Immunohistochemical characterization of transient receptor potential vanilloid types 2 and 1 in a trinitrobenzene sulfonic acid-induced rat colitis model with visceral hypersensitivity.

Transient receptor potential vanilloid type 2 (TRPV2) and type 1 (TRPV1) are originally identified as heat-sensitive TRP channels. We compared the expression patterns of TRPV2 and TRPV1 in the rat distal colon and extrinsic primary afferent neurons, and investigated their roles in visceral hypersensitivity in 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced colitis rats. Both TRPV2 and TRPV1 expressions in the colon, dorsal root ganglion (DRG), and nodose ganglion (NG) were significantly upregulated in the TNBS-induced colitis model.

The Current Concept of Paternal Bonding: A Systematic Scoping Review.

Bonding is crucial to perinatal mental health. Despite an extensive body of literature on maternal bonding, few studies have focused on paternal bonding. This scoping review aimed to clarify the current state of the concept of paternal-infant/fetus bonding.

Self-Assembled Structure of α-Isostearyl Glyceryl Ether Affects Skin Permeability-a Lamellar with 70-nm Spaces and L3 Phase Enhanced the Transdermal Delivery of a Hydrophilic Model Drug.

Self-assembled surfactant structures, such as liquid crystals, have the potential to enhance transdermal drug delivery. In the present study, the pseudo-ternary system of GET (composed of α-Isostearyl glyceryl ether (GEIS) and polysorbate 60)/1,3 butanediol (BG)/water) was shown to exhibit a complex phase diagram. Small- and wide-angle X-ray scattering (SWAXS) and freeze-fracture transmission electron microscopy (FF-TEM) revealed that GET6BG60 (6%GET/60%BG/34%Water) formed a lamellar phase with a repeated distance of approximately 72 nm.

[Transdermal Drug Delivery Systems: From the Dawn and Early Stage to the Development and Maturity Stage, and the Future].

This review describes the analytical methods for percutaneous absorption and skin permeation of chemical substances and the transdermal drug delivery system (TDDS) that I have been researching for about half a century. This period coincides with that of the dawn and early stage of TDDS through its development to the maturity stage. First, as an introduction, the skin structure, definitions of scientific terms such as percutaneous absorption, skin permeation, skin penetration, types of chemical substances that make contact with the skin, and the skin permeation pathway of chemical substances are outlined.

Chitosan-coated PLGA nanoparticles for transcutaneous immunization: Skin distribution in lysozyme-sensitized mice.

The effect of transcutaneous immunization was studied using a combined system of poly(DL-lactide-co-glycolide) (PLGA) nanoparticles and iontophoresis (IP). Both hen egg-white lysozyme (HEL)-loaded PLGA nanoparticles coated with chitosan hydroxypropyltrimonium chloride and their fluorescent nanoparticles were prepared using an antisolvent diffusion method. Their mean volume diameters were 87.

Computational and Crystallographic Analysis of Binding Structures of Inhibitory Compounds for HIV-1 RNase H Activity.

Chemotherapy of human immunodeficiency virus type-1 (HIV-1) has significantly developed over the last three decades. The emergence of drug-resistant variants is, however, still a severe problem. The RNase H activity of HIV-1 reverse transcriptase is an attractive target for a new class of antiviral drugs because there is no approved inhibitor.

Effects of Physicochemical Properties of Constituent Ions of Ionic Liquid on Its Permeation through a Silicone Membrane.

Ionic liquids (ILs), defined as liquid salts composed of anions and cations, have the advantage of allowing constituent ions to be stably absorbed through biological membranes, such as skin. However, limited information is currently available on the effects of the physicochemical properties of constituent ions on the membrane permeation of ILs. Therefore, we herein investigated the effects of the polarity of constituent cations on the membrane permeation of each constituent ion from IL.

Thermoresponsive Polyphosphoester via Polycondensation Reactions: Synthesis, Characterization, and Self-Assembly.

Using a novel strategy, amphiphilic polyphosphoesters based on poly(oxyethylene H-phosphonate)s (POEHP) with different poly(ethylene glycol) segment lengths and aliphatic alcohols with various alkyl chain lengths were synthesized using polycondensation reactions. They were characterized by H NMR, C {H} NMR P NMR, IR, and size exclusion chromatography (SEC). The effects of the polymer structure on micelle formation and stability, micelle size, and critical micelle temperature were studied via dynamic light scattering (DLS).

A Mouse Model for Tuberculosis Combined With Inhalable Imiquimod-PLGA Nanocomposite Particles Based on Macrophage Phenotype.

Background/aim: In vivo models of tuberculosis are effective tools for developing new drugs. The objective of this study was to prepare in vivo models for tuberculosis by utilizing nanocomposite particles (NCPs) containing imiquimod-loaded poly(lactic-co-glycolic acid) nanoparticles.

Materials And Methods: NCPs were prepared from dichloromethane with imiquimod and poly(lactic-co-glycolic acid) using a spray dryer.

Association between Bone-Related Physiological Substances and Oral Function in Community-Dwelling Older People.

Background: Oral dysfunction is related to long-term cares including activities of daily living. The objective of this study was to determine the association between oral function and the bone-related physiological substances osteocalcin (OC) and insulin-like growth factor-1 (IGF-1).

Methods: The study participants were 139 community-dwelling older people in Japan.

[Repellent Activity of Vanillin Derivatives and Monoterpenes to Olive Weevil].

Olive weevils, Pimelocerus (Dyscerus) perforatus Roelofs, utilize olive trees as a host plant. The adult female uses an elongated snout to puncture the trunk and lay one egg a day, resulting in dozens of eggs over its lifetime. The hatched larvae grow by eating the olive trunk.

Development of a Scale for COVID-19 Stigma and Its Psychometric Properties: A Study among Pregnant Japanese Women.

Background: Stigma towards COVID-19 may negatively impact people who suffer from it and those supporting and treating them. Objective: To develop and validate a scale to assess 11-item COVID-19−related stigma. Methods: A total of 696 pregnant women at a gestational age of 12 to 15 weeks were surveyed using an online survey with a newly developed scale for COVID-19 stigma and other variables.

Simulations of the Diffusion of Innovation by Trust-Distrust Model Focusing on the Network Structure.

The purpose of this study is to examine the role of interaction between mass media and people in the diffusion of innovation using the Trust-Distrust model, one of the theories of opinion dynamics. Therefore, in this study, we ran simulations using the Trust-Distrust model to confirm the differences in opinion distribution across different network structures. We used the five adopter categories as the agents of the Trust-Distrust model and applied the random network, scale-free network, and small-world network as the networks for simulation.

Cluster Gauss-Newton method analyses of PBPK model parameter combinations of coproporphyrin-I based on OATP1B-mediated rifampicin interaction studies.

Coproporphyrin I (CP-I) is an endogenous biomarker supporting the prediction of drug-drug interactions (DDIs) involving hepatic organic anion transporting polypeptide 1B (OATP1B). We previously constructed a physiologically-based pharmacokinetic (PBPK) model for CP-I using clinical DDI data with an OATP1B inhibitor, rifampicin (RIF). In this study, PBPK model parameters for CP-I were estimated using the cluster Gauss-Newton method (CGNM), an algorithm used to find multiple approximate solutions for nonlinear least-squares problems.

A Mathematical Approach Using Strat-M to Predict the Percutaneous Absorption of Chemicals under Finite Dose Conditions.

Estimation of the percutaneous absorption is essential for the safety assessment of cosmetic and dermopharmaceutical products. Currently, an artificial membrane, Strat-M, has been focused on as the tool which could obtain the permeation parameters close to the skin-derived values. Nevertheless, few practical methodologies using the permeation parameters for assessing percutaneous absorption under in-use conditions are available.

Clinical significance and safety of combined treatment with chemotherapy and pulmonary rehabilitation regarding health-related quality of life and physical function in nontuberculous mycobacterial pulmonary disease.

Background: In the treatment of patients with nontuberculous mycobacterial pulmonary disease (NTM-PD), pulmonary rehabilitation (PR) has been recommended as a non-pharmacological therapy. However, no study has validated the combination of chemotherapy and PR in this context. This study investigated the effect of chemotherapy and supervised PR on health-related quality of life (HRQoL) and physical function in NTM-PD patients.

Frequency of null genotypes of glutathione S-transferase M1 and T1 in Japanese patients with drug-induced liver injury.

Aim: Previous reports suggest that the null genotype (*0/*0) of glutathione S-transferase (GST) M1 and/or GSTT1 could be risk factors for drug-induced liver injury (DILI). However, multi-institutional pharmacogenetic research with various suspected drugs has rarely been performed in Japan. Therefore, the aim of this study was to investigate the role of GSTM1 and GSTT1 null genotype in the occurrence of DILI in Japanese patients.

High-throughput muscle fiber typing from RNA sequencing data.

Background: Skeletal muscle fiber type distribution has implications for human health, muscle function, and performance. This knowledge has been gathered using labor-intensive and costly methodology that limited these studies. Here, we present a method based on muscle tissue RNA sequencing data (totRNAseq) to estimate the distribution of skeletal muscle fiber types from frozen human samples, allowing for a larger number of individuals to be tested.

Preparation of Micelles Encapsulating Doxorubicin and Their Anticancer Effect in Combination With Tranilast in 3D Spheroids and .

Background/aim: The objective of this study was to prepare doxorubicin encapsulated in micelles (DOX-micelles) using poly(hexadecanyloxyethylene glycol-lactate phosphate), which we recently synthesized, and to evaluate the anticancer effect of DOX-micelles in vitro and in vivo.

Materials And Methods: To evaluate the anticancer effect of DOX-micelles in vitro, three-dimensional spheroids composed of B16 mouse melanoma cells and fibroblasts were prepared by changing the ratio of cancer cells to fibroblasts. In addition, for efficient doxorubicin treatment of the cells present in the center of the spheroids, tranilast, an anti-fibrotic drug was added to the spheroids before treatment with DOX-micelles, then the amount of doxorubicin and cell viability of spheroids were evaluated.

Clinical Relevance of Hepatic and Renal P-gp/BCRP Inhibition of Drugs: An International Transporter Consortium Perspective.

The role of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) in drug-drug interactions (DDIs) and limiting drug absorption as well as restricting the brain penetration of drugs with certain physicochemical properties is well known. P-gp/BCRP inhibition by drugs in the gut has been reported to increase the systemic exposure to substrate drugs. A previous International Transporter Consortium (ITC) perspective discussed the feasibility of P-gp/BCRP inhibition at the blood-brain barrier and its implications.

Effects of 1-day e-learning education on perinatal psychological support skills among midwives and perinatal healthcare workers in Japan: a randomised controlled study.

Background: Although midwives are expected to play a key role for psychological support throughout perinatal periods, their educational chances are limited. Versatile teaching strategies such as e-learning may be promising in expanding education. The objective of our study was to clarify the effects of an e-learning educational programme on midwives' empathic communication skills.

Robust physiologically based pharmacokinetic model of rifampicin for predicting drug-drug interactions via P-glycoprotein induction and inhibition in the intestine, liver, and kidney.

P-glycoprotein (P-gp) is an efflux transporter that plays an important role in the pharmacokinetics of its substrate, and P-gp activities can be altered by induction and inhibition effects of rifampicin. This study aimed to establish a physiologically based pharmacokinetic (PBPK) model of rifampicin to predict the P-gp-mediated drug-drug interactions (DDIs) and assess the DDI impact in the intestine, liver, and kidney. The induction and inhibition parameters of rifampicin for P-gp were estimated using two of seven DDI cases of rifampicin and digoxin and incorporated into our previously constructed PBPK model of rifampicin.

Transporters in Drug Development: International Transporter Consortium Update on Emerging Transporters of Clinical Importance.

During its fourth transporter workshop in 2021, the International Transporter Consortium (ITC) provided updates on emerging clinically relevant transporters for drug development. Previously highlighted and new transporters were considered based on up-to-date clinical evidence of their importance in drug-drug interactions and potential for altered drug efficacy and safety, including drug-nutrient interactions leading to nutrient deficiencies. For the first time, folate transport pathways (PCFT, RFC, and FRα) were examined in-depth as a potential mechanism of drug-induced folate deficiency and related toxicities (e.