés dont la PIT-deviation est proche de zéro sont également abordés.

5-Lipoxygenase converts arachidonic acid into leukotrienes, which are involved in inflammation and angiogenesis. The introduction of carboranes can improve the pharmacokinetic behavior of metabolically less stable pharmaceutics. Herein we report the syntheses of several carborane-based inhibitors of the 5-lipoxygenase pathway. The isosteric replacement of phenyl rings by carboranes leads to improved cytotoxicity toward several melanoma and colon cancer cell lines. For the colon cancer cell line HCT116, the co-inhibition of heat shock protein 90 was observed.

Background: Dual‐release mechanism of ethosomal gels (ie, ethosomes and gel) makes them as versatile drug delivery systems for topical applications. Clove oil is obtained from the clove buds exhibited broad antifungal and antibacterial activity. Cutaneous candidiasis is the infection caused by Candida albicans or other Candida species. Aim: The aim of the present study was to prepare ethosomal gel of clove oil and evaluate its effectiveness in the treatment of cutaneous candidiasis. Methods: Ethosomes of clove oil was formulated by using varying concentrations of soyaphosphotidyl choline and ethanol, and later, it was incorporated into carbapol 974 base gels to form ethosomal gel. The prepared ethosomal gels were also evaluated for spreadability, drug release studies, ex vivo permeation study, and antifungal activity. Results: The optimized formulation did not cause any irritation to the skin since the pH of formulation was in the pH range of skin. The ethosomal gel showed satisfactory antifungal activity against the fungus C. albicans compared to pure clove oil. Conclusions: The results showed that developed formulation could be promising one in the topical delivery of clove oil for the treatment of cutaneous candidiasis.

Sarıoğlu, Nurhan (Balikesir Author), In this study, we investigated the effects of certain respiratory drugs, which are mainly used on human serum paraoxonase-1 (hPON1; EC 3.1.8.1). hPON1 was purified from human serum, with 354.91 fold and 45% yield by using two simple step procedures including, first, ammonium sulfate precipitation, then, Sepharose-4B-l-tyrosine-1-naphthylamine hydrophobic interaction chromatography. SDS-polyacrylamide gel electrophoresis showed a single protein band belonging to hPON1 with 43 kDa. All the pharmaceutical compounds inhibited the PON1 enzyme highly at the micromolar level. The obtained IC50 values for nine different pharmaceutics ranged from 0.219 mu M (salbutamol sulfate) to 67.205 mu M (montelukast sodium). So, all drugs could be considered as potent hPON1 inhibitors. K-i values and inhibition types were determined by Lineweaver-Burk graphs. While varenicline tartrate and moxifloxacin hydrochloride inhibited the enzyme in a noncompetitive manner, others inhibited it in a mixed manner.

With the outbreak of new respiratory viruses and high mortality rates of pulmonary diseases, physiologically relevant models of human respiratory system are urgently needed to study disease pathogenesis, drug efficacy, and pharmaceutics. In this paper, a 3D alveolar barrier model fabricated by printing four human alveolar cell lines, namely, type I and II alveolar cells (NCI‐H1703 and NCI‐H441), lung fibroblasts (MRC5), and lung microvascular endothelial cells (HULEC‐5a) is presented. Automated high‐resolution deposition of alveolar cells by drop‐on‐demand inkjet printing enables to fabricate a three‐layered alveolar barrier model with an unprecedented thickness of ≈10 µm. The results show that the 3D structured model better recapitulate the structure, morphologies, and functions of the lung tissue, compared not only to a conventional 2D cell culture model, as expected, but also a 3D non‐structured model of a homogeneous mixture of the alveolar cells and collagen. Finally, it is demonstrated that this thin multilayered model reproduce practical tissue‐level responses to influenza infection. Drop‐on‐demand inkjet‐printing is an enabling technology for customization, scalable manufacturing, and standardization of their size and growth, and it is believed that this 3D alveolar barrier model can be used as an alternative to traditional test models for pathological and pharmaceutical applications., The morphological, functional, and microenvironmental features of human alveolar barrier tissue are recapitulated by providing uniform and continuous cell–cell contact sites and cell–matrix interaction in a carefully controlled 3D microarchitecture. To this end, high‐resolution inkjet bioprinting was used to reconstitute four essential alveolar cell types in 3D multilayered architecture. This model reproduced practical tissue‐level responses to influenza infection.

Glioblastoma is the most common lethal malignant intracranial tumor with a low 5-year survival rate. Currently, the maximal safe surgical resection, followed by high-dose radiotherapy (RT), is a standard treatment for glioblastoma. However, high-dose radiation to the brain is associated with brain injury and results in a high fatality rate. Here, integrated pharmaceutics (named D-iGSNPs) composed of gold sub-nanometer particles (GSNPs), blood-brain barrier (BBB) penetration peptide iRGD, and cell cycle regulator α-difluoromethylornithine is designed. In both simulated BBB and orthotopic murine GL261 glioblastoma models, D-iGSNPs are proved to have a beneficial effect on the BBB penetration and tumor targeting. Meanwhile, data from cell and animal experiments reveal that D-iGSNPs are able to sensitize RT. More importantly, the synergy of D-iGSNPs with low-dose RT can exhibit an almost equal therapeutic effect with that of high-dose RT. This study demonstrates the therapeutic advantages of D-iGSNPs in boosting RT, and may provide a facile approach to update the current treatment of glioblastoma.

A study of the ZnO nanowire array photocatalysis performance has been carried out under UV radiation for the degradation of the toxic organic compounds such as methylene blue (MB), methyl orange (MO), and acid red 14 (AR14) dyes, which are commonly used in textile and pharmaceutics industries. UV–Vis spectrometry has been used to follow the dye degradation characterization. The degradation mechanism has been proposed for each dye, which will give a reasonable explanation about different degradation degree under same experimental conditions. MB and AR14 showed a better degradation performance than MO.

This review article deals with latest literature studies on the potential use of polymer ultrathin and nanosized structures obtained by electrospinning to design novel engineered materials with bioactive properties. The electrofluidodynamic process offers the option to form high-performance bioactive systems based on polymer yarns of nanofibers or coatings of nanobeads with high surface-to-volume ratios. The electrospun and electrosprayed nanostructures can be further functionalized by encapsulation with bioactive fillers and substances. For both scenarios, the resultant polymer nanostructures present unique bioactive properties capable of providing a beneficial impact over human's health and with improved and advanced performance for biomedicine, pharmaceutics, nutrition, bioengineering, and healthcare applications. These novel functional materials attained by the electrospinning technology can be of interest for many bioactive applications such as functional food design, food packaging, functional coatings, controlled delivery of drug solutions and, mainly, tissue engineering. This article is purposely designed to gather, for the first time, most recent and promising multi- and inter-disciplinary developments based on electrospun systems for bioactive applications, which are either bioactive material concepts or can be advantageously applied to become such. POLYM. ENG. SCI., 56:500–527, 2016. © 2016 Society of Plastics Engineers

Ionic liquids (ILs), a class of materials with unique physicochemical properties, have been used extensively in the fields of chemical engineering, biotechnology, material sciences, pharmaceutics, and many others. Because ILs are very polar by nature, they can migrate into the environment with the possibility of inclusion in the food chain and bioaccumulation in living organisms. However, the chemical natures of ILs are not quintessentially biocompatible. Therefore, the practical uses of ILs must be preceded by suitable toxicological assessments. Among different methods, the use of microorganisms to evaluate IL toxicity provides many advantages including short generation time, rapid growth, and environmental and industrial relevance. This article reviews the recent research progress on the toxicological properties of ILs toward microorganisms and highlights the computational prediction of various toxicity models.

The file attached to this record is the author's final peer reviewed version. The engineering of advanced healthcare materials provides a platform to address challenges facing interdisciplinary scientists, clinicians, pharmacists, biomaterial scientists and biomedical engineers. Niche and timely developments arising from the synthesis or extraction of more biocompatible materials, new biologically active components, clearer insights into disease mechanisms and novel therapies or strategies provide several timely opportunities. These include enhanced therapies with greater patient compliance, improved disease targeting, better diagnosis and bespoke medications for individuals. Electrohydrodynamic atomisation (EHDA) engineering comprises several processes making use of electric fields (e.g. through an applied voltage) interplaying with several forces (e.g. gravity and surface tension). Coupled to advanced materials (e.g. formulated media) and specifically configured apparatuses (e.g. nozzles, collectors and downstream processes); effective and controlled fabrication of various structures (fibers, particles, bubbles, grids, droplets) on various scales (macro, micro and nano) possessing various dimensions (2D, 3D and 4D) is readily achieved. The processes have distinct advantages compared to established engineering methods (ambient environment engineering, low shear, scalability, compartmentalisation etc.). This detailed review focuses on key concepts and developments in EHDA engineering pertaining to underlying principles, enabling tools and engineered structures specifically for healthcare remits. From initial experiments involving the behaviour of non-formulated liquids on charged amber to recent developments in complex 3D matrix printing; the EHDA route has progressed significantly, most rapidly in the last two decades, and is capable of providing timely platform opportunities to tackle several global healthcare challenges

Resveratrol and its derivatives are a class of polyphenolic compounds recognized for their outstanding biological properties based on clinical trials. In addition, their possible uses in nutraceutics, cosmetics, and as pharmaceutics create a need for large-scale production with the possibility to use sustainable sources. In this review, we report on the biotechnological production of resveratrol and some of its derivatives through plant cell suspensions, such as grapevine cell culture systems. These cultures usually need elicitation. Methyljasmonate, cyclodextrins, the combination of both and chitosan are the elicitors leading to the best responses in terms of resveratrol amounts produced in flasks. Production performances of resveratrol can be optimized in flasks for scale-up in large culture volumes. We summarize the plant cell culture systems used for resveratrol bioproduction and transfer experiments from flasks to bioreactors as well as elicitor-mediated upregulation of the defense genes in those plant culture systems.

Scheme 1. Diterpenoid alkaloid lappaconine and preparation of lappaconine derivatives.[a] State Key Laboratory of Fine ChemicalsSchool of Pharmaceutical Science and TechnologyDalian University of TechnologyNo. 2 Linggong Road, Ganjingzi District, Dalian, LiaoningProvince 116012, P. R. ChinaE-mail: mengqw@dlut.edu.cnhttp://ceb.dlut.edu.cn/index.html[b] Department of Pharmaceutics, Daqing CampusHarbin Medical UniversityNo. 1 Xinyang Road, Gaoxin District, Daqing, HeilongjiangProvince 163319, P. R. ChinaSupporting information for this article is available on theWWW under http://dx.doi.org/10.1002/ejoc.201402019.

The design and development of multifunctional polymer capsules with controlled chemical composition and physical properties has been the focus of academic and industrial research in recent years. Especially in the biomedical field, the formulation of novel polymer-based encapsulation systems for the early-stage disease diagnostic and effective delivery of bioactive agents represent one of the most rapidly advancing areas of science. The stimuli-responsive release of cargo molecules from the carrier gains remarkable attention for in vitro and in vivo delivery of contrast agents, genes, and pharmaceutics. In this Review, the current status and the challenges of different polymer-based micro- and nanocapsule formulations are considered, emphasizing on their potential biological application as carriers for specific drug targeting and controlled release upon applying of external stimulus.

Significant efforts have been invested in finding a delivery system that can encapsulate and deliver therapeutics. Core-shell polymer-lipid hybrid nanoparticles have been studied as a promising platform because of their mechanical stability, narrow size distribution, biocompatibility, and ability to co-deliver diverse drugs. Here, novel core-shell nanoparticles based on a poly(lactic-co-glycolic acid) (PLGA) core and multilamellar lipid shell are designed, where the lipid bilayers are crosslinked between the two adjacent bilayers (PLGA-ICMVs). The cross-platform performance of the nanoparticles to other polymer-lipid hybrid platforms is examined, including physicochemical characteristics, ability to encapsulate a variety of therapeutics, biocompatibility, and functionality as a vaccine delivery platform. Differential abilities of nanoparticle systems to encapsulate distinct pharmaceutics are observed, which suggest careful consideration of the platform chosen depending on the therapeutic agent and desired function. The novel PLGA-ICMV platform herein demonstrates great potential in stably encapsulating water-soluble agents and therefore is an attractive platform for therapeutic delivery.

In the last decade, the application of monolithic materials has rapidly expanded to the realization of flow-through bioconversion processes. Up to these days, different classes of enzymes such as hydrolases, lyases, and oxidoreductases have been immobilized on organic, inorganic, or hybrid monolithic materials to prepare the effective flow-through enzymes reactors for application in proteomics, biotechnology, pharmaceutics, organic synthesis, and biosensoring. Current review describes the results of kinetic study and specialties of flow-through immobilized enzyme reactors based on the existing monolithic materials.

Argan oil is well known for its nutraceutical properties. Its specific fatty acid composition and antioxidant content contribute to the stability of the oil and to its dietetic and culinary values. There is an increasing interest to use argan oil in cosmetics, pharmaceutics, and food products. However, the formulation of highly stable emulsions with prolonged shelf life is needed. In this study, argan oil-in-water (O/W) emulsions were prepared using microchannel (MC) emulsification process, stabilized by different non-ionic emulsifiers. The effects of processing temperature on droplet size and size distribution were studied. Physical stability of argan O/W emulsions was also investigated by accelerated stability testing and during storage at room temperature (25 ± 2°C). Highly monodisperse argan O/W emulsions were produced at temperatures up to 70°C. The obtained emulsions were physically stable for several months at room temperature. Furthermore, emulsifier type, concentration, and temperature were the major determinants influencing the droplet size and size distribution. The results indicated that a suitable emulsifier should be selected by experimentation, since the interfacial tension and hydrophilic–lipophilic balance values were not suitable to predict the emulsifying efficiency. Practical applications: MC emulsification produces efficiently monodisperse droplets at wide range of temperatures. The findings of this work may be of great interest for both scientific and industrial purposes since highly stable and monodisperse argan oil-in-water emulsions were produced which can be incorporated into food, cosmetic, or pharmaceutical formulations.

Here we evaluate poly(2-ethyl-2-oxazoline)s (PEtOx) as a matrix excipient for the production of oral solid dosage forms by hot melt extrusion (HME) followed by injection molding (IM). Using metoprolol tartrate as a good water-soluble model drug we demonstrate that drug release can be delayed by HME/IM, with the release rate controlled by the molecular weight of the PEtOx. Using fenofibrate as a lipophilic model drug we demonstrate that relative to the pure drug the dissolution rate is strongly enhanced by formulation in HME/IM tablets. For both drug molecules we find that solid solutions, i.e. molecularly dissolved drug in a polymeric matrix, are obtained by HME/IM.

Stimuli-responsive hydrogels are extensively investigated to implement new biomedical and pharmaceutical approaches. In this work, novel pH-sensitive semi-interpenetrating polymer network (semi-IPN) hydrogels based on starch and poly(aspartic acid) (PAsp) with potential applicability in the field of pharmaceutics were prepared and characterized. The goal was to obtain a colon specific drug delivery system and to exploit the pH-sensitive behavior of the hydrogels. The obtained hydrogels were characterized by FTIR, thermogravimetric analysis (TGA), DSC, and SEM. The swelling behavior of the hydrogels with a suitable ratio of starch and poly(aspartic acid) was investigated in gastrointestinal simulated conditions. Moreover, the drug release studies were carried out using 5-Flurouracil as a model of anticancer drug in enzyme free simulated gastrointestinal conditions and simulated intestinal conditions containing α-amylase, respectively. The obtained hydrogels, due to their excellent pH-sensitive release property, could be potentially used as drug delivery systems for the oral treatment of colonic cancer.

Poly(D,L-lactic acid) (PLA) has been widely used in pharmaceutics and medicine. Low molecular weight (LMW) PLA is especially useful for rapidly degrading biomaterials such as those used for short-duration drug delivery systems. There is scant information available in the literature regarding the purification and analysis of LMW PLA. In this paper we report (1) a convenient and effective polymer purification/fractionation technique to produce LMW PLA with narrow molecular weight distribution (MWD) and (2) analyses that were used to characterize the molecular weight and MWD of these polymers. A novel, convenient and effective temperature-induced solution-phase separation method was developed to produce narrow MWD, LMW (600–2000 g mol−1) PLA. Molecular weights determined using gel permeation chromatography (GPC) with universal calibration, unlike those determined with the commonly used conventional calibration, showed good agreement with those obtained using several independent direct techniques. The phase separation induced by temperature reduction of a polymer in a single solvent system provided a simple and effective technique to produce narrow MWD, LMW PLA polymers. Additional advantages of this technique are: (1) only one solvent is required; (2) the risk of local complete solid polymer precipitation is eliminated; (3) it is reversible and not dependent on the rate of cooling; and (4) use of chlorinated solvents is avoided. This technology may open up a new opportunity for manufacturing LMW polymers with narrow MWD. We also found that GPC with universal calibration is a more accurate method than GPC with the commonly used conventional calibration for characterizing these polymers, and is straightforward to use especially now that on-line viscosity detectors are widely available. Copyright © 2010 Society of Chemical Industry

Hydrogel particles are versatile materials that provide exquisite, tunable control over the sequestration and delivery of materials in pharmaceutics, tissue engineering, and photonics. The favorable properties of hydrogel particles depend largely on their size, and particles ranging from nanometers to micrometers are used in different applications. Previous studies have only successfully fabricated these particles in one specific size regime and required a variety of materials and fabrication methods. We have developed a simple yet powerful system to easily tune the size of polypeptide-based, thermoresponsive hydrogel particles, from the nano to microscale, using a single starting material. We take advantage of the self-assembly and unique phase transition behavior of elastin-like polypeptides (ELPs) in bulk and within microfluidic-generated droplets to control particle size. These particles are then stabilized through ultraviolet irradiation of a photocrosslinkable unnatural amino acid (UAA) cotranslationally incorporated into the parent polypeptide. The thermoresponsive property of these particles provides an active mechanism for actuation and a dynamic responsive to the environment. This work represents a fundamental advance in the generation of crosslinked biomaterials, especially in the form of soft matter colloids, and is the one of the first demonstrations of successful use of UAAs in generating a novel material.

BACKGROUND: There is much interest in the recognition and determination the two ofloxacin enantiomers, not only from the point of view of investigating the pharmacokinetics of the enantiomers in vitro but also in the design and development of new chiral pharmaceutics. RESULTS: Chiral separation was performed on a C18 column, in which the mobile phase consisted of a methanol–water solution (containing different concentrations of L-phenylalanine and copper sulfate) and its flow rate was set at 0.7 mL min−1. The effect of different kinds and concentration of ligands, bivalent copper ion, organic modifier, ionic liquid modifier, pH of mobile phase, and temperature on enantioseparation were evaluated and the results show that the enantioselectivity was strongly affected by the pH and ligand concentration of the mobile phase. Under optimal conditions, baseline separation of the two enantiomers was obtained with a resolution of 4.69 in less than 40 min. CONCLUSION: The mechanism of chiral discrimination is based on the stabilities of the copper(II) binary complexes and their ternary diastereomeric complexes with amino acids formed in solution and stationary phase. The proposed method could be used for the quality evaluation of ofloxacin enantiomers. Copyright © 2009 Society of Chemical Industry

Novel hydrophilic-hydrophilic block copolymer with one block containing β-cyclodextrin was synthesized. Core-shell structured nano-assemblies with chemical sensitivity could be constructed by this copolymer in the presence of hydrophobic compounds. By selecting appropriate guest components, polyion complex micelles could also be assembled. These results suggest the potential versatile applications of this type of copolymers in pharmaceutics, nanomedicine, and nano-biotechnology.

A novel and simple spectrophotometric method for the determination of phenformin hydrochloride using sodium nitroprusside as chromogenic reagent is developed in this paper. The experiment indicates that the sodium nitroprusside can react with the phenformin hydrochloride in a basic solution to form a product with colored N-nitrosamines. The stoichiometric ratio of phenformin hydrochloride and sodium nitroprusside is 1:3 in the product. The maximal absorption wavelength (λ max ) of the product is 520 nm, e 520 = 2.2 × 10 3 Lmol -1 cm -1 . A Good linear relationship is obtained between the absorbance (A) and the concentration (C) of phenformin hydrochloride in a wide range of 0.20-400 μg mL -1 . The equation of the linear regression is A = 0.03461 + 0.00907C (μg mL -1 ) with a linear correlation coefficient of 0.9991. The detection limit is 0.13 μg mL -1 , and the relative standard deviation (R.S.D.) is 0.19%. The method is successfully applied to the determination of phenformin hydrochloride in tablet forms, and satisfactory recoveries are obtained.

The increase use of ion sensors in the fields of environmental, agricultural, and medical analysis is stimulating analytical chemists to develop new sensors for fast, accurate, reproducible, and selective determination of various ions. In this study a new samarium membrane sensor was constructed and for the first time, it was applied as a probe in indirect determination of hyoscine, homatropine, and tramadol drugs in their pharmaceutical formulation. The proposed membrane sensor was constructed based on a membrane containing 2% sodium tetraphenyl borate (NaTPB) as an anionic additive, 63% dibutyl phthalate (DBP) as solvent mediator, 5% ionophore, and 30% poly(vinyl chloride) (PVC). The proposed Sm(III) electrode exhibits a Nernstian response of 19.35±0.2 mV per decade of samarium concentration, and has a lower detection limit of 1.0×10−7 M. The linear range of the sensors was 1.0×10−7–1.0×10−1 M. It works well in the pH range of 3.0–8.0.

In the development of new detergent products, it is important to test the foaming behavior of different types of surfactants. Different types and concentrations of surfactant solutions prepared with three types of water are expected to present differences in their foamability. In this study, foam volumes produced by cetyl trimethyl ammonium bromide (CTAB; C19H42BrN), Tween 80® (T80; C64H124O26) and sodium dodecylsulfate (SDS; C12H25NaO4S) aqueous solutions (0.5, 1.0 and 1.5%, w/v) were compared using a stirring system, rotating at 8,000, 9,500 and 13,500 rpm. The foamability produced by CTAB, SDS and T80 solutions, in a concentration range between 0.2 and 1.0% (w/v), prepared using deionized, hard and hypersaline water were also compared. Foam volumes were higher at a stirring speed of 9,500 rpm than at 8,000 rpm. However, the results obtained at 9,500 and 13,500 rpm were not significantly different. In general, SDS solutions produced higher foam volumes than CTAB and T80 solutions. Water characteristics did not seem to influence significantly the foamability of the three types of surfactants in the studied concentrations. These studies related with foaming behavior appear to be an important step in the pre-formulation of detergent products, particularly in cosmetics and pharmaceutics.

Prediction of human response to drugs or chemicals is difficult as a result of the complexity of living organisms. We describe an in vitro model that can realistically and inexpensively study the adsorption, distribution, metabolism, elimination, and potential toxicity (ADMET) of chemicals. A microscale cell culture analog (microCCA) is a physical replica of the physiologically based pharmacokinetics (PBPK) model. Such a microfabricated device consists of a fluidic network of channels to mimic the circulatory system and chambers containing cultured mammalian cells representing key functions of animal "organ" systems. This paper describes the application of a two-cell system, four-chamber microCCA ("lung"-"liver"-"other tissue"-"fat") device for proof-of-concept study using naphthalene as a model toxicant. Naphthalene is converted into reactive metabolites (i.e., 1,2-naphthalenediol and 1,2-naphthoquinone) in the "liver" compartment, which then circulate to the "lung" depleting glutathione (GSH) in lung cells. Such microfabricated in vitro devices are potential human surrogates for testing chemicals and pharmaceutics for toxicity and efficacy.

This paper reviews the production technologies for sourcing lecithins from the oil-bearing seeds soybean, rapeseed and sunflower kernel. The phospholipid composition is measured by newly developed HPLC-LSD and 31P-NMR methods. The phospholipid compositions of the three types of lecithin show small differences, while the fatty acid composition is largely equivalent to the oil source. Regulatory specifications (FAO/WHO, EU, FCC) and DGF and AOCS analytical methods for product quality are compiled. Phospholipid modifications by enzymatic hydrolysis, solvent fractionation, acetylating and hydroxylation processes result in lecithins with specific enhanced hydrophilicity and oil-in-water emulsifying properties. New available phospholipase and lipase enzymes represent opportunities for the esterification of phospholipids with special omega fatty acids and serine groups. Application characteristics are given for use in yellow fat spreads, baked goods, chocolate, agglomerated instant powders, liposome encapsulation, animal feed, food supplements and pharmaceutics.

Molecular modeling techniques have been widely used in drug discovery fields for rational drug design and compound screening. Now these techniques are used to model or mimic the behavior of molecules, and help us study formulation at the molecular level. Computational pharmaceutics enables us to understand the mechanism of drug delivery, and to develop new drug delivery systems. The book discusses the modeling of different drug delivery systems, including cyclodextrins, solid dispersions, polymorphism prediction, dendrimer-based delivery systems, surfactant-based micelle, polymeric drug delivery systems, liposome, protein/peptide formulations, non-viral gene delivery systems, drug-protein binding, silica nanoparticles, carbon nanotube-based drug delivery systems, diamond nanoparticles and layered double hydroxides (LDHs) drug delivery systems. Although there are a number of existing books about rational drug design with molecular modeling techniques, these techniques still look mysterious and daunting for pharmaceutical scientists. This book fills the gap between pharmaceutics and molecular modeling, and presents a systematic and overall introduction to computational pharmaceutics. It covers all introductory, advanced and specialist levels. It provides a totally different perspective to pharmaceutical scientists, and will greatly facilitate the development of pharmaceutics. It also helps computational chemists to look for the important questions in the drug delivery field.

Multisubstituted guanidines have received much attention because of important applications in many fields, such as pharmaceutics, organometallic and coordination chemistry, and organic synthesis. Although classical methods are available for the preparation of guanidines, synthetic preparation approaches to guanidines are still in great demand. In this review, we summarize recent developments on synthetic methods via the C–N bond formation. Three aspects are included: transition-metal-catalyzed guanidine synthesis based on classical methods; catalytic guanylation reaction of amines with carbodiimides; and tandem catalytic guanylation/cyclization reactions.

Protein stability is critical to the outcome of nearly all thermally mediated applications to biomaterials such as thermal therapies (including cryosurgery), burn injury, and biopreservation. As such, it is imperative to understand as much as possible about how a protein loses stability and to what extent we can control this through the thermal environment as well as through chemical or mechanical modification of the protein environment. This review presents an overview of protein stability in terms of denaturation due to temperature alteration (predominantly high and some low) and its modification by use of chemical additives, pH modification as well as modification of the mechanical environment (stress) of the proteins such as collagen. These modifiers are able to change the kinetics of protein denaturation during heating. While pH can affect the activation energy (or activation enthalpy) and the frequency factor (or activation entropy) of the denaturation kinetics, many other chemical and mechanical modifiers only affect the frequency factor (activation entropy). Often, the modification affecting activation entropy appears to be linked to the hydration of the protein. While the heat-induced denaturation of proteins is reasonably well understood, the heat denaturation of structural proteins (e.g., collagen) within whole tissues remains an area of active research. In addition, while some literature exists on protein denaturation during cold temperatures, relatively little is known about the kinetics of protein denaturation during both freezing and drying. Further understanding of this kinetics will have an important impact on applications ranging from preservation of biomaterials and pharmaceutics to cryosurgery. Interestingly, both freezing and drying involve drastic shifts in the hydration of the proteins. It is clear that understanding protein hydration at the molecular, cellular, and tissue level will be important to the future of this evolving area.

Synthetic biology has advanced to contain not only whole cell systems but also cell-free systems. Combined with minimized genome and promoter engineering, synthetic biology can be used to engineer living systems or biomolecular components for production of chemicals, materials or pharmaceutics. The future looks bright!

Biodegradable polymers and the hydrogels have been increasingly applied in a variety of biomedical fields and pharmaceutics. α,β-Poly(N-2-hydroxyethyl-DL-aspartamide), PHEA, one of poly(amino acid)s with hydroxyethyl pendants, are known to be biodegradable and biocompatible, and has been studied as an useful biomaterial, especially for drug delivery, via appropriate structural modification. In this work, hydrogels based on PHEA were prepared by two-step reaction, that is, the crosslinking of polysuccinimide, the precursor polymer, with oligomeric PEG or PEI-diamines and the following nucleophilic ring-opening reaction by ethanolamine. Soft hydrogels possessing varying degrees of gel strength could be prepared easily, depending on the amount of different crosslinking reagents. The swelling degrees, which were in the range of 10–40 g–water/dry gel, increased somewhat at higher temperature, and also at alkaline pH of aqueous solution. A typical hydrogel remained almost unchanged for 1 week, at 37°C in phosphate buffer of pH 7.4, and then seemed to degrade slowly as time. A porous scaffold could be fabricated by the freeze drying of water-swollen gel. The PHEA-based hydrogels have potential for useful biomaterial applications including current drug delivery system. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 3741–3746, 2003

Zein is the major storage protein from corn with strong hydrophobicity and unique solubility and has been considered as a versatile food biopolymer. Due to the special tertiary structures, zein can self-assemble to form micro- and nano-particles through liquid–liquid dispersion or solvent evaporation approaches. Zein-based delivery systems have been particularly investigated for hydrophobic drugs and nutrients. Recently, increasing attention has been drawn to fabricate zein-based advanced drug delivery systems for various applications. In this review, the molecular models of zein tertiary structure and possible mechanisms involved in zein self-assembly micro- and nano-particles are briefly introduced. Then, a state-of-the-art introduction and discussion are given in terms of preparation, characterization, and application of zein-based particles as delivery systems in the fields of food science, pharmaceutics, and biomedicine. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014, 131, 40696.

Transition-metal catalyzed CC bond-forming reaction is a useful and straightforward method for the functionalization of azole heterocycles, [1] which are frequently found as key frameworks in natural products, pharmaceutics, and organic functional materials. [2a] Because the C2 position of 1,3azoles, such as oxazoles, thiazoles, and imidazoles, in many natural and synthetic compounds are alkylated, [2b–g] the development of simple and efficient methods for introducing an alkyl group in this position would be highly desirable for the synthesis of these compounds. The conventional reaction for the alkylation of 1,3-azoles includes the coupling of 2metalated azoles generated beforehand or in situ from the parent unsubstituted 1,3-azole under basic conditions with alkyl electrophiles (Scheme 1, path A) [3, 4] and the coupling

In this article, the applications of CD polymers are presented. The text consists of two parts. In the first one, the applications of CD polymers in environmental protection, especially detoxification from heavy metals and organic contaminants, are described. The second part concerns application of CD polymers in pharmaceutics and cosmetics. Keywords: cyclodextrin polymers; adsorption; drug; environment; wastewater