Influence of shaking culture on the biological functions of cell aggregates incorporating gelatin hydrogel microspheres.

The objective of this study is to investigate the influence of shaking culture on the biological functions of cell aggregates incorporating gelatin hydrogel microspheres in terms of the microspheres/cells ratio. The mixture of MC3T3-E1 cells and the microspheres was cultured in the U-bottomed wells of 96-well plate pre-coated with poly (vinyl alcohol) (PVA) to form cell aggregates incorporating microspheres. When incubated in the static or shaking culture, the size of cell aggregates increased with amounts of gelatin hydrogel microspheres but was similar between the two cultures.

Development of a Transdermal Delivery System for Tenofovir Alafenamide, a Prodrug of Tenofovir with Potent Antiviral Activity Against HIV and HBV.

Tenofovir alafenamide (TAF) is an effective nucleotide reverse transcriptase inhibitor that is used in the treatment of HIV-1 and HBV. Currently, it is being investigated for HIV prophylaxis. Oral TAF regimens require daily intake, which hampers adherence and increases the possibility of viral resistance.

Chitosan Coating Effect on Cellular Uptake of PLGA Nanoparticles for Boron Neutron Capture Therapy.

The usefulness of poly(lactide-co-glycolide) nanoparticles as a boron compound carrier for boron neutron capture therapy has been recently reported. In this study, chitosan-modified poly(DL-lactide-co-glycolide) (PLGA) nanoparticles were prepared to better facilitate the delivery of boron to the tumor. Chitosan hydroxypropyltrimonium chloride (CS), which can easily be modified for compatibility with PLGA nanoparticles, was used as chitosan.

Biocompatibility and effectiveness of paclitaxel-encapsulated micelle using phosphoester compounds as a carrier for cancer treatment.

Phosphoester compounds are promising materials with expected biocompatibility; however, little has been reported on the use of phosphoester compounds for micelle formulations. In this study, paclitaxel (PTX)-encapsulated micelles were prepared using four kinds of alkyl di(MePEG-lactate) phosphates. From the results of the determination of critical micelle concentrations and an in vitro stability test, it was shown that a compound to which 1-eicosanol was introduced as a side chain was desirable in the preparation of PTX-encapsulated micelles (PTX-micelles).

Effects of Novel Calpain Inhibitors in Transgenic Animal Model of Parkinson's disease/dementia with Lewy bodies.

Parkinson's disease (PD) and dementia with Lewy bodies (DLB) are neurodegenerative disorders of the aging population characterized by the accumulation of α-synuclein (α-syn). The mechanisms triggering α-syn toxicity are not completely understood, however, c-terminus truncation of α-syn by proteases such as calpain may have a role. Therefore, inhibition of calpain may be of value.

Therapeutic Effect of GGsTop, Selective Gamma-glutamyl Transpeptidase Inhibitor, on a Mouse Model of 5-Fluorouracil-induced Oral Mucositis.

Background: Oral mucositis (OM) induced by cancer chemotherapy has a high incidence and serious symptoms, which often force chemotherapy to be stopped. GGsTop is a newly-discovered gamma-glutamyl transpeptidase (GGT) inhibitor. Previous research suggested that inhibition of GGT suppressed reactive oxygen species and induced the production of collagen and elastin.

Transdermal delivery of 40-nm silk fibroin nanoparticles.

Transdermal administration of drugs improves their bioavailability and is capable of systemic and local treatment. To improve the skin permeability of drugs, nano-sized systems have attracted attention as drug carriers for transdermal drug delivery system. We considered that silk fibroin composed of a crystalline region with many hydrophobic amino acids and an amorphous region with many hydrophilic amino acids was useful as a carrier for transdermal administration of a drug because of the balance between hydrophilicity and hydrophobicity.

Formulation Development and Characterization of Nanoemulsion-Based Formulation for Topical Delivery of Heparinoid.

Heparinoid is commonly used for the treatment of superficial thrombophlebitis, a condition wherein inflammation and clotting occurs in the veins below the skin surface. However, stratum corneum is a major barrier that limits the delivery of hydrophilic heparinoid, in and across the skin. The aim of the present study was to develop a nonirritant topical formulation for heparinoid incorporating chemical penetration enhancers and investigate the delivery of heparinoid across the human epidermis using in vitro vertical Franz diffusion cells.

Synthesis of Phosphoester Compounds Using Lactic Acid for Encapsulation of Paclitaxel.

Background/aim: In the use of paclitaxel, side-effects caused by itself or solubilizing agents have become a major obstacle. In this study we aimed to synthesize biocompatible and degradable compounds for micelles to be used as carriers for paclitaxel.

Materials And Methods: Methoxypolyethylene glycol-lactate was obtained from methyl lactate and methoxypolyethylene glycol having a molecular weight of 350.

Characterization of rabies pDNA nanoparticulate vaccine in poloxamer 407 gel.

Plasmid DNA (pDNA) vaccines have the potential for protection against a wide range of diseases including rabies but are rapid in degradation and poor in uptake by antigen-presenting cells. To overcome the limitations, we fabricated a pDNA nanoparticulate vaccine. The negatively charged pDNA was adsorbed onto the surface of cationic PLGA (poly (d, l-lactide-co-glycolide))-chitosan nanoparticles and were used as a delivery vehicle.

Therapeutic efficacy of rebamipide-loaded PLGA nanoparticles coated with chitosan in a mouse model for oral mucositis induced by cancer chemotherapy.

Oral mucositis is one of the most common side effects induced by cancer therapy, and the prevention or rapid treatment of the symptoms of oral mucositis can improve patients' quality of life and reduce the need for treatment interruption. In this study, poly(dl-lactide-co-glycolide) (PLGA) nanoparticles coated with chitosan hydroxypropyltrimonium chloride was used as a carrier of rebamipide, and its usefulness was evaluated using a mouse model for oral mucositis. The surface properties and particle size of this nanoparticle were considered to be advantageous for the treatment of oral mucositis.

Decarboxylation of indomethacin induced by heat treatment.

As crystalline indomethacin is heated and subsequently cooled, it transforms into glassy indomethacin. While the original crystals are off-white in color, the glass becomes blackish-brown via a yellow intermediate stage. TLC of the components of the glass revealed three bands.

Push-Pull Controlled Drug Release Systems: Effect of Molecular Weight of Polyethylene Oxide on Drug Release.

First, an elementary osmotic pump (EOP) with a simple structure was prepared using polyethylene oxide (PEO) and NaCl as an excipient, and the influence of the molecular weight (Mw) of PEO on drug release was investigated. In the dissolution test of EOP, it was observed that the gelated core tablet was pushed out through the orifice. The dissolution profile of EOP was sigmoidal, and despite the short time, a zero-order release region was observed.

Minoxidil-encapsulated poly(L-lactide-co-glycolide) nanoparticles with hair follicle delivery properties prepared using W/O/W solvent evaporation and sonication.

Background: Nanoparticles with a diameter of 100-150 nm prepared using poly(lactide-co-glycolide) can be delivered to hair follicles. Moreover, it was shown that drug release from nanoparticles was prolonged by using poly(L-lactide-co-glycolide) (PLLGA).

Objective: The aim of this study was to prepared minoxidil-encapsulated PLLGA nanoparticles and accumulate minoxidil in hair follicles utilizing its drug delivery properties for effective treatment of male and female androgenetic alopecia.

Biodistribution of colloidal gold nanoparticles after intravenous injection: Effects of PEGylation at the same particle size.

Background: Recently, polyethylene glycol (PEG) modified gold nanoparticles have been studied to maintaining long-term stability in biological fluids. Its biodistribution was also reported, however, comparison of bare gold nanoparticles and PEGylated gold nanoparticles with equal particle size is not sufficient.

Objective: We prepared bare gold nanoparticles and PEGylated gold nanoparticles with diameters of 20-30-nm or 50-nm to avoid the influence of particle diameter, and studied their biodistribution in the mouse.

Hydrogels Containing Antibiofilm and Antimicrobial Agents Beneficial for Biofilm-Associated Wound Infection: Formulation Characterizations and In vitro Study.

Bacterial biofilm which adheres onto wound surface is shown to be impervious to antibiotics and this in turn delays wound healing. Previous studies showed that antibiofilm agents such as xylitol and ethylenediaminetetraacetic acid (EDTA) prevent bacterial adherence onto surfaces. Formulation of a wound dressing containing antibiofilm agents may be a plausible strategy in breaking the biofilm on wound surfaces and at the same time increase the efficacy of the antibiotic.

A Mouse Model for Oral Mucositis Induced by Cancer Chemotherapy.

Background: Oral mucositis (OM), one of the side-effects induced by chemotherapy, has 40% incidence and the incidence rate increases to approximately 100% in combination with radiotherapy. We describe OM in ICR mice induced using 5-fluorouracil (5-FU) and 20% acetic acid.

Materials And Methods: We optimized the dose of 5-FU and 20% acetic acid and validated the efficacy of standard therapies for OM.

Coenzyme Q10-Loaded Fish Oil-Based Bigel System: Probing the Delivery Across Porcine Skin and Possible Interaction with Fish Oil Fatty Acids.

Coenzyme Q10 (CoQ10) is a vitamin-like oil-soluble molecule that has anti-oxidant and anti-ageing effects. To determine the most optimal CoQ10 delivery vehicle, CoQ10 was solubilised in both water and fish oil, and formulated into hydrogel, oleogel and bigel. Permeability of CoQ10 from each formulation across porcine ear skin was then evaluated.

Intranasal administration of neuromedin U derivatives containing cell-penetrating peptides and a penetration-accelerating sequence induced memory improvements in mice.

Neuromedin U (NMU) is a neuropeptide that is expressed and secreted in the brain and gut. We previously demonstrated that the intracerebroventricular (i.c.

Iontophoretic transdermal delivery using chitosan-coated PLGA nanoparticles for positively charged drugs.

Recently, poly(dl-lactide-co-glycolide) (PLGA) nanoparticles prepared using a combination of an antisolvent diffusion method with preferential solvation was shown to be beneficial for the iontophoretic transdermal delivery of therapeutic agents. Also, this preparation method can contain a hydrophilic drug. However, since PLGA nanoparticles were negatively charged, it was difficult to apply iontophoresis for positively charged hydrophilic drugs.

Skin permeability and transdermal delivery route of 50-nm indomethacin-loaded PLGA nanoparticles.

Recently, nano-seized systems for transdermal delivery have attracted attention. To efficiently deliver drugs to hair follicles, we focused on poly(DL-lactide-co-glycolide) (PLGA) nanoparticles prepared using a combination of an antisolvent diffusion method with preferential solvation. The PLGA nanoparticles prepared using this method are suitable for iontophoresis because of their high surface charge number density.

Hydrophobic boron compound-loaded poly(l-lactide-co-glycolide) nanoparticles for boron neutron capture therapy.

Poly(DL-lactide-co-glycolide) (PLGA) has been widely used and studied because of its biocompatibility and biodegradability. Recently, the usefulness of nanoparticles using poly(L-lactide-co-glycolide) (PLLGA) having a higher glass transition temperature than PLGA was suggested. In this study, we investigated the availability of boron compound-loaded PLGA and PLLGA nanoparticles for boron neutron capture therapy (BNCT) by conducting biodistribution study using tumor-bearing mice.

Biodistribution and excretion of colloidal gold nanoparticles after intravenous injection: Effects of particle size.

Background: Inorganic gold nanoparticles (NPs) have a huge potential in targeted drug delivery. Simple preparation and surface modification procedure with their special physicochemical properties of gold NPs attract their use such as tumor targeting and the detection of cancerous cell.

Objective: Various studies were reported, however, details of biodistribution profile of gold NPs were not enough evaluated.

Estradiol-loaded PLGA nanoparticles for improving low bone mineral density of cancellous bone caused by osteoporosis: Application of enhanced charged nanoparticles with iontophoresis.

Postmenopausal osteoporosis among older women, which occurs by an ovarian hormone deficiency, is one of the major public health problems. 17 β-estradiol (E2) is used to prevent and treat this disease as a drug of hormone replacement therapy. In oral administration, E2 is significantly affected by first-pass hepatic metabolism, and high dose administration must be needed to obtain drug efficacy.

Antidepressant-like effects exerted by the intranasal administration of a glucagon-like peptide-2 derivative containing cell-penetrating peptides and a penetration-accelerating sequence in mice.

The intracerebroventicular (i.c.v.