The Critical Role of Passive Permeability in Designing Successful Drugs

Passive permeability is a key property in drug disposition and delivery. It is critical for gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance mechanisms and drug-drug interactions. Passive diffusion rate is translatable across tissues and animal species, while the extent of absorption is dependent on drug properties, as well as in vivo physiology/pathophysiology. Design principles have been developed to guide medicinal chemistry to enhance absorption, which combine the balance of aqueous solubility, permeability and the sometimes unfavorable compound characteristic demanded by the target. Permeability assays have been implemented that enable rapid development of structure-permeability relationships for absorption improvement. Future advances in assay development to reduce nonspecific binding and improve mass balance will enable more accurately measurement of passive permeability. Design principles that integrate potency, selectivity, passive permeability and other ADMET properties facilitate rapid advancement of successful drug candidates to patients.     

On‐the‐Spot Immobilization of Quantum Dots,Graphene Oxide,and Proteins via Hydrophobins

Class I hydrophobin Vmh2, a peculiar surface active and versatile fungal protein, is known to self‐assemble into chemically stable amphiphilic films, to be able to change wettability of surfaces, and to strongly adsorb other proteins. Herein, a fast, highly homogeneous and efficient glass functionalization by spontaneous self‐assembling of Vmh2 at liquid–solid interfaces is achieved (in 2 min). The Vmh2‐coated glass slides are proven to immobilize not only proteins but also nanomaterials such as graphene oxide (GO) and quantum dots (QDs). As models, bovine serum albumin labeled with Alexa 555 fluorophore, anti‐immunoglobulin G antibodies, and cadmium telluride QDs are patterned in a microarray fashion in order to demonstrate functionality, reproducibility, and versatility of the proposed substrate. Additionally, a GO layer is effectively and homogeneously self‐assembled onto the studied functionalized surface. This approach offers a quick and simple alternative to immobilize nanomaterials and proteins, which is appealing for new bioanalytical and nanobioenabled applications.     

A new deep convolutional neural network model for classifying breast cancer histopathological images and the hyperparameter optimisation of the proposed model

The Journal of Supercomputing - Deep learning algorithms have yielded remarkable results in medical diagnosis and image analysis, besides their contribution to improvements in a number of fields...     

Partitioning of predominant lipophilic bioactives (squalene, α-tocopherol and β-sitosterol) during olive oil processing

The partitioning of predominant lipophilic olive bioactives (squalene, β-sitosterol and α-tocopherol) in olive oil processing was studied for the first time using common integrated olive milling plant. 7% of the oil and 5% of the squalene present in the olives was lost in the last pomace. β-sitosterol and α-tocopherol, which are mainly concentrated in the seed of the olive fruit, was recovered in virgin olive oil to a lesser extent (66%, 67%) while 10% were lost in last pomace. Thus, the loss of β-sitosterol and α-tocopherol was higher than that of squalene and oil, due to nonrecovered bound forms. 19% of the α-tocopherol and 21% of the β-sitosterol loss was unaccounted for, which can be attributed to degradation of α-tocopherol and incomplete recovery of sterols from the olive and pomace matrices. This study provides a basis for process development studies.     

An MPEG‐4 Compliant Interactive Multimedia Streaming Platform Using Overlay Networks

This paper presents a multimedia streaming platform for efficiently transmitting MPEG‐4 content over IP networks. The platform includes an MPEG‐4 compliant streaming server and client, supporting object‐based representation of multimedia scenes, interactivity, and advanced encoding profiles defined by the ISO standard. For scalability purposes, we employ an application‐layer multicast scheme for media transmission using overlay networks. The overlay network, governed by the central entity of the network distribution manager, is dynamically deployed according to a set of pre‐defined criteria. The overlay network supports both broadcast delivery and video‐on‐demand content. The multimedia streaming platform is standards‐compliant and utilizes widespread multimedia protocols such as MPEG‐4, real‐time transport protocol, real‐time transport control protocol, and real‐time streaming protocol. The design of the overlay network was architected with the goal of transparency to both the streaming server and the client. As a result, many commercial implementations that use industry‐standard protocols can be plugged into the architecture relatively painlessly and can enjoy the benefits of the platform.     

The strategy of edge wear prediction in CIM concept

A monitoring of tool wear in different cutting operations has been studied for many years. Special techniques have been used to detect a wear status basing upon cutting forces, acoustic emission, temperature, torque and power, vibration, noise and acceleration sensors. The adapting of a proper prediction method allows to solve problems of an automatic supervision in Computer Integrated Manufacturing systems. A task of the abrasive edge wear index prediction can be formulated as follows: disposing by the data collection of the edge wear status in a time period preceding the concerning the wear status in the successive time period embraced by the prediction method.     

Evaluation of Monkman-Grant parameters for type 316LN and modified 9Cr-Mo stainless steels

The Monkman-Grant (M-G) and its modified parameters were evaluated for type 316LN and modified 9Cr-Mo stainless steels prepared with minor element variations. Several sets of creep data for the two alloy systems were obtained by constant-load creep tests in 550-650°C temperature range. The M-G parameters,m, m’,C, andC’ were proposed and discussed for the two alloy systems. Them value of the M-G relation was 0.90 in type 316LN steel and 0.84 in modified 9Cr-Mo steel. Them’, value of the modified relation was 0.94 in type 316LN steel and 0.89 in 9Cr-Mo steel. Although creep fracture modes and creep properties between type 316LN and modified 9Cr-Mo steels showed a basic difference, the M-G and its modified relations demonstrated linearity quite well. Them’ of modified relation almost overlapped regardless of the creep testing conditions and chemical variations in the two alloy systems, and the parameterm’ was closer to unity than that of the M-G relation.